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S.Muthukumar /ABARAJITHA.T
Assistant Professor/IIIrd
YEAR B.PHARM
Student
KMCH COLLEGE OF PHARMACY,
COIMBATORE.
Dept. of Pharmaceutics
DrugDrug
 Drug may be defined as an
agent or substance, intended
for use in the diagnosis,
mitigation, treatment, cure or
prevention of disease in
human beings or animals.
 Drugs are rarely administered
in their original or crude
forms. They are administered
in different dosage forms by
converting them into suitable
formulations.
Crude Drugs
Dosage FormsDosage Forms
 Dosage forms are the carrier through which
drug molecules are delivered to sites of
action within the body.
 Every dosage forms is a combination of the
drug and different kinds of non – drug
components called as Excipients or additives.
 The additives are used to give a particular
shape to the formulation, to increase
stability, palatability & more elegance to
preparations.
Need For Dosage FormsNeed For Dosage Forms
 Accurate dose.
 Protection e.g. coated tablets, sealed ampules.
 Protection from gastric juice, e.g. enteric
coated tablets.
 Masking unpleasant taste and odour.
 Provide drugs within body tissues, e.g.
injection
 Sustained release medication.
 Facilation of Insertion of drugs into body
Provide optimum drug action through
inhalation therapy.
Provide drug action through topical
administration at local area of body. e.g.
creams, ointment, emulsion, lotions etc.
Use of desired vehicle for insoluble drugs.
ClassificationClassification
Solid dosage
forms
Unit dosage
forms
Tablets
Capsule
Powders
Pills
Bulk
Internal
Fine powders &
granules
External
Dusting powders
Insufflations
Dentifrice
Snuffs
Ear powders
Liquid dosage
forms
Biphasic
Emulsion
Suspension
Monophasic
Internal External
Syrups
Elixirs
Linctus
Drops
Liniments
Lotions
Gargles
Throat paints
Mouth washes
Sprays
Eye lotions
Eye drops
Nasal drops
Semi solid dosage
forms
Internal External
Suppositories
Pessaries
Ointment
Creams
pastes
Jellies
Solid dosage forms
Solid dosage formsSolid dosage forms
Tablets Pills
Dusting Powders
Capsules
Granules
 SOLID DOSAGE FORMS
 Solid dosage forms one of the oldest dosage forms
and most of the solid dosage forms are available in
Unit dose.
 Unit dose may be defined as a exact quantity of the
drug administered at once. e.g. Tablets, Capsule, pills,
cachets, powders etc.
 When drugs are to be administered orally in dry state,
then tablets, capsules are most convenient dosage
forms.
 Some solids are supplied in bulk (Means quantity
available in large). Bulk powders can be supplied as
Internal (Granules, Fine powders) as well as External
(Dusting Powders, Insufflations etc)
Dusting PowdersDusting Powders
 Dusting powders are applied externally to skin, so
they should be applied in very fine state to avoid local
irritation. Hence dusting powders should be passed
through sieve no 80 to obtained fined powders.
 Dusting powders are prepared by mixing of more than
one ingredients in which either starch, kaolin, or talc
are used in their formulation. Generally talc or kaolin
are used because they are inert in nature.
 Dusting powders are used for antiseptic, astringent,
absorbent, antiperspirant etc.
 Dusting powders are of two sub type they are as
I) Medical dusting powder
II) Surgical Dusting powders
Medical Dusting PowdersMedical Dusting Powders
Medical Dusting powders are used to
increase superficial condition of skin.
These are not applied on wounds, burns etc
Medical dusting powders must be free from
dangerous pathogenic micro- organism.
Surgical Dusting PowdersSurgical Dusting Powders
Surgical dusting powders are used in body
cavities and also on major wounds like as
burns etc.
They should be sterilized before use.
They are mainly used for their antiseptic,
absorbent action.
InsufflationsInsufflations
 These are medicated dusting powders meant for
introduction into body cavities (nose, throat, ear,
vagina etc) with the help of an apparatus known as a
insufflator.
 It sprays the powders (in a state of fine particles) on
site of application.
 Now a days insufflations are also available in pressure
aerosols. This pressure aerosols are used for
administration of potent drug.
 They are used in the treatment of ear, nose, throat
infections with antibiotics to produce local effect of
drugs.
SnuffsSnuffs
These are finely divided solid dosage
forms of medicaments which are inhaled
into nostrils.
They are mainly used for their antiseptic,
bronchodilator and decongestion action.
GranulesGranules
 Granulation is the process in which primary
powder particles are made to adhere to form
larger multiparticle or large particles entities
called granules.
 The bitter, nauseous, unpleasant powders can
not be given tablets, capsule due to bulk
quantity are required to be taken, as well as
they are not given in liquid dosage forms due to
their stability such powders are given in the
granules forms.
 These powders are mixed with suitable
exicipent along with granulating agent, prepare
a coherent mass then dried & passed through
the sieve to obtained desired size of granules.
 E.g. Effervescent granules
Effervescent GranulesEffervescent Granules
 Effervescent granules are meant for internal use.
 They contained medicaments mixed with citric acid,
tartaric acid & sodium bi carbonates, sometime
saccharin or sucrose may be added for sweetening
taste.
 Before, administration desired quantity of granules are
dissolved in water, the acid & bicarbonate reacts with
each other to produce effervescence.
 Effervescent granules are prepared by two methods,
namely as, I) Heat method, II) Wet method
Heat methodHeat method
 A large porcelain or stainless steel evaporating dish is placed over
the boiling water bath.
 The dish must be sufficiently hot (generally heating takes place for
1 – 5 min.) before transferring the powders into it, to ensure rapid
liberation of water of crystallization from citric acid.
 If heating of the dish is delayed then the powder which is added to
it, will heat up slowly & liberated water of crystallization will also
be liberated simultaneously.
 As a result, sufficient water will not be available to make a
coherent mass.
 This coherent mass will pass through the sieve to obtained suitable
size of granules, dry it in oven at 600
c then packed in air tight
container.
Wet methodWet method
 In this methods all the ingredients are mixed thoroughly
 This powders mixture make moistened with non –
aqueous vehicle (e.g. alcohol), to prepare a coherent
mass which is then passed through sieve no 8 to
obtained suitable granules.
 Then dried in oven at 600
c. The dried granules are again
passed through the sieve to break the lumps which may
be formed during drying.
 The dried granules are packed in air tight container.
TabletsTablets
 These are solid dosage forms of medicaments which are
prepared by moulding or by compression with or
without Excipients.
 The tablets can be prepared by two methods namely as
I) Dry granulation
II) Wet Granulation
CapsuleCapsule
 Capsules are solid unit dosage forms in which one or more
medicaments enclosed within a shell.
 Capsules mainly divided in to two parts namely as –
I) Body (Longest part of capsule shell), II) Cap (Smallest part of
capsule shell)
 The capsule are generally prepared by gelatin.
 Depending on their formulation, two types of gelatin are used
namely as – I) Hard gelatin, II) Soft gelatin.
Body
Cap
PillsPills
 These are small, rounded solid dosage forms
containing medicaments intended for oral use.
 The medicaments are mixed with excipients to forms
a firms plastic mass.
 The mass is rolled to uniform pill pipe, which cut into
numbers of uniform pills. The pills are spherical in
shape & produced by rolling them under wooden pill
rounder.
 Sometimes pills are coated with varnish, gold leaf, etc
to improve finish, unpleasant taste & stability.
 Now a days pills are outdated preparations because of
number of disadvantages such as -
 Disintegration time of pill is uncertain means freshly prepared
pills are disintegrates readily rather than old dried pills.
 It is difficult to prepare pills of uniform size & weight.
Liquid dosage forms
Liquid dosage formsLiquid dosage forms
 It may be defined as “A solution is a liquid-preparation that
contains one or more soluble chemical substances dissolved
in a specified solvent”
 Liquid dosage forms are intended for External, Internal or
parenteral use.
 The component of the solution which is present in a large
quantity is known as “SOLVENT” where as the component
present in small quantity is termed as “SOLUTE”
 They mainly classified in to two category namely as –
I) Monophasic Liquid dosage forms.
II) Biphasic liquid dosage forms.
AdvantagesAdvantages
 Immediately available for absorption.
 Administration convenient, particularly for infants, psychotic
patients.
 Easy to color, flavor & sweeten.
 Liquids are easier to swallow than solids and are therefore
particularly acceptable for pediatric patient.
 A solution is an homogeneous system and therefore the drug
will be uniformly distributed throughout the preparation.
 Some drugs like aspirin, KCl can irritate gastric mucosa if
used orally as a solid dosage forms. But this effect can be
reduce by solution system.
DisadvantagesDisadvantages
 Less stable in aqueous system. Incompatibility is faster in
solution than solid dosage form.
 Patients have no accurate measuring device.
 Accident breakage of container results in complete loss.
 Solution often provide suitable media for the growth of micro
organisms.
 The taste of a drug, which is often unpleasant, is always more
pronounced when in solution than in a solid form.
 Bulky than tablets or capsule, so difficult to carry transport.
Monophasic liquid dosage formsMonophasic liquid dosage forms
 Monophasic liquid dosage forms are represent by true or
colloidal solution.
 The component of the solution which is present in a large
quantity is known as “SOLVENT” where as the component
present in small quantity is termed as “SOLUTE”.
 A solution is homogenous because the solute is an ionic or
molecular forms of subdivision.
 In case of colloidal solutions, the solutes are present as
aggregates although they cannot be seen by necked eye or
ordinary microscope.
 It is sub classified as –
I) Internal Use, II) External use
Monophasic Liquid Dosage
forms
Internal Use External Use
 Syrup
 Elixirs
 Linctuses
 Drops
 Liniments
 Lotions
 Gargles
 Mouth Wash
 Throat paints
 sprays
 Inhalations
 Nasal drops
 Eye drops
 Eye lotions
 Ear drops
SyrupSyrup
 It is a concentrated or saturated solutions of sucrose in
purified water.
 The concentration of sucrose is 66.7% w/w & due to that it is
a viscous preparations.
 The syrup which contains medical substance called as a
medicated syrup & those containing aromatic or flavored
substance known as a flavored syrup.
Importance of syrupImportance of syrup
 It retards oxidation because its partly hydrolyzed into
reducing sugar.
 It prevents decomposition of many vegetable substance
because its have high osmotic pressure which prevent the
growth of bacteria.
 They are palatable due sweet taste.
ElixirsElixirs
 It is clear, sweetened, aromatic,
hydroalcholic preparations meant
for oral use.
 The medicated elixirs are generally
contained potent drug like as
antibiotics, antihistamine or sedative
, where as non – medicated elixirs
contained flavoured.
 The composition of elixirs
contained mainly as ethyl alcohol
(active ingredients),water, glycerin
or propylene glycol, colouring agent,
flavouring agent & preservative.
LinctusesLinctuses
 These are viscous liquid preparations
that’s are used for the treatment of
cough.
 They contain medicaments which have
demulcent, sedative, expectorant action.
 They are taken in small doses without
diluting with water to have prolonged
effect of medicines.
 Simple syrup is used as a vehicle for most
of the linctuses.
 Tolu syrup is preferred in certain cases
because of its aromatic odour & flavour.
Moreover it have a mild expectorant
action
DropsDrops
 These are liquid preparations meant for oral
administration.
 The oil soluble vitamins, such as vitamin A & D
concentrates in fish – liver oil are presented as drops
for administration.
 Since these preparations contain potent medicaments,
the dose must be measured accurately
 The following two methods are commonly used for this
purpose.
 Use of a dropper which is accurately graduated in
fractions of a milliliters.
 Use of a pre – calibrated dropper.
LinimentsLiniments
 Liniments are liquid or semi- liquid preparations
meant for external application to the skin.
 They are usually applied to the skin with friction
& rubbing of the skin.
 Are usually alcoholic and oily liquid preparations
(monophasic) or emulsion (biphasic).
 Alcoholic liniments are used generally for their
rubefacient and counterirritant effects. Such
liniments penetrate the skin more readily than
do those with an oil base.
 The oily liniments are milder in their action and
may function solely as protective coatings
 Liniments should not be applied to skin that are
bruised or broken.
LotionsLotions
 Are usually aqueous, alcoholic or
oily liquid preparations.
 They are intended for external
application without friction or
rubbing to the affected area
 Usually applied with the help of
some absorbent material such as
cotton wool or gauze.
 It is generally used to provide
cooling, soothing and protective &
antiseptic action.
GarglesGargles
 Gargles are aqueous solutions used for treating throat infection
(pharynx and nasopharynx part)
 Supplied in concentrated forms with directions of dilution with warm
water before use
 They are used into intimate contact with the mucous membrane of
throat for few seconds, before they are thrown out of the mouth.
 They are used to relieve soreness in mild throat infection.
 They are also used for their antiseptics, antibiotics and/or anesthetics
Mouth washMouth wash
 These are aqueous solutions with
pleasant or acceptable taste & odour
 These are used to make clean &
deodorise the buccal cavity or used
for oral hygiene and to treat
infections of the mouth.
 They mainly contain antibacterial
agent, alcohol, glycerin, sweetening
agent, flavoring agent & colouring
agent.
Throat paintsThroat paints
 Throat paints are viscous liquid
preparations used for mouth and
throat infections
 Glycerin is commonly used as a
base because being viscous it
adheres to mucous membrane for
long period and it possess a sweet
taste.
SpraysSprays
 These are the preparations of drugs in media
which may be aqueous, alcoholic, or glycerin.
 They are applied to the mucous membrane
of throat or nose with an atomizer.
 The throat sprays must be sprayed from a
special type of atomizer known as a
nebulizer, which removes the large droplets
by baffling system. Only precaution should be
taken that the fine droplet will used to easily
reach the lungs.
Nebulizer
InhalationsInhalations
 These are liquid preparations containing volatile substance & are used to
relieve decongestion & inflammations of respiratory tract.
 The volatile substance in inhalations would be volatile at room
temperature so that they should be placed on some adsorbent pad or
handkerchief.
 In some cases inhalations will added to hot water (650
c) then vapors will
inhaled.
Nasal dropsNasal drops
 Drugs in solution may be instilled into the nose from a dropper or
from a plastic squeeze bottle.
 The drug may have a local effect, e.g. antihistamine, decongestant.
 Alternatively the drug may be absorbed through the nasal mucosa
to exert a systemic effect.
 The use of oily nasal drops should be avoided because of possible
damage to the cilia of the nasal mucosa & if it is used for long
period may reach the lungs & cause lipoid pneumonia.
 To avoid that Nasal drops are prepared so that they are similar in
many respects to nasal secretions, so that normal ciliary action is
maintained thus aqueous nasal solutions usually are isotonic and
slightly buffered to maintain a pH of 5.5 to 6.5.
Eye dropsEye drops
 Sterile, aqueous/oily solutions or suspensions intended for
instillation in eye sac.
 Eye drops may contain buffers, stabilizing agents, dispersing agents,
solubilising agents, anti-oxidants & agents required for tonicity/
viscosity adjustment
 Single dose container should not contain anti-microbial
preservative.
 In case of multi dose container a dropper should be supplied with
it for administration. Maximum size of such containers is 10 ml.
Eye lotionsEye lotions
 These are the aqueous solutions used for washing the eyes.
 These are supplied in concentrated forms & are required to diluted with
warm water immediately before use.
 They should be free from foreign particles to avoids irritation to the
eye.
 They are required to prepared fresh & should not be stored for more
than two days to avoid microbial contaminations.
Ear dropsEar drops
 These are the solutions of drugs that are instilled into ear cavity with the
help of dropper.
 These are generally used for cleaning the ear, softening the wax & for
treating the mild infections.
 The solutions is generally prepared in water, glycerin, propylene glycol &
dilute alcohol.
Biphasic liquid dosage formsBiphasic liquid dosage forms
 The liquid which consist of two phases are known as a biphasic
liquid dosage forms.
 They are sub categorized into two different forms namely as –
I) Emulsion
II) Suspension
 In emulsion both phases are available in liquid where as in
suspension, finely divided solid particles are suspended in liquid
medium.
EmulsionEmulsion
 Emulsion is a biphasic liquid preparations containing two immiscible
liquid (Continuous Phase & dispersed phase) made missicible.
 The liquid which is converted into minute globules is called as dispersed
phase & the liquid in which the globules are dispersed is called the
continuous phase
dispersed phase
continuous phase
Two Immiscible Liquids
Dispersed Phase
(Internal phase)
Continuous Phase
(External phase)
 An emulsion is a thermodynamically unstable system consisting of at least
two immiscible liquid phases one of which is dispersed as globules in the
other liquid phase stabilized by a third substance called emulsifying agent.
The globule size in emulsion varies from 0.25 to 25 µm.
Examples for emulsions:- milk, rubber latex, crude oil etc.
A.: Two immiscible liquids not emulsified
B. An emulsion of phase B dispersed in Phase A
C. Unstable emulsion slowly separates.
D. The emulsifying agent ( black film) places it self on the interface between
phase A and phase B and stabilizes the emulsion.
Types of emulsionsTypes of emulsions
Simple type
Water in oil (w/o)
Oil in water (o/w)
Depending on globule size
Micro emulsion
Fine emulsion
Special type
Multiple emulsion (w/o/w, o/w/o)
Water in oil (w/o)Water in oil (w/o)
 In this types of emulsion water is dispersed phase & oil is continuous
phase
 w/o types of emulsion generally meant for External use.
 Examples are butter, lotions, creams etc.
 In rare case they are used internally.
Water is dispersed
phase
Oil is continuous phase
Oil in water (o/w)Oil in water (o/w)
 In this types of emulsion oil is dispersed phase & water is continuous
phase
 o/w types of emulsion meant for both Internal use & External use.
 Examples for internal use are Vitamin A in corn oil, liquid paraffin in
water etc.
 Examples for External use are Benzyl benzonate emulsion.
Oil is dispersed phase
water is continuous phase
Micro EmulsionMicro Emulsion
 These are clear dispersions of o/w or w/o in which the globules have small
size like as a 10nm or 0.01 µm..
 Being cleared products micro emulsion are more popular now a days.
 Micro emulsions are thermodynamically stable optically transparent ,
mixtures of a biphasic oil –water system stabilized with surfactants.
Fine emulsionFine emulsion
 Normally these have a milky appearance.
 The globule size ranges from 0.25 to 25 µm.
Multiple emulsionMultiple emulsion
 These are emulsion with in emulsion & designated as w/o/w or
o/w/o.
 The drugs that is incorporated in the innermost phase must cross
two phase boundaries before getting absorbed.
 It is generally used in oral sustained release or intramuscular
therapy.
The following methods are used for the preparation of emulsions on a
small scale.
1.Dry gum method
2. Wet gum method
3. Bottle method
4. Other methods
Dry gum method:
1.Measure the required quantity of oil in a dry measure and transfer in to
mortar.
2.Add calculated quantity of gum acacia in to mortar and triturate to form a
uniform mixture.
3.Add water and triturate vigorously till the clicking sound is produced in the
product becomes white.
4.The emulsion produced this stage is known as primary emulsion.
5.Ratio of oil water gum
 Fixed oil-4:2:1(Caster oil, Arachis oil)
 Volatile oil-2:2:1(Peppermint oil, Cinnamon oil)
 Mineral oil-3:2:1(Liquid paraffin)
Ex: Arachis oil emulsion
Wet gum method:
1.Powder the gum acacia in in a mortar. Add water and triturate it with gum
so as to form a mucillage.
2.Add the required quantity of oil in small proportions with rapid trituration
until the clicking sound is produced and the water becomes white.To get a
primary emulsion
3.Add more water and triturate to produced required volume.Stirr thoroughly
so as to form a uniform emulsion.
Ex: Caster oil emulsion
Bottle Method:
 It is used for the preparations of volatile and other non-viscous oils.
 Measure the oil and transfer in to large bottle.
 Add required quantity of gum acacia.
 Shake the bottle vigorously until oil and gum mixed thoroughly.
 Add water and shake the mixture vigorously to form a primary emulsion.
Other Methods:
 Various blenders and homogeniser used for preparing emulsions.
 Hand homogeniser,colloidal mill are some of the homogeniser used for the
preparations of emulsions.
 The principle is large globules coarse emulsion are broken in to smaller
globules by passing them under pressure.
 A coarse emulsion is prepared in a mortar which is transferred in to hand
homogeniser.
Dilution test
Conductivity test
Dye test
Fluorescence test
Cobalt chloride test
Filter paper test
Dilution testDilution test
 The emulsion is diluted with water, after dilution emulsion remain stable
then it is said to be o/w type of emulsion because water is in continuous
phase. If emulsion is break after dilution with water then it is said to be
w/o type of emulsion.
Add drops of water
Water distribute
Uniformly
Add drops of water
O/W Emulsion W/O Emulsion
Conductivity testConductivity test
 Conductivity test can be performed by dipping a pair of electrode
connecting with low voltage bulb & pass the current.
 If bulb glows then it is said to be o/w type of emulsion because water is
in continuous phase & it is good conductor of electricity.
 If bulb doesn't glow then it is said to be w/o type of emulsion because oil
is bad conductor f electricity.
Bulb glows with O/W
Emulsion
Emulsion
Bulb doesn’t glow with W/O
Dye testDye test
 Oil soluble Scarlet red dye is mixed with emulsion.
 Place a drop of emulsion on microscopic slide cover it with cover
slip & examine under microscope.
 If disperse globules appears red & ground is colourless then it said
to be o/w type of emulsion because water is present in continuous
phase.
 If reserve condition occurs (If disperse globules appears colourless
& ground is red colour then it said to be w/o type of emulsion
because oil is present in continuous phase.)
Oil is dispersed phaseWater is
continuous phase
Water is disperse phase
Oil is continuous
phase
Fluorescence testFluorescence test
 Certain fixed oil posses the physical properties of fluorescing in the
presence of ultraviolet radiations.
 If examine under microscope ground is fluorescence then it said to be
w/o type of emulsion because oil is present in continuous phase.
 If examine under microscope droplet is fluorescence then it said to be
o/w type of emulsion because oil is present in disperse phase.
Creaming testCreaming test
 The direction of creaming identifies the emulsion type, if the densities
of aqueous and oil phases are known.
 Water-in-oil emulsions normally cream downward as oil is usually less
dense than water.
 Oil-in-water emulsions normally cream upwards.
Cobalt chloride testCobalt chloride test
 Pour the emulsion on filter paper then it is soaked in cobalt chloride
solutions & allowed to dry turns from blue to pink.
 Then this emulsion is said to be o/w type of emulsion.
 This test may fail if emulsion unstable or breaks in presence of
electrolyte.
Filter paper testFilter paper test
 This test is based on the fact that an o/w emulsion will spread out
rapidly when dropped onto filter paper.
 In contrast, a w/o emulsion will migrate only slowly. This method
should not be used for highly viscous creams.
SuspentionSuspention
 Suspensions are the biphasic liquid dosage forms
of medicament in which finely divided solid
particles ranging from 0.5 to 5 micron are
dispersed in a liquid or semisolid vehicle, with
aid of single or combination of suspending
agent.
 In which solid particles acts as disperse phase
where as liquid vehicle acts as continuous phase
 The external phase (suspending medium) is
generally aqueous in some instance, may be an
organic or oily liquid for non oral use.
 The particle size for non oral suspension is so
important to avoid grittiness to skin.
Advantage of suspensionAdvantage of suspension
 Suspension can improve chemical stability of certain drug. E.g.
Procaine penicillin
 Drug in suspension exhibits higher rate of bioavailability than other
dosage forms.
Solution > Suspension > Capsule > Compressed Tablet >
Coated tablet
 Duration and onset of action can be controlled. E.g. Protamine
Zinc-Insulin suspension.
 Suspension can mask the unpleasant/ bitter taste of drug. E.g.
Chloramphenicol
Disadvantage of suspensionDisadvantage of suspension
 Physical stability , sedimentation and compaction can causes problems.
 It is difficult to formulate.
 Uniform and accurate dose can not be achieved unless suspension are
packed in unit dosage form.
 All suspensions are required to be shaken before measuring of dose.
 The storage of suspension may lead to changes in disperse system
especially, when there is fluctuations in temperatures.
Ideal qualities of good suspensionIdeal qualities of good suspension
 It should settle slowly & easily re – dispersed on shaking
 It should readily & evenly pour from container.
 It should be chemically inert.
 It should not forms hard cake.
 It should prevent degradation of drug or to improve stability of drug.
 It should mask the taste of bitter of unpleasant drug.
Ideal qualities of good suspensionIdeal qualities of good suspension
 It should settle slowly & easily re – dispersed on shaking
 It should readily & evenly pour from container.
 It should be chemically inert.
 It should not forms hard cake.
 It should prevent degradation of drug or to improve stability of drug.
 It should mask the taste of bitter of unpleasant drug.
2.On the basis of proportion of solids:
i)Dilute suspension:
 It comprise of 2-10%W/V of solid constituents.
e.g:. Prednisolone acetate
ii) Concentrated suspension:
 It comprise of 50%W/V of solid constituents.
e.g:. External and Parenteral application.
3. On the basis of nature and behavior of solids:
i) Flocculated suspensions:
 The system involves chemical bridging between the particles to form
aggregates.
 Weak van der waal attraction forces are present in between these light and
fluffy aggregates.
 Aggregation can be facilitated through adding flocculating agents.
 Flocculation can be attained by adding extra anions.
Flocculated suspensionFlocculated suspension
 In this type, solid particles are loosely aggregates themselves, means
individual particles are come in contact with each other to forms network
like structure called as a floccules.
 These flocs are light, fluffy in nature, which are held together by weak van
der waals force of attraction.
 Aggregation is achieved by adding flocculating agent.
 This suspension will readily sediments.
 This suspension posses better physical stability but less bioavailability as
compared to deflocculated suspension due to dissolution of floccules.
Deflocculated suspensionDeflocculated suspension
 In this type of suspension, individual particle exits as a separate entity, means
particles carry a finite charges on their surface . Hence particles approaches
each other, they experience repulsive forces. This force create a high
potential barrier, which prevents a aggregation of particles.
 During storage, these suspension shows a sedimentation at slow rate, due to
that particles forms a close packing arrangement.
 So that it is difficult to re dispersed on agitation & forms a cake or claying
which is hard in nature.
 This type of suspension have shorter shelf life but high bioavailability as
compared to flocculated suspension.
Difference between flocculated & deflocculated suspensionDifference between flocculated & deflocculated suspension
Flocculated Suspension Deflocculated suspension
Particles form loose aggregates & forms
network like structure.
Particle exist as separate entities.
Particles experience attractive forces. Particles experience repulsive forces.
Supernatant liquid is clear. Supernatant liquid is cloudy.
The rate of sediment is high. The rate of sediment is slow.
Sediment is rapidly formed. Sediment is slowly formed.
sediment are loosely packed, hence hard
cake is not formed.
Sediments are closely packed, hence
hard cake is formed.
The sediment is easy to redisperse on
shaking.
Sediment is difficult to redisperse on
shaking. (due to formation of hard cake)
Bioavailability is comparatively less. Bioavailability is relatively high.
The suspension is not pleasing in
appearance.
The suspension is pleasing in
appearance.
Formulation of suspensionsFormulation of suspensions
Formulation problemsFormulation problems
1. Sedimentation.
2.Thermodynamic instability.
3.Wetting.
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SedimentationSedimentation
• The factors affecting the rate of sedimentation are in Stokes' equation:
• Where v= velocity of sedimentation of a spherical particle of radius r, and
density σ, in a liquid of density ρ, and viscosity , and where g is theŋ
acceleration due to gravity.
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Thermodynamic instabilityThermodynamic instability
• Interfacial free energy (IFE).
• IFE = Interfacial tension * surface area
• Flocculation
• Aggregation
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WettingWetting
The insoluble medicament may be :
• Diffusible solids (dispersible solids): These are insoluble solids that
are light and easily wetted by water. They mix readily with water,
and stay dispersed long enough for an adequate dose to be
measured. After settling they redisperse easily. Examples include
magnesium trisilicate, light magnesium carbonate, bismuth
carbonate and light kaolin.
• Indiffusible solids: Most insoluble solids are not easily wetted, and
some particles may form large porous clumps in the liquid,
whereas others may remain on the surface. These solids will not
remain evenly distributed in the vehicle long enough for an
adequate dose to be measured. They may not redisperse easily.
Examples for internal use includes aspirin, phenobarbital,
sulfadirnidine and chalk, and for external use calamine,
hydrocortisone, su1phur and zinc oxide.
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WettingWetting
 Because of the high interfacial tension between indiffusible
solids and water; air may be trapped in these poorly wetted
particles which causes them to float to the surface of the
preparation and prevents them from being readily dispersed
throughout the vehicle.
 Wetting of the particles can be encouraged by reducing the
interfacial tension between the solid and the vehicle, so that
adsorbed air is displaced from solid surfaces by liquid.
 Suitable wetting agents have this effect, but decrease inter-
particular forces thereby affecting flocculation.
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WettingWetting
Wetting agents:
 Hydrophilic colloids such as acacia and tragacanth can act as
wetting agents. However, care should be taken when using
these agents as they can promote deflocculation.
 Intermediate HLB (hydrophilic-lipophilic balance) surfactants
such as polysorbates (tweens) and sorbitan esters (spans) are
used for internal preparations. Sodium lauryl sulphate and
quillaia tincture are used in external preparations.
 Solvents such as ethanol, glycerol and the glycols also facilitate
wetting.
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Suspending agentsSuspending agents
 Suspending agents increase the viscosity of the vehicle, thereby
slowing down sedimentation.
 Most agents can form thixotropic gels which are semisolid on
standing, but flow readily after shaking.
 Care must be taken when selecting a suspending agent for oral
preparations.
 Suspending agents can be divided into five broad categories:
natural polysaccharides, semi-synthetic polysaccharides, clays,
synthetic thickeners and miscellaneous compounds.
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Suspending agentsSuspending agents
Natural polysaccharidesNatural polysaccharides
 The main problem with these agents is their natural variability
between batches and microbial contamination.
 These materials should not be used externally as they leave a sticky
feel on the skin.
 They include tragacanth, acacia gum, starch, agar, guar gum,
carrageenan and sodium alginate.
 Tragacanth:
 Is a widely used suspending agent and is less viscous at pH 4-7.5.
 As a rule: 0.2g tragacanth powder is added per 100 mL suspension or
2g compound tragacanth powder per 100 mL suspension. Compound
Tragacanth Powder BP 1980 contains tragacanth, acacia, starch and
sucrose and so is easier to use.
 Tragacanth powder requires to be dispersed with the insoluble
powders before water is added to prevent clumping .
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Suspending agentsSuspending agents
Semi-synthetic polysaccharidesSemi-synthetic polysaccharides
 These are derived from the naturally occurring polysaccharide
cellulose.
 Examples include
 Methylcellulose (Cologel ®, Celacol®)
 Hydroxyethylcellulose (Natrosol 250®)
 Sodium carboxymethylcellulose (Carmellose sodium®)
 Microcrystalline cellulose (Avicel®).
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Suspending agentsSuspending agents
ClaysClays
These are naturally occurring inorganic
materials which are mainly hydrated silicates.
Examples include bentonite and magnesium
aluminium silicate (Veegum®).
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Suspending agentsSuspending agents
Synthetic thickeners:
•These were introduced to overcome the variable quality of
natural products.
•Examples include:
Carbomer (Carboxyvinyl polymer, Carbopol®),
Colloidal silicon dioxide (Aerosil®, Cab-o-sil®)
Polyvinyl alcohol (PVA).
Miscellaneous thickeners:
 Gelatin used as a suspending agent and a viscosity increasing
agent
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Containers for suspensionContainers for suspension
Suspensions should be packed in amber bottles,
plain for internal use and ribbed for external use.
There should be adequate air space above the
liquid to allow shaking and ease of pouring.
A 5 mL medicine spoon or oral syringe should be
given when the suspension is for oral use.
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Special label and advice for suspensionSpecial label and advice for suspension
The most important additional label for suspensions is
'Shake well before use',
Store in a cool place. Stability of suspensions may be
adversely affected by both extremes and variations of
temperature.
 Some suspensions. such as those made from
reconstituting dry powders, may need to be stored in
a refrigerator.
Extemporaneously prepared and reconstituted are
required to be recently or freshly prepared, with a 1-
4-week expiry date.
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A simple example,A simple example,
Chalk Mixture, Paediatric BP. Mitte 100mlChalk Mixture, Paediatric BP. Mitte 100ml
Master formula 100ml
Chalk 100mg 2g
Tragacanth 10mg 200mg
Syrup 0.5ml 10ml
Concentrated cinnamon
water 0.02ml 0.4ml
Double strength chloroform
water 2.5ml 50ml
Water to 5ml to 100ml
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SummationSummation
Suspensions can be used to administer an
insoluble solid by the oral route.
Suspensions may be used to replace tablets, to
improve dissolution rate, to prolong action and
to mask a bad taste.
Solids may be diffusible or indiffusible and require
different dispensing techniques.
Stokes' equation can be applied when formulating
a suspension to help ensure accurate dosage of
the drug.
Flocculated particles settle quickly and redisperse
easily, whilst deflocculated particles settle slowly
but tend to cake.
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SummationSummation
Hydrophobic solids may require wetting agents.
Suspending agents are added to slow down the
rate of settling of the solid.
Suspending agents may be natural
polysaccharides, semi synthetic polysaccharides,
clays or synthetic polymers.
Some suspensions are made by adding water to
reconstitute manufactured powders when
stability is a problem.
Shake well before use' and 'Store in a cool place‘
should be part of the labels on a suspension.
Inhalations are suspensions of a volatile material
adsorbed onto a diffusible solid.
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Semisolid dosage formsSemisolid dosage forms
 Semisolid dosage forms meant for external application
 Semisolid dosage forms subcategorized are as-
I) ointment
II) creams
III) paste
IV) Jellies
V) Suppositories
 The suppositories are also included in this category but it is a unit
dosage forms.
OintmentOintment
 Ointment are semisolid preparation meant for application to skin or
mucous membrane.
 The ointments are mainly used for their protective or emollient
properties
 It may be defined as a medicament or medicaments dissolved,
suspended or emulsified in ointment base.
 There is no single ointment base which possesses all the qualities of
ideal ointment base, so it become necessary to use more than one
ointment base in the preparation of ointment.
Qualities of ideal ointment baseQualities of ideal ointment base
 It should be inert, odourless & colourless & smooth.
 It should be physically & chemically stable.
 It should be compatible with the skin & with incorporated medicaments.
 It should be of such consistency that it spread & soften when applied to
skin with stress.
 It should not retard healing of wound.
 It should produce irritation or sensitization of the skin.
Classification of ointment baseClassification of ointment base
 Oleaginous bases
 Absorption bases
 Emulsion bases
 Water soluble bases
Oleaginous baseOleaginous base
 These bases consist of water soluble hydrocarbons, vegetable oils,
animal fats & wax.
 The constituents of hydrocarbon bases are soft paraffin, hard
paraffin & liquid paraffin.
 The vegetable oils are mainly used in ointment to lower the
melting point or to soften the bases.
 These bases serve to keep the medicaments in prolonged contact
with the skin & also act as occlusive dressings. They have a low
capacity to absorb water & are used chiefly for their emollient
effect.
 These bases losing their importance now a days for the many
reason.
Disadvantages of oleaginous basesDisadvantages of oleaginous bases
 They are greasy.
 They are sticky & are difficult to remove both from skin & clothing.
 They retain body heat which may produce an uncomfortable feeling of
warmth.
 They do not help in the absorption of medicaments.
Absorption basesAbsorption bases
 These bases are generally anhydrous substance which have the
property of absorbing considerable quantities of water but still
retaining their ointment like consistency.
 The absorption bases are of two type namely as
I) Non emulsified bases
II) Water in oil emulsion
 Non emulsified bases absorb water & aqueous solutions producing
w/o emulsion. E.g. Wool fat, wool alcohol, beeswax & cholesterol.
 Water in oil emulsions are capable of absorbing more water &
have the properties of non- emulsified bases. E.g. hydrous wool fat
( lanoline)
Emulsion basesEmulsion bases

These bases are semisolid or have cream like consistency.
 Both o/w or w/o emulsions are used as a ointment base.
 The o/w emulsion base is more popular now days because ease of
application will easily achieved.
 The w/o type of emulsion bases are greasy & sticky.
 The emulsifying ointment is prepared from emulsifying wax, white soft
paraffin & liquid paraffin.
Water soluble basesWater soluble bases
 These are commonly known as greaseless ointment bases.
 The water soluble bases consist of water soluble ingredients such as
carbowaxes ( polyethylene glycol polymer)
 The carbowaxes are water soluble, non – volatile & inert substance.
 Selection of appropriate carbowaxes is depend on their molecular
weight.
Types of methodTypes of method
 Trituation method
 Fusion method
 Chemical reaction method
 Emulsification method
TRITURATION METHODTRITURATION METHOD
 It is the most commonly used method for the preparationn of
ointments.
 The method is used when the base is soft and the medicament is
insoluble in base.
 So for uniform mixing of medicament in the base ,it bacomes
necessary to reduce the medicament to fine powder.
Fusion methodFusion method
When an ointment base contains a number of solid ingredients of
different melting points, such as white beeswax,stearic acid,hard
paraffin and cetyl alcohol,it is necessary to melt them in decreasing
order to their melting point.
This will avoid the over heating of the substances having low
melting points.
Chemical reaction methodChemical reaction method
 Certain chemical reactions are involved in the preparation of
several ointments.
 For example, iodine ointment.
 Iodine may be present in free form or in combined formwith the
ointment base.
Emulsification methodEmulsification method
 In this method the fats,oils,and waxes are melted together on a
water bath at a temperature of 70 degree Celsius.
 The aqueous solution of all the heat stable water soluble
component is also heated almost at the same temperature as that
of the melted base.
CreamsCreams
 These are viscous semisolid emulsions which are meant for external
use.
 Cream is divided in to two types namely as
I) Aqueous creams
II) Oily creams
 In case of aqueous creams the emulsions are o/w type & it is relatively
non greasy. The emulsifying waxes are anionic, cationic & non –ionic
used. Generally polysorbate, triethanolamine soap are used as
emulsifying agent.
 In case of oily creams w/o type & it is relatively greasy. The
emulsifying agent such as wool fat, wool alcohols, beeswax & calcium
soap is used.
 The cream should be store in collapsible tube & supplied in well
closed container to prevent evaporation & contamination.
PastesPastes
 Pastes are semisolid preparations intended for
external application to skin.
 The pastes are generally very thick & stiff.
 They do not melt at ordinary temperature & thus
forms a protective coating over the area where
they are applied.
 Pastes are differ from ointment as they contain a
high proportion of finely powdered medicaments.
 They are mainly used as a antiseptic, protective,
soothing dressings.
 Pastes should be stored & supplied in containers
made of materials which do not allow absorption
or diffusion of content.
Paste basePaste base
 Hydro carbon:
Soft paraffin and liquid paraffin are commonly used
bases for the preparation of paste.
 Water miscible bases:
Emulsifying ointment is used as water miscible base
for the preparation of pastes
 Water soluble bases:
Suitable combined of high and low molecular weight
polyethylene glycols are mixed together to get product of desired
consistancy.
SuppositoriesSuppositories
 Suppositories are solid dosage form of medicament for insertion
into body cavities other than mouth.
 They may be inserted into rectum,vagina or nasal cavity
suppositories are available in different shapes, sizes and weights.
 Suppositories are used to produce local, systemic and mechanical
action.
ADVANTAGES:
1) THESE ARE INSERTED INTO THE RECTUM TO
EXERT A DIRECT AND RAPID ACTION ON THE RECTUM .
2 )THESE ARE INSERTED INTO THE RECTUM TO
PROMOTE EVACUATION OF THE BOWL .
DISADVANTAGES:
1) THE IRRITANT DRUGS CAN’T BE ADMINISTERED BY
THIS ROUTE.
2) SUPPOSITORIES CAUSE EMBARRASSMENT TO THE
PATIENT, WHEN A DRUG IS ADMINISTERED BY INSERTING A
SUPPOSITORY INTO A BODY CAVITY .
TYPES OF SUPPOSITORIESTYPES OF SUPPOSITORIES
 RECTAL SUPPOSITORIES : These are meant for
introduction into the rectum for their systemic action.
 VAGINAL SUPPOSITORIES:These are meant for
introduction into the vagina.These suppositories are also know as
pessaries and are larger than rectal suppositories.
 NASAL SUPPOSITORIES:These are meant for introduced
into the nasal cavity and are also know as nasal bougies.
 URETHRAL SUPPOSITORIES:These are meant for
introduced the urethra and also known as urethral bougies.
 EAR CONES:These are meant for introduction into the ear and
and also known as aaurinaria.
Types of basesTypes of bases
Fatty bases
Water soluble and water miscible bases
Emulsifying bases
Fatty basesFatty bases
 Theobroma oil: It is a yellowish white solid obtained from crushed
and roasted seeds of theobroma cocoa.
 It also called as cocoa buttter.
 It has butter like consistency having melting point of 30 to 35
degree celsius.
 It is a mixture of glycerol ester of of stearic ,oleic,palmitric and
other fatty acids.
 Theobromal oil melts at body temperature and release the
medicament for rapid absorption.
 It is readily liquefy on warming and quickly settle on cooling.
DisadvantagesDisadvantages
 It melts in warm weather.
 It has the tendency to stick to the sides of the mould when
solidified.
 The leakage from the body cavities on melting can take place.
 It is relatively costly.
 It is immiscible with body fluids.
 It shows the phenomena of polymorphism i.e., when theobroma
oil is melted and cooled, it gets solidified into different crystalline
forms depending upon melting temperature ,rate of cooling and
size of the mass.
Emusified theobroma oilEmusified theobroma oil
 This may be used as abase when large quantity of aqueous
solutions are to be incorporated.
 The use of 5% glyceryl monostearate,10% lenette wax ,2-3% cetyl
alcohol,4% beeswax and 12% spermaceti is recommended to
prepare emulsified theobroma oil suppositories.
Hydrogenated oilsHydrogenated oils
 These are obtained by dehygenation of various vegetables,such as
arachi’s oils,cotton seed oils,coconut oils,palm oils,etc.,
Advantages:
 They are resistant to oxidation.
 Lubrication of the moulds is not required.
 Over heating does not affect the solifying point.
Disadvantages:
 The suppositories become brittle on rapid cooling in a
refrigerator.
Water soluble and water miscibleWater soluble and water miscible
basesbases
 Glycero-gelatin bases:
 It is a mixture of glycerine and water which is made stiff by the
addition of gelatin.
 The bases may be for preparing all types of supositories but it is
particularly used for making pessaries.
 Soap-glycerin bases:
 In glycero-gelatin bases,the gelatin is replaced with either curd
soap or sodium stearate which makes the base sufficiently hard to
prepare good quality of suppositories.
 Soap also helps in the evacuation action of glycerin.
 Polyethylene glycol:
 Polyethylene glycol polymers are commonly known as carbowaxes
or polyglycol or macrogols.
 The physical character of these carbowaxes varies according to the
molecular weight.
 The macrogals having molecular weight less than 1000 are liquids
and those with molecular weight higher than 1000 wax like solids.
 Advantages:
 They are chemically stable.
 They are non irritant.
 They do not allow to bacteria or mould growth to take place.
 They are physically inert substances.
Emusifying basesEmusifying bases
 Witepsol: They consist of triglycerides of saturated vegetable
acid with varying percentage of partial ester.
 A small amount of beeswax is used for in hot climates.
 Massa estarinum: It is a mixture of mono ,di and triglycerides of
saturated fatty acids. This also known as adeps solidus.
 Massuppol: It consist of glyceryl esters mainly of lauric acid to
which small amount of glyceryl monostearate has been added to
improve its water absorbing capacity.
 Disadvantages:
 They should be cooled rapidly in a refrigerator because they
become brittle.
 They are not very viscous on melting , so the medication
incorporated with the base settle down rapidly.
PESSARIESPESSARIES
 These are solid preparations containing one or more active
incredients and are suitable for vaginal insertion.They are intented
for as use as a single dose.
Types of pessaries:
 Compressed pessaries
 Moulded pessaries
 Compressed pessaries:
 These are also known as vaginal tablets,have the general
charecteristics of uncoated tablets but usually large and of great
weight . It should be stored in a well cclosed containers ,protected
from moisture and being crushed.
 Moulded pessaries:
 These are manufactured by pouring the liquified mass containing
the medicaments and auxillary substances into moulds of suitable
volume and cooling inorder to solidify the mass.
 Auxillary substances used are macrogols ,theobroma oil and
glycerogelatin bases.
JelliesJellies
 Jellies are transparent or translucent, non greasy, semi solid preparations
mainly used for external application to skin.
 These are also used for lubricating catheters, surgical gloves & rectal
thermometer.
 The substance like gelatin, starch, tragacanth, sodium alginate & cellulose
derivatives are used for the formulation of jellies.
 Jellies are of three types namely as
 Medicated jellies
 Lubricating jellies
 Miscellaneous jellies
 Gels: gels may be defined as semisolid
preparations which may contain small and
large of organic molecules dispersed in a
suitable liquid.
Introduction
With the advancement of pharmaceutical sciences, a new concept have
evolved various modern dosage forms & methods of their
administration. Some of the modern dosage forms are
 Implants
 Films & strips
 Liposome drug carriers
 Controlled drug delivery modules
 Erythrocytes
 Nanoparticles
 prodrugs
Implants These are hypodermic tablets are placed under the skin by a minor
surgery in order to release drugs over prolonged periods of time.
 Now the magnetically controlled implants have been developed which
can be opened or closed at will in order to release or stop the drug.
 These implants are placed at upper thigh at a depth of 5mm.
 These implants are useful in hormone therapy.
Films & stripsThese are meant for topical application for slow release of drug over
predetermined period of time. Films & strips are more popular these
days. They are sub categorized in to following types namely as
 Zero order release films
 Buccal strips
 Spray bandages
Zero order release films These are called as laminates & meant for topical application. E.g.
 Nitroglycerine laminates are prepared by mixing propylene glycol
with about 1% carbopol resin. The mixture is neutralized with NaoH
solution & then 0.1% of nitroglycerin is added. It is then placed in
polythene sheet 5*5 cm & its edges are sealed by heat. It is then
placed on pressure sensitive adhesive sheet of 5.5 * 5.5 cm so that it
can be properly adhesive to skin. Such laminates release the drug
slowly into circulation for about 12 hours.
Buccal strips
 The buccal & sublingual tablets are now replaced with buccal strips.
 These strips consist of a thin absorbent base of fabrics, filter paper &
cotton etc.
 The buccal strips are prepared by immersing a long piece of fabric
made from polyamide fibers into a molten mixture of carbowaxes &
dissolved or dispersed the drug.
 The fabric is then cooled & cut into small pieces.
 It should be contact with buccal mucosa for about 15 min. & then
removed & discarded.
Spray bandage
 These bandage are prepared by spraying the solution of drug in
polylactide (polymer of lactic acid anhydride)
 A solution of purified lactide polymer is made in chloroform.
 It is then packed in aerosol container having suitable propellant.
 When these solution sprayed then it will be a comfortable bandage
which can simply washed of with warm water.
Liposome drug carriers These are several carriers in our body which transport both to an
other like as enzymes, proteins etc.
 These are phospholipids which can transport both hydrophilic &
hydrophobic drugs.
 The large multilamellar vesicles (LMV), small unilamellar vesicles
(SUV), large unilamellar vesicles (LUV) are some of the liposome's
known today.
Applications
 Used in diseases caused by intracellular parasites. E.g. malaria,
tuberculosis & amoebiasis.
 It entrapped insulin is active orally & can be replaced by IM
administration of insulin.
 It can be used to transport functional DNA/RNA molecules into cell.
 It can be used to transport radio pharmaceuticals & immunological
products.
 Liposomal daunomycin has longer duration of action than free
daunomycin which is used in the treatment of neoplasia.
Controlled drug delivery modules
 These are the device which are formed by embedding the drug within
a polymeric matrix so that it gets released slowly to the body over a
long period of time.
 It will formed drug – polymer complex & may be formulated in to
tablet, capsule or any other suitable formulation.
 These modules are punctured before administration with leaser beam
to make a small orifice for release of the drugs.
 The drugs is released from these modules by diffusion, osmosis or
chemical reactions.
 These are applied to skin, implanted subcutaneously or inserted into
various body cavities.
Erythrocytes
 Erythrocytes are tried in order to achieve controlled release of drugs.
 The life span of erythrocytes are 120 days.
 It can allow a drug to circulate in the body for long period of time
which help slow release of the drugs in to serum.
 Released erythrocytes are prepared by putting them in to a hypotonic
medium. So that they can easily swollen.
 The aqueous solutions of the drug is added to the medium so that
drugs gets in to erythrocytes through open pores.
 When isotonicity is adjusted the erythrocytes shrink, thus
encapsulating the drug with in them. These erythrocytes may be
suspended in normal saline solutions for preparing injections.
Applications Released erythrocytes of urease have been used in kidney failure to
degrade serum urea.
 Released erythrocytes of asparaginase have shown good result in
asparaginase dependent leukemia.
 Released erythrocytes of methotrexate & adrianycin have been tried
in cancer therapy.
 Released erythrocytes of prednisolone have shown good result to
prolong the anti-inflammatory action.
Nanoparticles
 It is based on colloidal drug delivery system.
 The particles size of this system is in nanometer range (200 – 500
mm)
 The system consist of a drug & carriers to deposit the drug at target
site.
 The carriers used are naturally occurring macromolecules like human
serum albumin, bovine serum albumin, & other substances like
gelatin, casein & ethylcellulose.
Applications
 Flourescein isothinocyanate (FITC) nanoparticles have been used to
incorporate cytotoxic agent into tumor cell in cancer chemotherapy.
 Nanoparticles along with biological maker like immunoglobulin can
be used to target the drugs to very specific site.
Prodrugs
 The compound which undergo biotransformation before showing
desired pharmacological activity are called prodrugs or proagents.
 Prodrugs are generally the ester or amides of parent drugs.
 These are useful to improving the stability, solubility, bioavailability
of drugs, masking the unpleasant taste & odour of the parent drug &
reducing the toxicity
Applications
 Choramphenicol palmitate, the prodrug of chloramphenicol is used
in the preparation of pediatrics suspension because it has no bitter
taste.
 Procaine penicillin G & benzathine penicillin G are prodrugs of
penicillin G which shows resistance to hydrolysis as compared to the
parent drug.
 Cindamycin 2- phosphate the prodrug of cindamycin has no bitter
taste of parent drug.
Thank You

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Pharmaceutical dosage form BY ABARAJITHA&MUTHUKUMAR KMCH COP

  • 1. S.Muthukumar /ABARAJITHA.T Assistant Professor/IIIrd YEAR B.PHARM Student KMCH COLLEGE OF PHARMACY, COIMBATORE. Dept. of Pharmaceutics
  • 2. DrugDrug  Drug may be defined as an agent or substance, intended for use in the diagnosis, mitigation, treatment, cure or prevention of disease in human beings or animals.  Drugs are rarely administered in their original or crude forms. They are administered in different dosage forms by converting them into suitable formulations. Crude Drugs
  • 3. Dosage FormsDosage Forms  Dosage forms are the carrier through which drug molecules are delivered to sites of action within the body.  Every dosage forms is a combination of the drug and different kinds of non – drug components called as Excipients or additives.  The additives are used to give a particular shape to the formulation, to increase stability, palatability & more elegance to preparations.
  • 4. Need For Dosage FormsNeed For Dosage Forms  Accurate dose.  Protection e.g. coated tablets, sealed ampules.  Protection from gastric juice, e.g. enteric coated tablets.  Masking unpleasant taste and odour.  Provide drugs within body tissues, e.g. injection  Sustained release medication.  Facilation of Insertion of drugs into body
  • 5. Provide optimum drug action through inhalation therapy. Provide drug action through topical administration at local area of body. e.g. creams, ointment, emulsion, lotions etc. Use of desired vehicle for insoluble drugs.
  • 6. ClassificationClassification Solid dosage forms Unit dosage forms Tablets Capsule Powders Pills Bulk Internal Fine powders & granules External Dusting powders Insufflations Dentifrice Snuffs Ear powders Liquid dosage forms Biphasic Emulsion Suspension Monophasic Internal External Syrups Elixirs Linctus Drops Liniments Lotions Gargles Throat paints Mouth washes Sprays Eye lotions Eye drops Nasal drops Semi solid dosage forms Internal External Suppositories Pessaries Ointment Creams pastes Jellies
  • 8. Solid dosage formsSolid dosage forms Tablets Pills Dusting Powders Capsules Granules
  • 9.  SOLID DOSAGE FORMS  Solid dosage forms one of the oldest dosage forms and most of the solid dosage forms are available in Unit dose.  Unit dose may be defined as a exact quantity of the drug administered at once. e.g. Tablets, Capsule, pills, cachets, powders etc.  When drugs are to be administered orally in dry state, then tablets, capsules are most convenient dosage forms.  Some solids are supplied in bulk (Means quantity available in large). Bulk powders can be supplied as Internal (Granules, Fine powders) as well as External (Dusting Powders, Insufflations etc)
  • 10. Dusting PowdersDusting Powders  Dusting powders are applied externally to skin, so they should be applied in very fine state to avoid local irritation. Hence dusting powders should be passed through sieve no 80 to obtained fined powders.  Dusting powders are prepared by mixing of more than one ingredients in which either starch, kaolin, or talc are used in their formulation. Generally talc or kaolin are used because they are inert in nature.  Dusting powders are used for antiseptic, astringent, absorbent, antiperspirant etc.  Dusting powders are of two sub type they are as I) Medical dusting powder II) Surgical Dusting powders
  • 11. Medical Dusting PowdersMedical Dusting Powders Medical Dusting powders are used to increase superficial condition of skin. These are not applied on wounds, burns etc Medical dusting powders must be free from dangerous pathogenic micro- organism.
  • 12. Surgical Dusting PowdersSurgical Dusting Powders Surgical dusting powders are used in body cavities and also on major wounds like as burns etc. They should be sterilized before use. They are mainly used for their antiseptic, absorbent action.
  • 13. InsufflationsInsufflations  These are medicated dusting powders meant for introduction into body cavities (nose, throat, ear, vagina etc) with the help of an apparatus known as a insufflator.  It sprays the powders (in a state of fine particles) on site of application.  Now a days insufflations are also available in pressure aerosols. This pressure aerosols are used for administration of potent drug.  They are used in the treatment of ear, nose, throat infections with antibiotics to produce local effect of drugs.
  • 14. SnuffsSnuffs These are finely divided solid dosage forms of medicaments which are inhaled into nostrils. They are mainly used for their antiseptic, bronchodilator and decongestion action.
  • 15. GranulesGranules  Granulation is the process in which primary powder particles are made to adhere to form larger multiparticle or large particles entities called granules.  The bitter, nauseous, unpleasant powders can not be given tablets, capsule due to bulk quantity are required to be taken, as well as they are not given in liquid dosage forms due to their stability such powders are given in the granules forms.  These powders are mixed with suitable exicipent along with granulating agent, prepare a coherent mass then dried & passed through the sieve to obtained desired size of granules.  E.g. Effervescent granules
  • 16. Effervescent GranulesEffervescent Granules  Effervescent granules are meant for internal use.  They contained medicaments mixed with citric acid, tartaric acid & sodium bi carbonates, sometime saccharin or sucrose may be added for sweetening taste.  Before, administration desired quantity of granules are dissolved in water, the acid & bicarbonate reacts with each other to produce effervescence.  Effervescent granules are prepared by two methods, namely as, I) Heat method, II) Wet method
  • 17. Heat methodHeat method  A large porcelain or stainless steel evaporating dish is placed over the boiling water bath.  The dish must be sufficiently hot (generally heating takes place for 1 – 5 min.) before transferring the powders into it, to ensure rapid liberation of water of crystallization from citric acid.  If heating of the dish is delayed then the powder which is added to it, will heat up slowly & liberated water of crystallization will also be liberated simultaneously.  As a result, sufficient water will not be available to make a coherent mass.  This coherent mass will pass through the sieve to obtained suitable size of granules, dry it in oven at 600 c then packed in air tight container.
  • 18. Wet methodWet method  In this methods all the ingredients are mixed thoroughly  This powders mixture make moistened with non – aqueous vehicle (e.g. alcohol), to prepare a coherent mass which is then passed through sieve no 8 to obtained suitable granules.  Then dried in oven at 600 c. The dried granules are again passed through the sieve to break the lumps which may be formed during drying.  The dried granules are packed in air tight container.
  • 19. TabletsTablets  These are solid dosage forms of medicaments which are prepared by moulding or by compression with or without Excipients.  The tablets can be prepared by two methods namely as I) Dry granulation II) Wet Granulation
  • 20. CapsuleCapsule  Capsules are solid unit dosage forms in which one or more medicaments enclosed within a shell.  Capsules mainly divided in to two parts namely as – I) Body (Longest part of capsule shell), II) Cap (Smallest part of capsule shell)  The capsule are generally prepared by gelatin.  Depending on their formulation, two types of gelatin are used namely as – I) Hard gelatin, II) Soft gelatin. Body Cap
  • 21. PillsPills  These are small, rounded solid dosage forms containing medicaments intended for oral use.  The medicaments are mixed with excipients to forms a firms plastic mass.  The mass is rolled to uniform pill pipe, which cut into numbers of uniform pills. The pills are spherical in shape & produced by rolling them under wooden pill rounder.  Sometimes pills are coated with varnish, gold leaf, etc to improve finish, unpleasant taste & stability.  Now a days pills are outdated preparations because of number of disadvantages such as -
  • 22.  Disintegration time of pill is uncertain means freshly prepared pills are disintegrates readily rather than old dried pills.  It is difficult to prepare pills of uniform size & weight.
  • 24.
  • 26.  It may be defined as “A solution is a liquid-preparation that contains one or more soluble chemical substances dissolved in a specified solvent”  Liquid dosage forms are intended for External, Internal or parenteral use.  The component of the solution which is present in a large quantity is known as “SOLVENT” where as the component present in small quantity is termed as “SOLUTE”  They mainly classified in to two category namely as – I) Monophasic Liquid dosage forms. II) Biphasic liquid dosage forms.
  • 27. AdvantagesAdvantages  Immediately available for absorption.  Administration convenient, particularly for infants, psychotic patients.  Easy to color, flavor & sweeten.  Liquids are easier to swallow than solids and are therefore particularly acceptable for pediatric patient.  A solution is an homogeneous system and therefore the drug will be uniformly distributed throughout the preparation.  Some drugs like aspirin, KCl can irritate gastric mucosa if used orally as a solid dosage forms. But this effect can be reduce by solution system.
  • 28. DisadvantagesDisadvantages  Less stable in aqueous system. Incompatibility is faster in solution than solid dosage form.  Patients have no accurate measuring device.  Accident breakage of container results in complete loss.  Solution often provide suitable media for the growth of micro organisms.  The taste of a drug, which is often unpleasant, is always more pronounced when in solution than in a solid form.  Bulky than tablets or capsule, so difficult to carry transport.
  • 29. Monophasic liquid dosage formsMonophasic liquid dosage forms
  • 30.  Monophasic liquid dosage forms are represent by true or colloidal solution.  The component of the solution which is present in a large quantity is known as “SOLVENT” where as the component present in small quantity is termed as “SOLUTE”.  A solution is homogenous because the solute is an ionic or molecular forms of subdivision.  In case of colloidal solutions, the solutes are present as aggregates although they cannot be seen by necked eye or ordinary microscope.  It is sub classified as – I) Internal Use, II) External use
  • 31. Monophasic Liquid Dosage forms Internal Use External Use  Syrup  Elixirs  Linctuses  Drops  Liniments  Lotions  Gargles  Mouth Wash  Throat paints  sprays  Inhalations  Nasal drops  Eye drops  Eye lotions  Ear drops
  • 32.
  • 33. SyrupSyrup  It is a concentrated or saturated solutions of sucrose in purified water.  The concentration of sucrose is 66.7% w/w & due to that it is a viscous preparations.  The syrup which contains medical substance called as a medicated syrup & those containing aromatic or flavored substance known as a flavored syrup.
  • 34. Importance of syrupImportance of syrup  It retards oxidation because its partly hydrolyzed into reducing sugar.  It prevents decomposition of many vegetable substance because its have high osmotic pressure which prevent the growth of bacteria.  They are palatable due sweet taste.
  • 35. ElixirsElixirs  It is clear, sweetened, aromatic, hydroalcholic preparations meant for oral use.  The medicated elixirs are generally contained potent drug like as antibiotics, antihistamine or sedative , where as non – medicated elixirs contained flavoured.  The composition of elixirs contained mainly as ethyl alcohol (active ingredients),water, glycerin or propylene glycol, colouring agent, flavouring agent & preservative.
  • 36. LinctusesLinctuses  These are viscous liquid preparations that’s are used for the treatment of cough.  They contain medicaments which have demulcent, sedative, expectorant action.  They are taken in small doses without diluting with water to have prolonged effect of medicines.  Simple syrup is used as a vehicle for most of the linctuses.  Tolu syrup is preferred in certain cases because of its aromatic odour & flavour. Moreover it have a mild expectorant action
  • 37. DropsDrops  These are liquid preparations meant for oral administration.  The oil soluble vitamins, such as vitamin A & D concentrates in fish – liver oil are presented as drops for administration.  Since these preparations contain potent medicaments, the dose must be measured accurately  The following two methods are commonly used for this purpose.  Use of a dropper which is accurately graduated in fractions of a milliliters.  Use of a pre – calibrated dropper.
  • 38.
  • 39. LinimentsLiniments  Liniments are liquid or semi- liquid preparations meant for external application to the skin.  They are usually applied to the skin with friction & rubbing of the skin.  Are usually alcoholic and oily liquid preparations (monophasic) or emulsion (biphasic).  Alcoholic liniments are used generally for their rubefacient and counterirritant effects. Such liniments penetrate the skin more readily than do those with an oil base.  The oily liniments are milder in their action and may function solely as protective coatings  Liniments should not be applied to skin that are bruised or broken.
  • 40. LotionsLotions  Are usually aqueous, alcoholic or oily liquid preparations.  They are intended for external application without friction or rubbing to the affected area  Usually applied with the help of some absorbent material such as cotton wool or gauze.  It is generally used to provide cooling, soothing and protective & antiseptic action.
  • 41. GarglesGargles  Gargles are aqueous solutions used for treating throat infection (pharynx and nasopharynx part)  Supplied in concentrated forms with directions of dilution with warm water before use  They are used into intimate contact with the mucous membrane of throat for few seconds, before they are thrown out of the mouth.  They are used to relieve soreness in mild throat infection.  They are also used for their antiseptics, antibiotics and/or anesthetics
  • 42. Mouth washMouth wash  These are aqueous solutions with pleasant or acceptable taste & odour  These are used to make clean & deodorise the buccal cavity or used for oral hygiene and to treat infections of the mouth.  They mainly contain antibacterial agent, alcohol, glycerin, sweetening agent, flavoring agent & colouring agent.
  • 43. Throat paintsThroat paints  Throat paints are viscous liquid preparations used for mouth and throat infections  Glycerin is commonly used as a base because being viscous it adheres to mucous membrane for long period and it possess a sweet taste.
  • 44. SpraysSprays  These are the preparations of drugs in media which may be aqueous, alcoholic, or glycerin.  They are applied to the mucous membrane of throat or nose with an atomizer.  The throat sprays must be sprayed from a special type of atomizer known as a nebulizer, which removes the large droplets by baffling system. Only precaution should be taken that the fine droplet will used to easily reach the lungs. Nebulizer
  • 45. InhalationsInhalations  These are liquid preparations containing volatile substance & are used to relieve decongestion & inflammations of respiratory tract.  The volatile substance in inhalations would be volatile at room temperature so that they should be placed on some adsorbent pad or handkerchief.  In some cases inhalations will added to hot water (650 c) then vapors will inhaled.
  • 46. Nasal dropsNasal drops  Drugs in solution may be instilled into the nose from a dropper or from a plastic squeeze bottle.  The drug may have a local effect, e.g. antihistamine, decongestant.  Alternatively the drug may be absorbed through the nasal mucosa to exert a systemic effect.  The use of oily nasal drops should be avoided because of possible damage to the cilia of the nasal mucosa & if it is used for long period may reach the lungs & cause lipoid pneumonia.  To avoid that Nasal drops are prepared so that they are similar in many respects to nasal secretions, so that normal ciliary action is maintained thus aqueous nasal solutions usually are isotonic and slightly buffered to maintain a pH of 5.5 to 6.5.
  • 47. Eye dropsEye drops  Sterile, aqueous/oily solutions or suspensions intended for instillation in eye sac.  Eye drops may contain buffers, stabilizing agents, dispersing agents, solubilising agents, anti-oxidants & agents required for tonicity/ viscosity adjustment  Single dose container should not contain anti-microbial preservative.  In case of multi dose container a dropper should be supplied with it for administration. Maximum size of such containers is 10 ml.
  • 48. Eye lotionsEye lotions  These are the aqueous solutions used for washing the eyes.  These are supplied in concentrated forms & are required to diluted with warm water immediately before use.  They should be free from foreign particles to avoids irritation to the eye.  They are required to prepared fresh & should not be stored for more than two days to avoid microbial contaminations.
  • 49. Ear dropsEar drops  These are the solutions of drugs that are instilled into ear cavity with the help of dropper.  These are generally used for cleaning the ear, softening the wax & for treating the mild infections.  The solutions is generally prepared in water, glycerin, propylene glycol & dilute alcohol.
  • 50.
  • 51.
  • 52. Biphasic liquid dosage formsBiphasic liquid dosage forms  The liquid which consist of two phases are known as a biphasic liquid dosage forms.  They are sub categorized into two different forms namely as – I) Emulsion II) Suspension  In emulsion both phases are available in liquid where as in suspension, finely divided solid particles are suspended in liquid medium.
  • 53. EmulsionEmulsion  Emulsion is a biphasic liquid preparations containing two immiscible liquid (Continuous Phase & dispersed phase) made missicible.  The liquid which is converted into minute globules is called as dispersed phase & the liquid in which the globules are dispersed is called the continuous phase dispersed phase continuous phase Two Immiscible Liquids Dispersed Phase (Internal phase) Continuous Phase (External phase)  An emulsion is a thermodynamically unstable system consisting of at least two immiscible liquid phases one of which is dispersed as globules in the other liquid phase stabilized by a third substance called emulsifying agent. The globule size in emulsion varies from 0.25 to 25 µm.
  • 54. Examples for emulsions:- milk, rubber latex, crude oil etc. A.: Two immiscible liquids not emulsified B. An emulsion of phase B dispersed in Phase A C. Unstable emulsion slowly separates. D. The emulsifying agent ( black film) places it self on the interface between phase A and phase B and stabilizes the emulsion.
  • 55. Types of emulsionsTypes of emulsions Simple type Water in oil (w/o) Oil in water (o/w) Depending on globule size Micro emulsion Fine emulsion Special type Multiple emulsion (w/o/w, o/w/o)
  • 56. Water in oil (w/o)Water in oil (w/o)  In this types of emulsion water is dispersed phase & oil is continuous phase  w/o types of emulsion generally meant for External use.  Examples are butter, lotions, creams etc.  In rare case they are used internally. Water is dispersed phase Oil is continuous phase
  • 57. Oil in water (o/w)Oil in water (o/w)  In this types of emulsion oil is dispersed phase & water is continuous phase  o/w types of emulsion meant for both Internal use & External use.  Examples for internal use are Vitamin A in corn oil, liquid paraffin in water etc.  Examples for External use are Benzyl benzonate emulsion. Oil is dispersed phase water is continuous phase
  • 58. Micro EmulsionMicro Emulsion  These are clear dispersions of o/w or w/o in which the globules have small size like as a 10nm or 0.01 µm..  Being cleared products micro emulsion are more popular now a days.  Micro emulsions are thermodynamically stable optically transparent , mixtures of a biphasic oil –water system stabilized with surfactants.
  • 59. Fine emulsionFine emulsion  Normally these have a milky appearance.  The globule size ranges from 0.25 to 25 µm.
  • 60. Multiple emulsionMultiple emulsion  These are emulsion with in emulsion & designated as w/o/w or o/w/o.  The drugs that is incorporated in the innermost phase must cross two phase boundaries before getting absorbed.  It is generally used in oral sustained release or intramuscular therapy.
  • 61.
  • 62. The following methods are used for the preparation of emulsions on a small scale. 1.Dry gum method 2. Wet gum method 3. Bottle method 4. Other methods
  • 63. Dry gum method: 1.Measure the required quantity of oil in a dry measure and transfer in to mortar. 2.Add calculated quantity of gum acacia in to mortar and triturate to form a uniform mixture. 3.Add water and triturate vigorously till the clicking sound is produced in the product becomes white. 4.The emulsion produced this stage is known as primary emulsion. 5.Ratio of oil water gum  Fixed oil-4:2:1(Caster oil, Arachis oil)  Volatile oil-2:2:1(Peppermint oil, Cinnamon oil)  Mineral oil-3:2:1(Liquid paraffin) Ex: Arachis oil emulsion
  • 64. Wet gum method: 1.Powder the gum acacia in in a mortar. Add water and triturate it with gum so as to form a mucillage. 2.Add the required quantity of oil in small proportions with rapid trituration until the clicking sound is produced and the water becomes white.To get a primary emulsion 3.Add more water and triturate to produced required volume.Stirr thoroughly so as to form a uniform emulsion. Ex: Caster oil emulsion Bottle Method:  It is used for the preparations of volatile and other non-viscous oils.  Measure the oil and transfer in to large bottle.  Add required quantity of gum acacia.  Shake the bottle vigorously until oil and gum mixed thoroughly.  Add water and shake the mixture vigorously to form a primary emulsion.
  • 65. Other Methods:  Various blenders and homogeniser used for preparing emulsions.  Hand homogeniser,colloidal mill are some of the homogeniser used for the preparations of emulsions.  The principle is large globules coarse emulsion are broken in to smaller globules by passing them under pressure.  A coarse emulsion is prepared in a mortar which is transferred in to hand homogeniser.
  • 66.
  • 67. Dilution test Conductivity test Dye test Fluorescence test Cobalt chloride test Filter paper test
  • 68. Dilution testDilution test  The emulsion is diluted with water, after dilution emulsion remain stable then it is said to be o/w type of emulsion because water is in continuous phase. If emulsion is break after dilution with water then it is said to be w/o type of emulsion. Add drops of water Water distribute Uniformly Add drops of water O/W Emulsion W/O Emulsion
  • 69. Conductivity testConductivity test  Conductivity test can be performed by dipping a pair of electrode connecting with low voltage bulb & pass the current.  If bulb glows then it is said to be o/w type of emulsion because water is in continuous phase & it is good conductor of electricity.  If bulb doesn't glow then it is said to be w/o type of emulsion because oil is bad conductor f electricity. Bulb glows with O/W Emulsion Emulsion Bulb doesn’t glow with W/O
  • 70. Dye testDye test  Oil soluble Scarlet red dye is mixed with emulsion.  Place a drop of emulsion on microscopic slide cover it with cover slip & examine under microscope.  If disperse globules appears red & ground is colourless then it said to be o/w type of emulsion because water is present in continuous phase.  If reserve condition occurs (If disperse globules appears colourless & ground is red colour then it said to be w/o type of emulsion because oil is present in continuous phase.) Oil is dispersed phaseWater is continuous phase Water is disperse phase Oil is continuous phase
  • 71. Fluorescence testFluorescence test  Certain fixed oil posses the physical properties of fluorescing in the presence of ultraviolet radiations.  If examine under microscope ground is fluorescence then it said to be w/o type of emulsion because oil is present in continuous phase.  If examine under microscope droplet is fluorescence then it said to be o/w type of emulsion because oil is present in disperse phase.
  • 72. Creaming testCreaming test  The direction of creaming identifies the emulsion type, if the densities of aqueous and oil phases are known.  Water-in-oil emulsions normally cream downward as oil is usually less dense than water.  Oil-in-water emulsions normally cream upwards.
  • 73. Cobalt chloride testCobalt chloride test  Pour the emulsion on filter paper then it is soaked in cobalt chloride solutions & allowed to dry turns from blue to pink.  Then this emulsion is said to be o/w type of emulsion.  This test may fail if emulsion unstable or breaks in presence of electrolyte.
  • 74. Filter paper testFilter paper test  This test is based on the fact that an o/w emulsion will spread out rapidly when dropped onto filter paper.  In contrast, a w/o emulsion will migrate only slowly. This method should not be used for highly viscous creams.
  • 75.
  • 76. SuspentionSuspention  Suspensions are the biphasic liquid dosage forms of medicament in which finely divided solid particles ranging from 0.5 to 5 micron are dispersed in a liquid or semisolid vehicle, with aid of single or combination of suspending agent.  In which solid particles acts as disperse phase where as liquid vehicle acts as continuous phase  The external phase (suspending medium) is generally aqueous in some instance, may be an organic or oily liquid for non oral use.  The particle size for non oral suspension is so important to avoid grittiness to skin.
  • 77. Advantage of suspensionAdvantage of suspension  Suspension can improve chemical stability of certain drug. E.g. Procaine penicillin  Drug in suspension exhibits higher rate of bioavailability than other dosage forms. Solution > Suspension > Capsule > Compressed Tablet > Coated tablet  Duration and onset of action can be controlled. E.g. Protamine Zinc-Insulin suspension.  Suspension can mask the unpleasant/ bitter taste of drug. E.g. Chloramphenicol
  • 78. Disadvantage of suspensionDisadvantage of suspension  Physical stability , sedimentation and compaction can causes problems.  It is difficult to formulate.  Uniform and accurate dose can not be achieved unless suspension are packed in unit dosage form.  All suspensions are required to be shaken before measuring of dose.  The storage of suspension may lead to changes in disperse system especially, when there is fluctuations in temperatures.
  • 79. Ideal qualities of good suspensionIdeal qualities of good suspension  It should settle slowly & easily re – dispersed on shaking  It should readily & evenly pour from container.  It should be chemically inert.  It should not forms hard cake.  It should prevent degradation of drug or to improve stability of drug.  It should mask the taste of bitter of unpleasant drug.
  • 80. Ideal qualities of good suspensionIdeal qualities of good suspension  It should settle slowly & easily re – dispersed on shaking  It should readily & evenly pour from container.  It should be chemically inert.  It should not forms hard cake.  It should prevent degradation of drug or to improve stability of drug.  It should mask the taste of bitter of unpleasant drug.
  • 81. 2.On the basis of proportion of solids: i)Dilute suspension:  It comprise of 2-10%W/V of solid constituents. e.g:. Prednisolone acetate ii) Concentrated suspension:  It comprise of 50%W/V of solid constituents. e.g:. External and Parenteral application. 3. On the basis of nature and behavior of solids: i) Flocculated suspensions:  The system involves chemical bridging between the particles to form aggregates.  Weak van der waal attraction forces are present in between these light and fluffy aggregates.  Aggregation can be facilitated through adding flocculating agents.  Flocculation can be attained by adding extra anions.
  • 82. Flocculated suspensionFlocculated suspension  In this type, solid particles are loosely aggregates themselves, means individual particles are come in contact with each other to forms network like structure called as a floccules.  These flocs are light, fluffy in nature, which are held together by weak van der waals force of attraction.  Aggregation is achieved by adding flocculating agent.  This suspension will readily sediments.  This suspension posses better physical stability but less bioavailability as compared to deflocculated suspension due to dissolution of floccules.
  • 83. Deflocculated suspensionDeflocculated suspension  In this type of suspension, individual particle exits as a separate entity, means particles carry a finite charges on their surface . Hence particles approaches each other, they experience repulsive forces. This force create a high potential barrier, which prevents a aggregation of particles.  During storage, these suspension shows a sedimentation at slow rate, due to that particles forms a close packing arrangement.  So that it is difficult to re dispersed on agitation & forms a cake or claying which is hard in nature.  This type of suspension have shorter shelf life but high bioavailability as compared to flocculated suspension.
  • 84. Difference between flocculated & deflocculated suspensionDifference between flocculated & deflocculated suspension Flocculated Suspension Deflocculated suspension Particles form loose aggregates & forms network like structure. Particle exist as separate entities. Particles experience attractive forces. Particles experience repulsive forces. Supernatant liquid is clear. Supernatant liquid is cloudy. The rate of sediment is high. The rate of sediment is slow. Sediment is rapidly formed. Sediment is slowly formed. sediment are loosely packed, hence hard cake is not formed. Sediments are closely packed, hence hard cake is formed. The sediment is easy to redisperse on shaking. Sediment is difficult to redisperse on shaking. (due to formation of hard cake) Bioavailability is comparatively less. Bioavailability is relatively high. The suspension is not pleasing in appearance. The suspension is pleasing in appearance.
  • 85. Formulation of suspensionsFormulation of suspensions Formulation problemsFormulation problems 1. Sedimentation. 2.Thermodynamic instability. 3.Wetting. 03/09/19
  • 86. SedimentationSedimentation • The factors affecting the rate of sedimentation are in Stokes' equation: • Where v= velocity of sedimentation of a spherical particle of radius r, and density σ, in a liquid of density ρ, and viscosity , and where g is theŋ acceleration due to gravity. 03/09/19 BA-FP-JU-C
  • 87. Thermodynamic instabilityThermodynamic instability • Interfacial free energy (IFE). • IFE = Interfacial tension * surface area • Flocculation • Aggregation 03/09/19 BA-FP-JU-C
  • 88. WettingWetting The insoluble medicament may be : • Diffusible solids (dispersible solids): These are insoluble solids that are light and easily wetted by water. They mix readily with water, and stay dispersed long enough for an adequate dose to be measured. After settling they redisperse easily. Examples include magnesium trisilicate, light magnesium carbonate, bismuth carbonate and light kaolin. • Indiffusible solids: Most insoluble solids are not easily wetted, and some particles may form large porous clumps in the liquid, whereas others may remain on the surface. These solids will not remain evenly distributed in the vehicle long enough for an adequate dose to be measured. They may not redisperse easily. Examples for internal use includes aspirin, phenobarbital, sulfadirnidine and chalk, and for external use calamine, hydrocortisone, su1phur and zinc oxide. 03/09/19 BA-FP-JU-C
  • 89. WettingWetting  Because of the high interfacial tension between indiffusible solids and water; air may be trapped in these poorly wetted particles which causes them to float to the surface of the preparation and prevents them from being readily dispersed throughout the vehicle.  Wetting of the particles can be encouraged by reducing the interfacial tension between the solid and the vehicle, so that adsorbed air is displaced from solid surfaces by liquid.  Suitable wetting agents have this effect, but decrease inter- particular forces thereby affecting flocculation. 03/09/19 BA-FP-JU-C
  • 90. WettingWetting Wetting agents:  Hydrophilic colloids such as acacia and tragacanth can act as wetting agents. However, care should be taken when using these agents as they can promote deflocculation.  Intermediate HLB (hydrophilic-lipophilic balance) surfactants such as polysorbates (tweens) and sorbitan esters (spans) are used for internal preparations. Sodium lauryl sulphate and quillaia tincture are used in external preparations.  Solvents such as ethanol, glycerol and the glycols also facilitate wetting. 03/09/19 BA-FP-JU-C
  • 91. Suspending agentsSuspending agents  Suspending agents increase the viscosity of the vehicle, thereby slowing down sedimentation.  Most agents can form thixotropic gels which are semisolid on standing, but flow readily after shaking.  Care must be taken when selecting a suspending agent for oral preparations.  Suspending agents can be divided into five broad categories: natural polysaccharides, semi-synthetic polysaccharides, clays, synthetic thickeners and miscellaneous compounds. 03/09/19 BA-FP-JU-C
  • 92. Suspending agentsSuspending agents Natural polysaccharidesNatural polysaccharides  The main problem with these agents is their natural variability between batches and microbial contamination.  These materials should not be used externally as they leave a sticky feel on the skin.  They include tragacanth, acacia gum, starch, agar, guar gum, carrageenan and sodium alginate.  Tragacanth:  Is a widely used suspending agent and is less viscous at pH 4-7.5.  As a rule: 0.2g tragacanth powder is added per 100 mL suspension or 2g compound tragacanth powder per 100 mL suspension. Compound Tragacanth Powder BP 1980 contains tragacanth, acacia, starch and sucrose and so is easier to use.  Tragacanth powder requires to be dispersed with the insoluble powders before water is added to prevent clumping . 03/09/19 BA-FP-JU-C
  • 93. Suspending agentsSuspending agents Semi-synthetic polysaccharidesSemi-synthetic polysaccharides  These are derived from the naturally occurring polysaccharide cellulose.  Examples include  Methylcellulose (Cologel ®, Celacol®)  Hydroxyethylcellulose (Natrosol 250®)  Sodium carboxymethylcellulose (Carmellose sodium®)  Microcrystalline cellulose (Avicel®). 03/09/19 BA-FP-JU-C
  • 94. Suspending agentsSuspending agents ClaysClays These are naturally occurring inorganic materials which are mainly hydrated silicates. Examples include bentonite and magnesium aluminium silicate (Veegum®). 03/09/19 BA-FP-JU-C
  • 95. Suspending agentsSuspending agents Synthetic thickeners: •These were introduced to overcome the variable quality of natural products. •Examples include: Carbomer (Carboxyvinyl polymer, Carbopol®), Colloidal silicon dioxide (Aerosil®, Cab-o-sil®) Polyvinyl alcohol (PVA). Miscellaneous thickeners:  Gelatin used as a suspending agent and a viscosity increasing agent 03/09/19 BA-FP-JU-C
  • 96. Containers for suspensionContainers for suspension Suspensions should be packed in amber bottles, plain for internal use and ribbed for external use. There should be adequate air space above the liquid to allow shaking and ease of pouring. A 5 mL medicine spoon or oral syringe should be given when the suspension is for oral use. 03/09/19 BA-FP-JU-C
  • 97. Special label and advice for suspensionSpecial label and advice for suspension The most important additional label for suspensions is 'Shake well before use', Store in a cool place. Stability of suspensions may be adversely affected by both extremes and variations of temperature.  Some suspensions. such as those made from reconstituting dry powders, may need to be stored in a refrigerator. Extemporaneously prepared and reconstituted are required to be recently or freshly prepared, with a 1- 4-week expiry date. 03/09/19 BA-FP-JU-C
  • 98. A simple example,A simple example, Chalk Mixture, Paediatric BP. Mitte 100mlChalk Mixture, Paediatric BP. Mitte 100ml Master formula 100ml Chalk 100mg 2g Tragacanth 10mg 200mg Syrup 0.5ml 10ml Concentrated cinnamon water 0.02ml 0.4ml Double strength chloroform water 2.5ml 50ml Water to 5ml to 100ml 03/09/19 BA-FP-JU-C
  • 99. SummationSummation Suspensions can be used to administer an insoluble solid by the oral route. Suspensions may be used to replace tablets, to improve dissolution rate, to prolong action and to mask a bad taste. Solids may be diffusible or indiffusible and require different dispensing techniques. Stokes' equation can be applied when formulating a suspension to help ensure accurate dosage of the drug. Flocculated particles settle quickly and redisperse easily, whilst deflocculated particles settle slowly but tend to cake. 03/09/19 BA-FP-JU-C
  • 100. SummationSummation Hydrophobic solids may require wetting agents. Suspending agents are added to slow down the rate of settling of the solid. Suspending agents may be natural polysaccharides, semi synthetic polysaccharides, clays or synthetic polymers. Some suspensions are made by adding water to reconstitute manufactured powders when stability is a problem. Shake well before use' and 'Store in a cool place‘ should be part of the labels on a suspension. Inhalations are suspensions of a volatile material adsorbed onto a diffusible solid. 03/09/19 BA-FP-JU-C
  • 101.
  • 102. Semisolid dosage formsSemisolid dosage forms  Semisolid dosage forms meant for external application  Semisolid dosage forms subcategorized are as- I) ointment II) creams III) paste IV) Jellies V) Suppositories  The suppositories are also included in this category but it is a unit dosage forms.
  • 103.
  • 104. OintmentOintment  Ointment are semisolid preparation meant for application to skin or mucous membrane.  The ointments are mainly used for their protective or emollient properties  It may be defined as a medicament or medicaments dissolved, suspended or emulsified in ointment base.  There is no single ointment base which possesses all the qualities of ideal ointment base, so it become necessary to use more than one ointment base in the preparation of ointment.
  • 105. Qualities of ideal ointment baseQualities of ideal ointment base  It should be inert, odourless & colourless & smooth.  It should be physically & chemically stable.  It should be compatible with the skin & with incorporated medicaments.  It should be of such consistency that it spread & soften when applied to skin with stress.  It should not retard healing of wound.  It should produce irritation or sensitization of the skin.
  • 106. Classification of ointment baseClassification of ointment base  Oleaginous bases  Absorption bases  Emulsion bases  Water soluble bases
  • 107. Oleaginous baseOleaginous base  These bases consist of water soluble hydrocarbons, vegetable oils, animal fats & wax.  The constituents of hydrocarbon bases are soft paraffin, hard paraffin & liquid paraffin.  The vegetable oils are mainly used in ointment to lower the melting point or to soften the bases.  These bases serve to keep the medicaments in prolonged contact with the skin & also act as occlusive dressings. They have a low capacity to absorb water & are used chiefly for their emollient effect.  These bases losing their importance now a days for the many reason.
  • 108. Disadvantages of oleaginous basesDisadvantages of oleaginous bases  They are greasy.  They are sticky & are difficult to remove both from skin & clothing.  They retain body heat which may produce an uncomfortable feeling of warmth.  They do not help in the absorption of medicaments.
  • 109. Absorption basesAbsorption bases  These bases are generally anhydrous substance which have the property of absorbing considerable quantities of water but still retaining their ointment like consistency.  The absorption bases are of two type namely as I) Non emulsified bases II) Water in oil emulsion  Non emulsified bases absorb water & aqueous solutions producing w/o emulsion. E.g. Wool fat, wool alcohol, beeswax & cholesterol.  Water in oil emulsions are capable of absorbing more water & have the properties of non- emulsified bases. E.g. hydrous wool fat ( lanoline)
  • 110. Emulsion basesEmulsion bases  These bases are semisolid or have cream like consistency.  Both o/w or w/o emulsions are used as a ointment base.  The o/w emulsion base is more popular now days because ease of application will easily achieved.  The w/o type of emulsion bases are greasy & sticky.  The emulsifying ointment is prepared from emulsifying wax, white soft paraffin & liquid paraffin.
  • 111. Water soluble basesWater soluble bases  These are commonly known as greaseless ointment bases.  The water soluble bases consist of water soluble ingredients such as carbowaxes ( polyethylene glycol polymer)  The carbowaxes are water soluble, non – volatile & inert substance.  Selection of appropriate carbowaxes is depend on their molecular weight.
  • 112.
  • 113. Types of methodTypes of method  Trituation method  Fusion method  Chemical reaction method  Emulsification method
  • 114. TRITURATION METHODTRITURATION METHOD  It is the most commonly used method for the preparationn of ointments.  The method is used when the base is soft and the medicament is insoluble in base.  So for uniform mixing of medicament in the base ,it bacomes necessary to reduce the medicament to fine powder.
  • 115. Fusion methodFusion method When an ointment base contains a number of solid ingredients of different melting points, such as white beeswax,stearic acid,hard paraffin and cetyl alcohol,it is necessary to melt them in decreasing order to their melting point. This will avoid the over heating of the substances having low melting points.
  • 116. Chemical reaction methodChemical reaction method  Certain chemical reactions are involved in the preparation of several ointments.  For example, iodine ointment.  Iodine may be present in free form or in combined formwith the ointment base.
  • 117. Emulsification methodEmulsification method  In this method the fats,oils,and waxes are melted together on a water bath at a temperature of 70 degree Celsius.  The aqueous solution of all the heat stable water soluble component is also heated almost at the same temperature as that of the melted base.
  • 118. CreamsCreams  These are viscous semisolid emulsions which are meant for external use.  Cream is divided in to two types namely as I) Aqueous creams II) Oily creams  In case of aqueous creams the emulsions are o/w type & it is relatively non greasy. The emulsifying waxes are anionic, cationic & non –ionic used. Generally polysorbate, triethanolamine soap are used as emulsifying agent.  In case of oily creams w/o type & it is relatively greasy. The emulsifying agent such as wool fat, wool alcohols, beeswax & calcium soap is used.  The cream should be store in collapsible tube & supplied in well closed container to prevent evaporation & contamination.
  • 119.
  • 120. PastesPastes  Pastes are semisolid preparations intended for external application to skin.  The pastes are generally very thick & stiff.  They do not melt at ordinary temperature & thus forms a protective coating over the area where they are applied.  Pastes are differ from ointment as they contain a high proportion of finely powdered medicaments.  They are mainly used as a antiseptic, protective, soothing dressings.  Pastes should be stored & supplied in containers made of materials which do not allow absorption or diffusion of content.
  • 121. Paste basePaste base  Hydro carbon: Soft paraffin and liquid paraffin are commonly used bases for the preparation of paste.  Water miscible bases: Emulsifying ointment is used as water miscible base for the preparation of pastes  Water soluble bases: Suitable combined of high and low molecular weight polyethylene glycols are mixed together to get product of desired consistancy.
  • 122.
  • 123. SuppositoriesSuppositories  Suppositories are solid dosage form of medicament for insertion into body cavities other than mouth.  They may be inserted into rectum,vagina or nasal cavity suppositories are available in different shapes, sizes and weights.  Suppositories are used to produce local, systemic and mechanical action.
  • 124. ADVANTAGES: 1) THESE ARE INSERTED INTO THE RECTUM TO EXERT A DIRECT AND RAPID ACTION ON THE RECTUM . 2 )THESE ARE INSERTED INTO THE RECTUM TO PROMOTE EVACUATION OF THE BOWL . DISADVANTAGES: 1) THE IRRITANT DRUGS CAN’T BE ADMINISTERED BY THIS ROUTE. 2) SUPPOSITORIES CAUSE EMBARRASSMENT TO THE PATIENT, WHEN A DRUG IS ADMINISTERED BY INSERTING A SUPPOSITORY INTO A BODY CAVITY .
  • 125. TYPES OF SUPPOSITORIESTYPES OF SUPPOSITORIES  RECTAL SUPPOSITORIES : These are meant for introduction into the rectum for their systemic action.  VAGINAL SUPPOSITORIES:These are meant for introduction into the vagina.These suppositories are also know as pessaries and are larger than rectal suppositories.  NASAL SUPPOSITORIES:These are meant for introduced into the nasal cavity and are also know as nasal bougies.  URETHRAL SUPPOSITORIES:These are meant for introduced the urethra and also known as urethral bougies.  EAR CONES:These are meant for introduction into the ear and and also known as aaurinaria.
  • 126.
  • 127. Types of basesTypes of bases Fatty bases Water soluble and water miscible bases Emulsifying bases
  • 128. Fatty basesFatty bases  Theobroma oil: It is a yellowish white solid obtained from crushed and roasted seeds of theobroma cocoa.  It also called as cocoa buttter.  It has butter like consistency having melting point of 30 to 35 degree celsius.  It is a mixture of glycerol ester of of stearic ,oleic,palmitric and other fatty acids.  Theobromal oil melts at body temperature and release the medicament for rapid absorption.  It is readily liquefy on warming and quickly settle on cooling.
  • 129. DisadvantagesDisadvantages  It melts in warm weather.  It has the tendency to stick to the sides of the mould when solidified.  The leakage from the body cavities on melting can take place.  It is relatively costly.  It is immiscible with body fluids.  It shows the phenomena of polymorphism i.e., when theobroma oil is melted and cooled, it gets solidified into different crystalline forms depending upon melting temperature ,rate of cooling and size of the mass.
  • 130. Emusified theobroma oilEmusified theobroma oil  This may be used as abase when large quantity of aqueous solutions are to be incorporated.  The use of 5% glyceryl monostearate,10% lenette wax ,2-3% cetyl alcohol,4% beeswax and 12% spermaceti is recommended to prepare emulsified theobroma oil suppositories.
  • 131. Hydrogenated oilsHydrogenated oils  These are obtained by dehygenation of various vegetables,such as arachi’s oils,cotton seed oils,coconut oils,palm oils,etc., Advantages:  They are resistant to oxidation.  Lubrication of the moulds is not required.  Over heating does not affect the solifying point. Disadvantages:  The suppositories become brittle on rapid cooling in a refrigerator.
  • 132. Water soluble and water miscibleWater soluble and water miscible basesbases  Glycero-gelatin bases:  It is a mixture of glycerine and water which is made stiff by the addition of gelatin.  The bases may be for preparing all types of supositories but it is particularly used for making pessaries.  Soap-glycerin bases:  In glycero-gelatin bases,the gelatin is replaced with either curd soap or sodium stearate which makes the base sufficiently hard to prepare good quality of suppositories.  Soap also helps in the evacuation action of glycerin.
  • 133.  Polyethylene glycol:  Polyethylene glycol polymers are commonly known as carbowaxes or polyglycol or macrogols.  The physical character of these carbowaxes varies according to the molecular weight.  The macrogals having molecular weight less than 1000 are liquids and those with molecular weight higher than 1000 wax like solids.  Advantages:  They are chemically stable.  They are non irritant.  They do not allow to bacteria or mould growth to take place.  They are physically inert substances.
  • 134. Emusifying basesEmusifying bases  Witepsol: They consist of triglycerides of saturated vegetable acid with varying percentage of partial ester.  A small amount of beeswax is used for in hot climates.  Massa estarinum: It is a mixture of mono ,di and triglycerides of saturated fatty acids. This also known as adeps solidus.  Massuppol: It consist of glyceryl esters mainly of lauric acid to which small amount of glyceryl monostearate has been added to improve its water absorbing capacity.  Disadvantages:  They should be cooled rapidly in a refrigerator because they become brittle.  They are not very viscous on melting , so the medication incorporated with the base settle down rapidly.
  • 135. PESSARIESPESSARIES  These are solid preparations containing one or more active incredients and are suitable for vaginal insertion.They are intented for as use as a single dose. Types of pessaries:  Compressed pessaries  Moulded pessaries
  • 136.  Compressed pessaries:  These are also known as vaginal tablets,have the general charecteristics of uncoated tablets but usually large and of great weight . It should be stored in a well cclosed containers ,protected from moisture and being crushed.  Moulded pessaries:  These are manufactured by pouring the liquified mass containing the medicaments and auxillary substances into moulds of suitable volume and cooling inorder to solidify the mass.  Auxillary substances used are macrogols ,theobroma oil and glycerogelatin bases.
  • 137. JelliesJellies  Jellies are transparent or translucent, non greasy, semi solid preparations mainly used for external application to skin.  These are also used for lubricating catheters, surgical gloves & rectal thermometer.  The substance like gelatin, starch, tragacanth, sodium alginate & cellulose derivatives are used for the formulation of jellies.  Jellies are of three types namely as  Medicated jellies  Lubricating jellies  Miscellaneous jellies  Gels: gels may be defined as semisolid preparations which may contain small and large of organic molecules dispersed in a suitable liquid.
  • 138.
  • 139. Introduction With the advancement of pharmaceutical sciences, a new concept have evolved various modern dosage forms & methods of their administration. Some of the modern dosage forms are  Implants  Films & strips  Liposome drug carriers  Controlled drug delivery modules  Erythrocytes  Nanoparticles  prodrugs
  • 140. Implants These are hypodermic tablets are placed under the skin by a minor surgery in order to release drugs over prolonged periods of time.  Now the magnetically controlled implants have been developed which can be opened or closed at will in order to release or stop the drug.  These implants are placed at upper thigh at a depth of 5mm.  These implants are useful in hormone therapy.
  • 141. Films & stripsThese are meant for topical application for slow release of drug over predetermined period of time. Films & strips are more popular these days. They are sub categorized in to following types namely as  Zero order release films  Buccal strips  Spray bandages
  • 142. Zero order release films These are called as laminates & meant for topical application. E.g.  Nitroglycerine laminates are prepared by mixing propylene glycol with about 1% carbopol resin. The mixture is neutralized with NaoH solution & then 0.1% of nitroglycerin is added. It is then placed in polythene sheet 5*5 cm & its edges are sealed by heat. It is then placed on pressure sensitive adhesive sheet of 5.5 * 5.5 cm so that it can be properly adhesive to skin. Such laminates release the drug slowly into circulation for about 12 hours.
  • 143. Buccal strips  The buccal & sublingual tablets are now replaced with buccal strips.  These strips consist of a thin absorbent base of fabrics, filter paper & cotton etc.  The buccal strips are prepared by immersing a long piece of fabric made from polyamide fibers into a molten mixture of carbowaxes & dissolved or dispersed the drug.  The fabric is then cooled & cut into small pieces.  It should be contact with buccal mucosa for about 15 min. & then removed & discarded.
  • 144. Spray bandage  These bandage are prepared by spraying the solution of drug in polylactide (polymer of lactic acid anhydride)  A solution of purified lactide polymer is made in chloroform.  It is then packed in aerosol container having suitable propellant.  When these solution sprayed then it will be a comfortable bandage which can simply washed of with warm water.
  • 145. Liposome drug carriers These are several carriers in our body which transport both to an other like as enzymes, proteins etc.  These are phospholipids which can transport both hydrophilic & hydrophobic drugs.  The large multilamellar vesicles (LMV), small unilamellar vesicles (SUV), large unilamellar vesicles (LUV) are some of the liposome's known today.
  • 146. Applications  Used in diseases caused by intracellular parasites. E.g. malaria, tuberculosis & amoebiasis.  It entrapped insulin is active orally & can be replaced by IM administration of insulin.  It can be used to transport functional DNA/RNA molecules into cell.  It can be used to transport radio pharmaceuticals & immunological products.  Liposomal daunomycin has longer duration of action than free daunomycin which is used in the treatment of neoplasia.
  • 147. Controlled drug delivery modules  These are the device which are formed by embedding the drug within a polymeric matrix so that it gets released slowly to the body over a long period of time.  It will formed drug – polymer complex & may be formulated in to tablet, capsule or any other suitable formulation.  These modules are punctured before administration with leaser beam to make a small orifice for release of the drugs.  The drugs is released from these modules by diffusion, osmosis or chemical reactions.  These are applied to skin, implanted subcutaneously or inserted into various body cavities.
  • 148. Erythrocytes  Erythrocytes are tried in order to achieve controlled release of drugs.  The life span of erythrocytes are 120 days.  It can allow a drug to circulate in the body for long period of time which help slow release of the drugs in to serum.  Released erythrocytes are prepared by putting them in to a hypotonic medium. So that they can easily swollen.  The aqueous solutions of the drug is added to the medium so that drugs gets in to erythrocytes through open pores.  When isotonicity is adjusted the erythrocytes shrink, thus encapsulating the drug with in them. These erythrocytes may be suspended in normal saline solutions for preparing injections.
  • 149. Applications Released erythrocytes of urease have been used in kidney failure to degrade serum urea.  Released erythrocytes of asparaginase have shown good result in asparaginase dependent leukemia.  Released erythrocytes of methotrexate & adrianycin have been tried in cancer therapy.  Released erythrocytes of prednisolone have shown good result to prolong the anti-inflammatory action.
  • 150. Nanoparticles  It is based on colloidal drug delivery system.  The particles size of this system is in nanometer range (200 – 500 mm)  The system consist of a drug & carriers to deposit the drug at target site.  The carriers used are naturally occurring macromolecules like human serum albumin, bovine serum albumin, & other substances like gelatin, casein & ethylcellulose.
  • 151. Applications  Flourescein isothinocyanate (FITC) nanoparticles have been used to incorporate cytotoxic agent into tumor cell in cancer chemotherapy.  Nanoparticles along with biological maker like immunoglobulin can be used to target the drugs to very specific site.
  • 152. Prodrugs  The compound which undergo biotransformation before showing desired pharmacological activity are called prodrugs or proagents.  Prodrugs are generally the ester or amides of parent drugs.  These are useful to improving the stability, solubility, bioavailability of drugs, masking the unpleasant taste & odour of the parent drug & reducing the toxicity
  • 153. Applications  Choramphenicol palmitate, the prodrug of chloramphenicol is used in the preparation of pediatrics suspension because it has no bitter taste.  Procaine penicillin G & benzathine penicillin G are prodrugs of penicillin G which shows resistance to hydrolysis as compared to the parent drug.  Cindamycin 2- phosphate the prodrug of cindamycin has no bitter taste of parent drug.

Notas del editor

  1. The factors are: Particle size, greater the difference in density between the particles and vehic1e, the greater wi11 be the rate of descent. Increasing the viscosity of the dispersion medium, within limits so that the suspension is still pourable, will reduce the rate of sedimentation of a solid drug. Thus a decrease in settling rate in a suspension may be achieved by reducing the size of the partic1es and by increasing the density and the viscosity of the continuous phase. The factors are: Particle size, greater the difference in density between the particles and vehic1e, the greater wi11 be the rate of descent. Increasing the viscosity of the dispersion medium, within limits so that the suspension is still pourable, will reduce the rate of sedimentation of a solid drug. Thus a decrease in settling rate in a suspension may be achieved by reducing the size of the partic1es and by increasing the density and the viscosity of the continuous phase.