2. Topicals
•Preparations applied to the skin either for their
physical effects or for the specific effect of a medicinal
agent
•Protectants, lubricants, emollients, drying agents,
astringents
Transdermals
•Designed to support the passage of drug substances from
the surface of the skin, through its various layers, and even
into the systemic circulation
INTRODUCTION
3. Functions of Dermatologicals
•Protect injured areas from the environment
•Provide for skin hydration (emollient)
•Vehicle for medication transport
Drug Penetration Is Dependent Upon:
•Amount of pressure and vigor of rubbing
•Surface area covered
•Condition of the skin
•Base used
•Occlusive dressing use
Application Areas for Dermatologicals
LOTIONS
CREAMS
OINTMENTS
Intertriginous areas
Moist, weeping lesions
Dry, scaly lesions
INTRODUCTION
4. Ointments
•Semisolid preparations intended for external
application to the skin or mucous membranes.
•Semisolid plastic flow characteristics
•Definite yield value
•Resistance to flow drops as application continues
5. Compendial Requirements for Ointments
•Microbial Content
•Minimum Fill
•Packaging, Storage, and Labeling
•Additional Standards
•Oleaginous Bases
•Absorption Bases
•Water-Removable Bases
•Water-Soluble Bases
Ointment Bases Preparation of Ointments
•Incorporation
•Fusion
Ointments
7. Emulsion Base
Water-in-Oil
•Water insoluble
•Not water
washable
•Can absorb water
•Contains water
Examples:
•Cold Cream (Petrolatum-Rose Water Ointment)
•Lanolin
•Nivea
•Eucerin
Emulsion Bases
Oil-in-Water
•Water insoluble
•Water washable
•Can absorb water
•Contains water
Examples:
•Hydrophilic Ointment
•Velvachol
•Unibase
•Dermabase
•Vanicream
•Acid Mantle
Ointments
8. Humectants
•Glycerin
•Propylene glycol
•Sorbitol 70%
Water-Soluble Bases
•Water soluble
•Water washable
•Can absorb water
•Anhydrous or hydrous
•All water soluble, no oil phase
Example:
•Polyethylene Glycol Ointment
•Biozyme Ointment, Desenex Ointment,
Whitfields Ointment
•Veegum 10% Dermatological base
•Veegum 5% Thixotropic lotion
Ointments
9. Selection of the Appropriate Base
•Release rate
•Topical or percutaneous drug absorption
•Occlusion
•Stability of drug
•Effect of drug on ointment base
•Easily removable?
•Characteristics of surface for application
Incorporation
•Mortar and pestle
•Pill tile and spatula
•Ointment mill
•Unguator
•Incorporation of solids
•Incorporation of liquid
Ointment Preparation
•Ointment Slab/Pill Tile
•Mortar/Pestle
•Ointment Mill
•Fusion
Heat highest melting point material
first
Water phase a few degrees higher
W/O: add water slowly
O/W: add oil slowly
Ointments
10. Ointment Packaging
•Jars: Glass, Plastic
Do not pour in while hot!
•Disp. Jars: Plastic
•Tubes: Plastic, tin, aluminum
•Syringes: Individually dosed, good
protection of the product
Labeling and Storage
•Labeling
Protect with tape
Dual labels
Creativity often required
•Storage
Store in a cool place
Ointments
11. Creams
•Opaque, soft solids, or thick liquids intended for external
application.
•Semisolid, pseudoplastic flow
•Very little yield value
•Won’t flow under force of gravity but small force will
initiate flow
•Viscous liquids or semisolid emulsions of either the O/W
type or the W/O type
•Term “cream” is most frequently applied to soft,
cosmetically acceptable types of preparations.
12. Gels
•Semisolid systems consisting of dispersions of small or
large molecules in an aqueous liquid vehicle rendered
jelly-like through the addition of a gelling agent
•A semirigid system in which the movement of the
dispersing medium is restricted by an interlacing
network of particles or solvated macromolecules of the
dispersed phase
13. Types of Gels
•Single Phase
Gels in which the macromolecules
are uniformly distributed throughout
a liquid with no apparent boundaries
between the dispersed
macromolecules and the liquid
Usually involve organics
•Two Phase
When the gel mass consists of
floccules of small distinct particles
Usually involve inorganics
Gels
14. Gel Composition
•Gelling agent
•Water
•Cosolvents
•Preservatives
•Stabilizers
Kinds of Gels
•Hydrogels
Silica, bentonite, pectin, sodium alginate,
methylcellulose, alumina
•Organic Gels
Contain an organic liquid (e.g., Plastibase)
•Carbomer Gels
Aqueous dispersion neutralized with sodium
hydroxide or triethanolamine
•Methylcellulose Gels
•Starch Glycerite
•Aluminum Hydroxide Gel
Gelation
•As a hot, colloidal dispersion of gelatin
cools, the gelatin macromolecules lose
kinetic energy.
•With a reduction of kinetic energy or
thermal agitation.
•Gelatin, agar, pectin, Irish moss, pectin,
tragacanth form gels by this mechanism.
Gels
15. Phenomena Associated with Gels
•Syneresis
- When the interaction between particles of the dispersed phase
becomes so great that on standing, the dispersing medium is
squeezed out in droplets and the gel shrinks
•Swelling
-The taking up of liquid by a gel with an increase in volume
•Imbibition
- The taking up of a certain amount of liquid without a measurable
increase in volume
•Thixotropy
-A reversible gel-sol formation with no change in volume or
temperature
•Jelene/Plastibase
- A combination of mineral oils and heavy hydrocarbon waxes with a
MW of about 1300
•Carbomer 934
- A polymer of acrylic acid cross-linked with a polyfunctional agent;
recognized as an official emulsifying and suspending agent
Gels
19. Features and Use of Ophthalmic
Ointments and Gels
•Relative short residence time after
application
•Sterile
•Nonirritating
•Softening point close to body
temperature
•Application technique
Features and Use of Nasal Ointments and Gels
•Primarily local effects but some systemic
also
•Rich blood supply in nasal lining
Gels
20. Features and Use of Rectal Preparations
•Ointments, creams, gels
•Perianal area and anal canal
•Anorectal pruritus, inflammation,
hemorrhoids
•Proper instruction for use to patient
Features and Use of Vaginal Preparations
•Ointments, creams, foams, and gels
•Anti-infectives, hormones, pH modifiers,
spermicides
Gels
21. Pastes
•Thick, stiff ointments that do not
ordinarily flow at body temperature, and
therefore serve as protective coatings
over the areas to which they are applied.
Usually >20% solids.
•Semisolid, dilatant flow
•Definite yield value
•Resistance to flow increased with
increased force of application
Lotions
•Aqueous preparations with insoluble
material for external application without
friction
•Fluid preparations, Newtonian flow
•No yield value
•Flow under gravity
•“Lotions” actually also refers to fluid oil-
in-water and water-in-oil emulsions.
Others
22. Cerates
•Semisolid preparations containing a
relatively high wax content
•Semisolid
•High yield point
•Not to be directly rubbed onto skin
Plasters
•Solid or semisolid preparations that
cannot be spread at room temperature
Cataplasms or Poultices
•Wet masses of solid matter applied to the skin
to reduce inflammation and act as
counterirritants
Others