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Recent advances in
tablet

October 20, 2013

etn ashtami semwal

1
Recent advances in





Tablet formulation
New techniques
Recent equipments
New polymers

October 20, 2013

etn ashtami semwal

2
Tablet Formulation






Mouth Dissolving Tablet
Microtablet
Fast-melting Tablets Based On Highly Plastic
Granules
3-dimensional Printing Technology In Tablet

October 20, 2013

etn ashtami semwal

3
Mouth dissolving tablet
Chatap V.K ,gupta R.D ,jaiswal N.R, M.P India oct 2007 .

This tablet fast disintegrates when placed on
tongue.release the drug that dissolve in
saliva.
 Also known as orodispersible,fast
disintegrating,rapiment,porous tablet.


October 20, 2013

etn ashtami semwal

4
Mouth dissolving tablet
Techniques:
 Freeze drying
 Moulding
 Sublimation
 Spray drying
 Direct compression
 Wet granulation
 Dry granulation
October 20, 2013

etn ashtami semwal

5
Mouth dissolving tablet:
Patented technology:






Zydus technology
Durasolve technology
Orasolve technology
Flash dose technology
Sheaform technology

October 20, 2013



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Ceform technology
Wowtab technology
Flashtab technology
Cotton candy
technology

etn ashtami semwal

6
Microtablet
Gul Majid khan ,DOP ,Pakistan.





Prepared by wet granulation method.
Hydrophillic matrix was formed with xanthin
gum,karaya gum,HPMC together with a
choice of additives from Lactose,avicel PH
101,Talc & Lubritab.
Multiunit dosage form obtained by
encapsulating the mini matrix tablet into hard
gelatin capsule.

October 20, 2013

etn ashtami semwal

7
Fast-melting tablets
Yourong Fua, Seong Hoon Jeongb and Kinam Parkb, aAkina Inc., 1291
Cumberland Ave., West Lafayette, IN 47906, USA, 2 November 2005.




Highly plastic granules that can be compressed into tablets at
low pressure were developed to make fast-melting tablets
(FMTs) by compression method.
The highly plastic granules are composed of three components
highly plastic
granules

plastic material
October 20, 2013

material enhancing
water penetration

etn ashtami semwal

Wet binder
8
3-Dimensional Printing technology in
tablet
Chee Kong Lai,1 Wendy E. Katstra,1Department of Materials Science and
Engineering, Massachusetts Institute of Technology, Cambridge, MA
02139: January 27, 2004







A system using light-induced fluorescence (LIF)
technology was developed for rapid and
nondestructive analysis of active pharmaceutical
ingredients on tablet surfaces.
Non homogeneous tablets with defined layer of
active ingredients were made by 3-Dimensional
Printing technology to determine penetration depths
of the light source and the resultant fluorescence
responses.
The LIF method of analysis showed penetration to
depths of up to 3 mm into tablets.

October 20, 2013

etn ashtami semwal

9
3-Dimensional Printing technology in
tablet






A correlation between LIF signals from analysis of
tablet surfaces and the total drug content of the
respective tablets was established.
This method of surface analysis was verified with UV
spectrometric methods.
The use of on-line monitoring of the individual tablet
for surface content up to 3000 tablets a minute.

October 20, 2013

etn ashtami semwal

10
Recent Advancement in
Granulations
http//www.pharmapedia.com

Steam Granulation
 Melt Granulation
 Moisture Activated Dry Granulation
 Thermal Adhesion Granulation Process
 Foam Granulation


October 20, 2013

etn ashtami semwal

11
Steam Granulation






It is modification of wet granulation. Here steam is
used as a binder instead of water.
Its several benefits includes higher distribution
uniformity, higher diffusion rate into powders, more
favourable thermal balance during drying step.
Processing time is shorter therefore more number of
tablets are produced per batch.

October 20, 2013

etn ashtami semwal

12
Melt Granulation /
Thermoplastic Granulation








Here granulation is achieved by the addition of
meltable binder.
That is binder is in solid state at room temperature but
melts in the temperature range of 50 – 80˚C.
There is no need of drying phase.
Producing SR granulation or solid dispersion.
Polyethylene Glycol (PEG) is used as melting
binders. When water insoluble binders are needed.

October 20, 2013

etn ashtami semwal

13
Moisture Activated Dry Granulation
(MADG)










It involves minimal moisture addition, distribution and
agglomeration.
No drying step is required.
Water distribution is via high shear mixer, or low-shear mixer
with highly atomized water spray.
Better content uniformity than direct compression.
Excess moisture is absorbed by hydrophilic polymers such as
cellulose or silica added to the moist pre-blend.
Applicable to controlled release.

October 20, 2013

etn ashtami semwal

14
Thermal Adhesion Granulation
Process (TAGP)






It is applicable for preparing direct tableting
formulations.
TAGP is performed by subjecting a mixture
containing excipients to heating at a temperature in
the range from about 30ºC to about 130ºC in a closed
system under mixing by tumble rotation until the
formation of granules.
It provides granules with good flow properties and
binding capacity to form tablets of low friability,
adequate hardness and have a high uptake capacity
for active substances whose tableting is poor.

October 20, 2013

etn ashtami semwal

15
Foam Granulation





Here liquid binders are added as aqueous foam.
useful for granulating water sensitive formulations,
Reduces drying time
Reduce manufacturing time, less binder required for
Immediate Release (IR) and Controlled Release (CR)
formulations.

October 20, 2013

etn ashtami semwal

16
Recent Coating Techniques

Electrostatic coating

October 20, 2013

Dry coating

etn ashtami semwal

17
Electrostatic dry powder coating for
Immediate release
Eur J Pharm Biopharm. 2010 Jun 19. Qiao M ,Zhang L, Ma Y,Zhu J ,Chow K.
University of Western Ontario, canada







Developed electrostatic dry powder coating in a pan
coater system.
Two immediate release coating compositions
Opadry(R) AMB and Eudragit(R) EPO were
successfully applied using this process.
A liquid plasticizer was sprayed onto the surface of
the tablet cores to increase the conductivity of tablet
cores to enhance particle deposition,

October 20, 2013

etn ashtami semwal

18
Electrostatic dry powder coating for
Immediate release






The application of liquid plasticizer was followed by
spraying charged coating particles using an
electrostatic charging gun to enhance the uniform
deposition on tablet surface.
The coating particles were coalesced into a thin film
by acceptable processing temperature as formation
was confirmed by SEM micrographs.
The results also show coating process produces
tablets with smooth surface.

October 20, 2013

etn ashtami semwal

19
Dry coating in a rotary fluid bed
Caroline Désirée Kablitz , a, Kim Hardera, and Nora Anne
Urbanetza a Institute of Pharmaceutics, Germany 14 November
2005.






A highly efficient dry coating process was developed
to obtain an enteric film avoiding completely the use
of organic solvents and water.
Using hydroxypropyl methylcellulose acetate
succinate (HPMCAS) an enteric coat should be
obtained without adding talc as anti-tacking agent
because of problems arising from microbiological
contamination..
The process was conducted in the rotary fluid bed .

October 20, 2013

etn ashtami semwal

20
Dry coating in a rotary fluid bed




The determined coating efficiency of the talcfree formulation was high with 94% and
storage stability regarding tacking could be
achieved using colloidal silicon dioxide as top
powder.
coating process in rotary fluid bed. serious
alternative to conventional solvent or water
based coating processes.

October 20, 2013

etn ashtami semwal

21
Automated Equipment




Currently several supplier of equipment are develop
and introducing automated system which not only
monitor & control each important parameter but
integrate the controls so that a change in one
condition cause a corrective or compensating action
in the system.
If change is critical the system shut itself down.

October 20, 2013

etn ashtami semwal

22
Automated Equipment
Automated Equipment attached to each other.

SIFTER
AUTOMATI
C

RMG
CO-MILL
DISCHARGE BOWL/FBD
BOWL
Automated Equipment
MANUAL

FBD BOWL
FBD

{RECIPE

SET}
AUTOMATI
C

BLENDER
COMPRESSION
MACHINE
Automated Equipment
COMPRESSION MACHINE
AUTOMATI
C

BLISTER/STRIP MACHINE
CARTON
AUTOFILL

MANUA
L

SHIPPER
Automated Equipment

October 20, 2013

etn ashtami semwal

26
New non contact firm grip handler new
tablet printing machine
Purto rico,NY javits apr 2007 newyork







Its capable printing of clear quality character
number,bar codes,logos ,data on tablet.
Its capable of 250-750,000 tablets per hour.
100% vision product verification camera
station is an automated.
Computerized control is integrated with a 21
CFR part 11.

October 20, 2013

etn ashtami semwal

27
NEW POLYMERS







AQUA ZEIN
HYDROXYPROPYL
DERIVATIVE
FG 90 CHITOSAN
EUDRAGIT
International Journal of Pharmaceutics
Volume 377, Issues 1-2, 30 July 2009, Pages 1201-2,
127

Disintegrating material




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



October 20, 2013

CYCLODEXTRIN
MALTODEXTRIN
CORNSTARCH
ALGINIC ACID
METHOCEL®
STARCH-AGAR
MIXTURE
VEEGUM® HV

etn ashtami semwal

28
October 20, 2013

etn ashtami semwal

29

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Recent Advances in Tablet Formulation Technologies

  • 1. Recent advances in tablet October 20, 2013 etn ashtami semwal 1
  • 2. Recent advances in     Tablet formulation New techniques Recent equipments New polymers October 20, 2013 etn ashtami semwal 2
  • 3. Tablet Formulation     Mouth Dissolving Tablet Microtablet Fast-melting Tablets Based On Highly Plastic Granules 3-dimensional Printing Technology In Tablet October 20, 2013 etn ashtami semwal 3
  • 4. Mouth dissolving tablet Chatap V.K ,gupta R.D ,jaiswal N.R, M.P India oct 2007 . This tablet fast disintegrates when placed on tongue.release the drug that dissolve in saliva.  Also known as orodispersible,fast disintegrating,rapiment,porous tablet.  October 20, 2013 etn ashtami semwal 4
  • 5. Mouth dissolving tablet Techniques:  Freeze drying  Moulding  Sublimation  Spray drying  Direct compression  Wet granulation  Dry granulation October 20, 2013 etn ashtami semwal 5
  • 6. Mouth dissolving tablet: Patented technology:      Zydus technology Durasolve technology Orasolve technology Flash dose technology Sheaform technology October 20, 2013     Ceform technology Wowtab technology Flashtab technology Cotton candy technology etn ashtami semwal 6
  • 7. Microtablet Gul Majid khan ,DOP ,Pakistan.    Prepared by wet granulation method. Hydrophillic matrix was formed with xanthin gum,karaya gum,HPMC together with a choice of additives from Lactose,avicel PH 101,Talc & Lubritab. Multiunit dosage form obtained by encapsulating the mini matrix tablet into hard gelatin capsule. October 20, 2013 etn ashtami semwal 7
  • 8. Fast-melting tablets Yourong Fua, Seong Hoon Jeongb and Kinam Parkb, aAkina Inc., 1291 Cumberland Ave., West Lafayette, IN 47906, USA, 2 November 2005.   Highly plastic granules that can be compressed into tablets at low pressure were developed to make fast-melting tablets (FMTs) by compression method. The highly plastic granules are composed of three components highly plastic granules plastic material October 20, 2013 material enhancing water penetration etn ashtami semwal Wet binder 8
  • 9. 3-Dimensional Printing technology in tablet Chee Kong Lai,1 Wendy E. Katstra,1Department of Materials Science and Engineering, Massachusetts Institute of Technology, Cambridge, MA 02139: January 27, 2004    A system using light-induced fluorescence (LIF) technology was developed for rapid and nondestructive analysis of active pharmaceutical ingredients on tablet surfaces. Non homogeneous tablets with defined layer of active ingredients were made by 3-Dimensional Printing technology to determine penetration depths of the light source and the resultant fluorescence responses. The LIF method of analysis showed penetration to depths of up to 3 mm into tablets. October 20, 2013 etn ashtami semwal 9
  • 10. 3-Dimensional Printing technology in tablet    A correlation between LIF signals from analysis of tablet surfaces and the total drug content of the respective tablets was established. This method of surface analysis was verified with UV spectrometric methods. The use of on-line monitoring of the individual tablet for surface content up to 3000 tablets a minute. October 20, 2013 etn ashtami semwal 10
  • 11. Recent Advancement in Granulations http//www.pharmapedia.com Steam Granulation  Melt Granulation  Moisture Activated Dry Granulation  Thermal Adhesion Granulation Process  Foam Granulation  October 20, 2013 etn ashtami semwal 11
  • 12. Steam Granulation    It is modification of wet granulation. Here steam is used as a binder instead of water. Its several benefits includes higher distribution uniformity, higher diffusion rate into powders, more favourable thermal balance during drying step. Processing time is shorter therefore more number of tablets are produced per batch. October 20, 2013 etn ashtami semwal 12
  • 13. Melt Granulation / Thermoplastic Granulation      Here granulation is achieved by the addition of meltable binder. That is binder is in solid state at room temperature but melts in the temperature range of 50 – 80˚C. There is no need of drying phase. Producing SR granulation or solid dispersion. Polyethylene Glycol (PEG) is used as melting binders. When water insoluble binders are needed. October 20, 2013 etn ashtami semwal 13
  • 14. Moisture Activated Dry Granulation (MADG)       It involves minimal moisture addition, distribution and agglomeration. No drying step is required. Water distribution is via high shear mixer, or low-shear mixer with highly atomized water spray. Better content uniformity than direct compression. Excess moisture is absorbed by hydrophilic polymers such as cellulose or silica added to the moist pre-blend. Applicable to controlled release. October 20, 2013 etn ashtami semwal 14
  • 15. Thermal Adhesion Granulation Process (TAGP)    It is applicable for preparing direct tableting formulations. TAGP is performed by subjecting a mixture containing excipients to heating at a temperature in the range from about 30ºC to about 130ºC in a closed system under mixing by tumble rotation until the formation of granules. It provides granules with good flow properties and binding capacity to form tablets of low friability, adequate hardness and have a high uptake capacity for active substances whose tableting is poor. October 20, 2013 etn ashtami semwal 15
  • 16. Foam Granulation     Here liquid binders are added as aqueous foam. useful for granulating water sensitive formulations, Reduces drying time Reduce manufacturing time, less binder required for Immediate Release (IR) and Controlled Release (CR) formulations. October 20, 2013 etn ashtami semwal 16
  • 17. Recent Coating Techniques Electrostatic coating October 20, 2013 Dry coating etn ashtami semwal 17
  • 18. Electrostatic dry powder coating for Immediate release Eur J Pharm Biopharm. 2010 Jun 19. Qiao M ,Zhang L, Ma Y,Zhu J ,Chow K. University of Western Ontario, canada    Developed electrostatic dry powder coating in a pan coater system. Two immediate release coating compositions Opadry(R) AMB and Eudragit(R) EPO were successfully applied using this process. A liquid plasticizer was sprayed onto the surface of the tablet cores to increase the conductivity of tablet cores to enhance particle deposition, October 20, 2013 etn ashtami semwal 18
  • 19. Electrostatic dry powder coating for Immediate release    The application of liquid plasticizer was followed by spraying charged coating particles using an electrostatic charging gun to enhance the uniform deposition on tablet surface. The coating particles were coalesced into a thin film by acceptable processing temperature as formation was confirmed by SEM micrographs. The results also show coating process produces tablets with smooth surface. October 20, 2013 etn ashtami semwal 19
  • 20. Dry coating in a rotary fluid bed Caroline Désirée Kablitz , a, Kim Hardera, and Nora Anne Urbanetza a Institute of Pharmaceutics, Germany 14 November 2005.    A highly efficient dry coating process was developed to obtain an enteric film avoiding completely the use of organic solvents and water. Using hydroxypropyl methylcellulose acetate succinate (HPMCAS) an enteric coat should be obtained without adding talc as anti-tacking agent because of problems arising from microbiological contamination.. The process was conducted in the rotary fluid bed . October 20, 2013 etn ashtami semwal 20
  • 21. Dry coating in a rotary fluid bed   The determined coating efficiency of the talcfree formulation was high with 94% and storage stability regarding tacking could be achieved using colloidal silicon dioxide as top powder. coating process in rotary fluid bed. serious alternative to conventional solvent or water based coating processes. October 20, 2013 etn ashtami semwal 21
  • 22. Automated Equipment   Currently several supplier of equipment are develop and introducing automated system which not only monitor & control each important parameter but integrate the controls so that a change in one condition cause a corrective or compensating action in the system. If change is critical the system shut itself down. October 20, 2013 etn ashtami semwal 22
  • 23. Automated Equipment Automated Equipment attached to each other. SIFTER AUTOMATI C RMG CO-MILL DISCHARGE BOWL/FBD BOWL
  • 25. Automated Equipment COMPRESSION MACHINE AUTOMATI C BLISTER/STRIP MACHINE CARTON AUTOFILL MANUA L SHIPPER
  • 26. Automated Equipment October 20, 2013 etn ashtami semwal 26
  • 27. New non contact firm grip handler new tablet printing machine Purto rico,NY javits apr 2007 newyork     Its capable printing of clear quality character number,bar codes,logos ,data on tablet. Its capable of 250-750,000 tablets per hour. 100% vision product verification camera station is an automated. Computerized control is integrated with a 21 CFR part 11. October 20, 2013 etn ashtami semwal 27
  • 28. NEW POLYMERS      AQUA ZEIN HYDROXYPROPYL DERIVATIVE FG 90 CHITOSAN EUDRAGIT International Journal of Pharmaceutics Volume 377, Issues 1-2, 30 July 2009, Pages 1201-2, 127 Disintegrating material        October 20, 2013 CYCLODEXTRIN MALTODEXTRIN CORNSTARCH ALGINIC ACID METHOCEL® STARCH-AGAR MIXTURE VEEGUM® HV etn ashtami semwal 28
  • 29. October 20, 2013 etn ashtami semwal 29