design of dosage form

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Presented by
Chinchole Pravin Sonu
M.Pharm. (2nd Sem.)
Dept. of Pharmaceutics and Quality Assurance
R.C.Patel Institute of Pharmaceutical Education and Research, Shirpur,
Maharashtra

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Contents covered in the presentation
R.C.Patel Institute of Pharmaceutical Education and Research, Shirpur, Maharashtra
Introduction
Advantages
Disadvatages
Ideal candidates for BDDS
Anatomy of Buccal mucosa
Formulation of buccal dosage form
 Evaluation of buccal dosage form
References
Conclusion

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Introduction
R.C.Patel Institute of Pharmaceutical Education and Research, Shirpur, Maharashtra
•Administration of a drug via buccal mucosa (lining of
cheek) to the systemic circulation is defined as buccal
delivery.
•The buccal mucosa lies in inner
cheek.
•Placed between upper
gingivae.
•To treat local systemic
condition

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R.C.Patel Institute of Pharmaceutical Education and Research, Shirpur, Maharashtra
Advantages of Buccal Drug Delivery
Avoids first pass metabolism.
Avoids acid/Enzyme metabolism.
Permeation is faster with respect to skin & TDDS (4- 4000)
Large surface area with respect to sub-lingual mucosa.
Good patient compliance with respect to parenteral.
Easy administration & removal in case of toxicity.
For unconscious or comatose patients.

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R.C.Patel Institute of Pharmaceutical Education and Research, Shirpur, Maharashtra
Drugs with bitter taste or irritant to mucosa or having
noxious smell.
Not for children.
Eating & drinking difficulty.
Salivary erosion & it may enter GIT & choke esophagus.
Less surface area than skin.
Drugs unstable at buccal pH(6.5 to 7)
Disadvantages

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•Mucoadhesion of the device is a key element.
•The term ‘mucoadhesive’ is commonly used for
materials that bind to the mucin layer of a biological
membrane.
•Achieve systemic delivery of drugs include tablets,
patches, tapes, films, semisolids and powders.
BDDS and Mucoadhesivity

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Mechanism of Buccal Drug Delivery

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R.C.Patel Institute of Pharmaceutical Education and Research, Shirpur, Maharashtra
1. Molecular size 75-100 Daltons.
2. Molecular weight 200-500
3. Drug should be hydrophilic/hydrophobic in nature.
4. Drug should be stable in buccal pH(6.4-7.2)
5. Drug should be odorless.
6. Drug which are absorbed only by passive diffusion.
Ideal Candidates For Buccal Drug Delivery System

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R.C.Patel Institute of Pharmaceutical Education and Research, Shirpur, Maharashtra
Anatomy of Buccal Mucosa
Structure of oral mucosa
1) Epithelium
- stratum distendum
- stratum filamentosum
- stratum suprabasale
- stratum basale
2) Basal lamina
3) Connective tissue
- lamina propria
- submucosa
Fig- Anatomy of buccal mucosa

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The basic components of buccal drug delivery
system-
 Drug substance
 Bio adhesive polymers
 Backing membrane
 Permeation enhancers
Formulation of BDDS

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IDEAL CHARACTERISTICS:
 Non toxic, non irritable, free from leachable impurities.
Polymer pH should be biocompatible.
Quick adherence, and suffice mechanical strength.
 Bioadhesive in both dry and liquid state.
Acceptable shelf life.
Optimum molecular weight.
TYPES:
1 st generation polymers : PAA, NaCMC , HPMC,
Carbapol , Chitosan , Xanthan gum, PVA etc.
2 nd generation polymers : Lectins , Multifunctional
polymers, Thiolated polymers etc.
Bioadhesive polymer

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 Ability to attachment of bio adhesive device to mucus
membrane
Backing membrane
 Inert in nature and impermeable to the drug
 Such impermeable membrane prevent dug loss and
good patient compliances
 Examples – Carbapol, Magnesium sterate, Polycarbapol

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Substances that help to promote drug permeation through
the buccal epithelium are referred to as penetration enhancers,
permeation promoters or absorption enhancers.
 Most of the compounds used as buccal mucosal penetration
enhancers are the ones generally used to compromise barrier
function.
Examples-sodium lauryl sulfate, sodiumlaurate
Bile salts: Sodium glycodeoxycholate, sodium glycocholate,
sodium taurodeoxycholate, sodium taurocholate
Permeation Enhancers

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R.C.Patel Institute of Pharmaceutical Education and Research, Shirpur, Maharashtra
• Propranalol
• Metoprolol
• Metoclopromide
• Insulin
• Nitro glycerine
• Codeine
• Morphine
• Diltiazem
• Chlorpheniramine maleate
Drugs given as buccal tablets

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Transport Route
R.C.Patel Institute of Pharmaceutical Education and Research, Shirpur, Maharashtra

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R.C.Patel Institute of Pharmaceutical Education and Research, Shirpur, Maharashtra
In vitro
 Swelling rate and bio adhesion studies
Surface pH studies
 Drug release studies
 Permeation studies
Mucoadhesion strength
 Residence time
Evaluation test

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R.C.Patel Institute of Pharmaceutical Education and Research, Shirpur, Maharashtra
In vitro
Animals are sacrificed.
Buccal mucosa with underlying connective tissue is surgically
removed, and then isolated.
Placed and stored in ice-cold (4°C) buffers. (usually Krebs
buffer) .
Generally dogs, monkeys and pigs are used.

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R.C.Patel Institute of Pharmaceutical Education and Research, Shirpur, Maharashtra
In vivo
Drug release studies
Stability studies in human saliva
Ex vivo
Mucoadhesion time
Mucoadhesion force
 Transmucosal permeation studied.

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R.C.Patel Institute of Pharmaceutical Education and Research, Shirpur, Maharashtra
The buccal mucosa offers several advantages for
controlled drug delivery for extended periods of
time. The mucosa is well supplied with both vascular
and lymphatic drainage and first-pass metabolism in
the liver and pre-systemic elimination in the
gastrointestinal tract are avoided.
Conclusion

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References
1.Shojaei Amir H., Buccal Mucosa As A Route For Systemic Drug Delivery: A
Review,
University of Alberta, Faculty of Pharmacy and Pharmaceutical Sciences, Edmonton,
Alberta, Canada, J Pharm Pharmaceut Sci 1 (1):15-30, 1998
2.Hans E. Junginger , Janet A. Hoogstraate, J. Coos Verhoef, Recent advances in
buccal drug delivery and absorption — in vitro and in vivo studies, Journal of
Controlled Release 62 (1999) 149–159
3.N.Chidambaram and A.K.Srivatsava, buccal drug delivery systems, Drug
development and industrial pharmacy, 21(9), 1009-1036 (1995)

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R.C.Patel Institute of Pharmaceutical
Education and Research, Shirpur,
Maharashtra