A CRITICAL REVIEW ON BUCCAL FILMS A NOVEL FORMULATION OF WIDE SPECTRUM DRUGS

Presented by VINY DAVE

M.Pharm IIIrd semester Department of Pharmacy

Barkatullah Universityat

Sagar Institute of Technology, Bhopal

Guided By Prof. A.K.PathakProf. Aswani Mishra

INDEX Introduction Need for buccal adminstration Limitation Classification of buccal systems Formulation consideration Active pharmaceutical ingredients Methods of manufacturing of buccal film Evaluation of buccal films

INTRODUCTION Buccal administration refers to a topical route of

administration by which drugs held or applied in the buccal area (in the cheek) diffuse through the oral mucosa (tissues which line the mouth) and enter directly into the bloodstream. Buccal administration may provide better bioavailability of some drugs and a more rapid onset of action as compared to oral administration because the medication does not pass through the digestive system and thereby avoids first pass metabolism.

NEED FOR BUCCAL ADMINISTREATIONDrug administration via the buccoadhesive drug

delivery offers several advantages such as: Improved clinical effect which are demonstrated for

pain killers or local anaesthetics. Certain pathologies requires instant release as well

as rapid clinical effect by individual as in case of migraine.

In case of sore, throat, cough, allergy and other local oral manifestations region-specific delivery of medicament is required.

This dosage form can also be used for natural extracts and neutraceuticals including vitamin B12, chromium picolinate melatonin and possibly CoQ10.

As oral cavity rich in blood supply the drugs absorption from buccal cavity is relatively fast.

Due to its good accessibility for membranes which makes application painless and comfort.

Patients can control the period of administration or terminate delivery in case of emergencies..

Drug can be administered in case of unconsciousness and trauma patient

Drug’s bioavailability is increased as it bypass the metabolism.

Drugs which are unstable in acidic environment of stomach can be administered by this delivery.

LIMITATIOJN Drugs which are unstable at buccal pH.cannot be

administered Drugs cannot be formulated for buccal cavity which will

cause allergic reactions, discoloration of teeth or contain antimicrobial agents which affects desired natural microbes..

As compared to sublingual membrane buccal membrane has low permeability.

Drugs which have bitter taste or unpleasant taste or an obnoxious odor or irritate the mucosa are not applicable for this route

FORMULATION CONSIDERATIONS:

Formulation is decided by keeping in mind various parameter such as performance characteristics such as taste masking, fast dissolving, physical appearance, mouth feel etc. Fast dissolving film is a thin film incorporate with an active ingredient.

Sr no. NAME OF EXCIPIENT QUANTITY in %

1 Drug 5-30

2 Film forming agent 40-50

3 Plasticizers 0-20

4 Saliva stimulating agent 2-6

5 Sweetning agent Q.S

6 Surfactant Q.S

7 Flavouring agent Q.S

8 Colouring agent Q.S

CLASSIFICATION OF BUCCAL SYSTEMS

Buccal tablets Buccal semisolid dosage forms Buccal films Buccal powders Micro particle

CHARACTERSTICS OF DRUG REQUIRED

The drug should have following characteristics . The conventional single dose of the drug should be small. The drugs having biological half-life between 2-8 hrs are

good candidates for controlled drug delivery. Tmax of the drug shows wider-fluctuations or higher values

when given orally. Through oral route drug may exhibit first pass effect or

presystemic drug elimination. The drug absorption should be passive when given orally.

ACTIVE PHARMACEUTICAL AGENTS

From any class of drugs, active substance can be used for administration but it must be compatible to the buccal environment. Drug can be added from 5%-25%w/w of total weight of polymer. Dose of drug in mg(less than 20mg/day) is required for effective formulation.

FORMULATION RELATED FACTORS

Molecular Size Partition coefficient pH value pKa value

CLASS OF DRUG USED IN BUCCAL FILM

Several class of drugs can be formulated as mouth dissolving films including paediatrics (anti-tussive, expectorants,anti–asthmatics), geriatrics,antiepileptic,expectorants), gastrointestinal diseases, nausea (e.g. due to cytostatic therapy), pain (e.g. migraine), CNS (ex. Anti Parkinsonism therapy).Depending on their compatibilty with the formulation and different physiochemical properties of Drug .

Anti-emetics Ondansetron, Granisetron, Plonosetron, Dronabinol, Aprepitant, Ramosetron, Trimethobezamide, Nabilone,Metoclopramide, Dolasetron, Dimenhydramine

Serotonin inhibitors

Fluoxetine, Setraline, Paroxetine, Fluxoamine, Citalopram and Alaproclate,

5HT3 antagonists

Alosetron, Ondansetron, Granisetron, Palonosetron, Rmosetron and Tropisetron

Anti-epileptics Carbamezapine, Clonazepalm, Diazepam, Divalproex sodium, Fosphenyloin, Gabapentin, Lamotrigine, Levetiracetam, Oxacarbazepine, Phenytoin, Primidone and Valproate sodium

Anti-migraines Almotriptan, Dihydrogotamine Mesylate, Eletriptan, Frovatriptan, Naratriptan,Rizatriptan, Sumatriptan and Zolmitriptan

Dopamine D1 and D2 antagonists

A misulpride, Bromperidol, Cabergoline, Domeperidone, Fenoldopam, Halopiridol, Metoclopramide, Metopimazine, PergolideMesylate, Prochlorperazine, Quetiapine, Ropinirole Hydrochloride, Sulpiride, Tiapride, and Zotepine

Statins Atorvastatin, Cerivastatin, Fluvastatin, Lovastatin,

Pitavastatin, Pravastatin, Rosuvastatin and

Simvastatin

FEW RECENT RESEARCH DONE IN BUCOADHESIVE DOSAGE FORMDrug Polymer Dosage form

Transforming growth factor-b (TGF-b)

Chitosan-H Gel

Ibuprofen PVP Carboxymethylcellulose sodium salt (NaCMC)

Patch

Nystatin Carbomer Hydroxypropylmethylcellulose Double-Layered tablet

Propranolol Ethyl cellulose, polyvinyl pyrolidone K-30, hydroxypropyl methyl cellulose-15cps,

hydroxyl ethyl cellulose-10cps

Film

Clotrimazole Carbopol-934P Hydroxypropyl cellulose-M Film

Miconazole nitrate Hydroxypropylmethylcellulose, Sodium carboxymethylcellulose, Carbopol 934P,

and sodium alginate.

Slow-Release Tablets

Benzocaine Sodium carboxymethylcellulose, Xanthan gum

Liquid gel, Ointment

METHODS OF MANUFACTURE OF FILMS

Solvent casting Greater uniformity of thickness and much

clarity than extrusion. Film has fine gloss and freedom from defects

such as die lines. More flexibility and better physical Properties

Finished film in thickness is typically 12-100 μm

Hot-melt extrusionBetter method for poorly soluble drugsLower processing steps More uniform dispersion because of intense

mixing and agitationLess energy compared with high shear

methods.

EVALUATIONS OF BUCCAL PATCH: Surface pH Thickness measurements Swelling study. Folding endurance Water absorption capacity test Ex-vivo bioadhesion test In vitro drug release Permeation study of buccal patch Ex-vivo mucoadhesion time:- Measurement of mechanical properties:- Stability study in human saliva

CONCLUSION Pharmaceutical industries have recognized the

potential for delivering medicinal products through buccal film and have launched several products for various kind of drugs in the market using this technology. Recently buccal films have gained popularity as dosage forms. Gaining importance as they are ideal dosage form for use in every categories of patient whether young children, as well as geriatric patients. Also, many industries have pipelines of molecules of shifting their existing tablets preparation to oral strips.

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