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Design, evaluation and in vitro - in vivo correlation of glibenclamide buccoadhesive films
BACKGROUND: Glibenclamide (G) is a popular anti-diabetic drug, belonging to the class of sulfonylurea. The drug is widely used for treating type II diabetes but it undergoes first-pass effect. A novel aspiration in treatment of diabetes, to provide greater therapeutic effect, bypass first pass effec...
Autores principales: | , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Medknow Publications & Media Pvt Ltd
2012
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3465157/ https://www.ncbi.nlm.nih.gov/pubmed/23071957 http://dx.doi.org/10.4103/2230-973X.96923 |
Sumario: | BACKGROUND: Glibenclamide (G) is a popular anti-diabetic drug, belonging to the class of sulfonylurea. The drug is widely used for treating type II diabetes but it undergoes first-pass effect. A novel aspiration in treatment of diabetes, to provide greater therapeutic effect, bypass first pass effect and to improve patient compliance upon administering buccal drug delivery of Glibenclamide (G) have not been tested literally. Hence, the present study was designed to develop the buccal mucoadhesive films of glibenclamide by solvent casting technique; that is by using different polymers such as Hydroxy Propyl Methyl Cellulose 15 cps (HPMC), carbopol (CP), and poly vinyl pyrrolidone. Propylene glycol, which served the purpose of plasticizer as well as penetration enhancer and the backing membrane used was aluminium foil. MATERIALS AND METHODS: The films were subjected to physicochemical parameters, in-vitro drug release and ex vivo bucco adhesive strength. RESULTS: The satisfactory results were obtained in all prepared formulation and based on the results G14 [HPMC (150 mg) + CP(20 mg) + PVP (30 mg)] was the best one compared to others. The drug release of all formulation follows zero order kinetics by diffusion mechanism of non-fickian diffusion type. Ex vivo, buccal permeation studies by using sheep buccal mucosa and finally stability studies by using human saliva were carried out for the optimized formulation G14.Good correlation was observed between in-vitro and in vivo correlation, thus revealing the ability of the formulation to reproduce the in-vitro release pattern through the in vivo. CONCLUSION: Glibenclamide muck-adhesive buccal films could be promising one as they, increase bioavailability by bypassing the first pass effect, minimize the dose, reduces the side effects, and improve patient compliance and also glibenclamide might be a right and suitable candidate for oral controlled drug delivery via buccoadhesive films. |
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