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Development and In vitro Evaluation of Mucoadhesive Buccal Films of Nebivolol

Nebivolol, a cardioselective β-blocker undergoes extensive metabolism in the liver after its oral administration resulting in low bioavailability. Oral administration of nebivolol also causes gastrointestinal disturbances characterised by stomach ache. To overcome these short comings, mucoadhesive b...

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Autores principales: Mane, P. P., Bushetti, S. S., Keshavshetti, G. G.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Medknow Publications & Media Pvt Ltd 2014
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4023287/
https://www.ncbi.nlm.nih.gov/pubmed/24843191
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author Mane, P. P.
Bushetti, S. S.
Keshavshetti, G. G.
author_facet Mane, P. P.
Bushetti, S. S.
Keshavshetti, G. G.
author_sort Mane, P. P.
collection PubMed
description Nebivolol, a cardioselective β-blocker undergoes extensive metabolism in the liver after its oral administration resulting in low bioavailability. Oral administration of nebivolol also causes gastrointestinal disturbances characterised by stomach ache. To overcome these short comings, mucoadhesive buccal films of nebivolol were prepared using different concentrations of hydroxypropyl methylcellulose and hydroxyl ethylcellulose in the ratios of 2:1, 4:1 and 6:1 and hydroxypropyl methylcellulose and methylcellulose in the ratio of 2:2, 4:3 and 6:4 by solvent casting technique. All the prepared films were found to be smooth, elegant and uniform in thickness and weight. Among the three polymer combinations used, 6:4 (BFN(6)) showed increased in vitro residence time, which appeared to be mainly due to mucoadhesive nature of hydroxylpropyl methylcellulose and methylcellulose. Evaluation of the films showed uniform dispersion of the drug throughout the formulation (96.21±0.71 to 97.02±0.12%). In vitro drug release studies showed better results at the end of 8 h. The release profile of all the formulations was subjected to kinetic analyses, which suggested that the drug was released by diffusion mechanism following super case-II transport.
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spelling pubmed-40232872014-05-19 Development and In vitro Evaluation of Mucoadhesive Buccal Films of Nebivolol Mane, P. P. Bushetti, S. S. Keshavshetti, G. G. Indian J Pharm Sci Short Communication Nebivolol, a cardioselective β-blocker undergoes extensive metabolism in the liver after its oral administration resulting in low bioavailability. Oral administration of nebivolol also causes gastrointestinal disturbances characterised by stomach ache. To overcome these short comings, mucoadhesive buccal films of nebivolol were prepared using different concentrations of hydroxypropyl methylcellulose and hydroxyl ethylcellulose in the ratios of 2:1, 4:1 and 6:1 and hydroxypropyl methylcellulose and methylcellulose in the ratio of 2:2, 4:3 and 6:4 by solvent casting technique. All the prepared films were found to be smooth, elegant and uniform in thickness and weight. Among the three polymer combinations used, 6:4 (BFN(6)) showed increased in vitro residence time, which appeared to be mainly due to mucoadhesive nature of hydroxylpropyl methylcellulose and methylcellulose. Evaluation of the films showed uniform dispersion of the drug throughout the formulation (96.21±0.71 to 97.02±0.12%). In vitro drug release studies showed better results at the end of 8 h. The release profile of all the formulations was subjected to kinetic analyses, which suggested that the drug was released by diffusion mechanism following super case-II transport. Medknow Publications & Media Pvt Ltd 2014 /pmc/articles/PMC4023287/ /pubmed/24843191 Text en Copyright: © Indian Journal of Pharmaceutical Sciences http://creativecommons.org/licenses/by-nc-sa/3.0 This is an open-access article distributed under the terms of the Creative Commons Attribution-Noncommercial-Share Alike 3.0 Unported, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Short Communication
Mane, P. P.
Bushetti, S. S.
Keshavshetti, G. G.
Development and In vitro Evaluation of Mucoadhesive Buccal Films of Nebivolol
title Development and In vitro Evaluation of Mucoadhesive Buccal Films of Nebivolol
title_full Development and In vitro Evaluation of Mucoadhesive Buccal Films of Nebivolol
title_fullStr Development and In vitro Evaluation of Mucoadhesive Buccal Films of Nebivolol
title_full_unstemmed Development and In vitro Evaluation of Mucoadhesive Buccal Films of Nebivolol
title_short Development and In vitro Evaluation of Mucoadhesive Buccal Films of Nebivolol
title_sort development and in vitro evaluation of mucoadhesive buccal films of nebivolol
topic Short Communication
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4023287/
https://www.ncbi.nlm.nih.gov/pubmed/24843191
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