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Propranolol Hydrochloride Buccoadhesive Tablet: Development and In-vitro Evaluation

Propranolol HCl is a beta blocker commonly used worldwide; however, it shows a low bioavailability due to its extensive first-pass metabolism. To overcome this problem, a novel drug delivery system such as buccoadhesive system might be helpful. The aim of the present investigation is to prepare the...

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Autores principales: Mortazavi, Seyedeh Maryam, Mortazavi, Seyed Alireza
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Shaheed Beheshti University of Medical Sciences 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7667541/
https://www.ncbi.nlm.nih.gov/pubmed/33224208
http://dx.doi.org/10.22037/ijpr.2019.13866.13346
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author Mortazavi, Seyedeh Maryam
Mortazavi, Seyed Alireza
author_facet Mortazavi, Seyedeh Maryam
Mortazavi, Seyed Alireza
author_sort Mortazavi, Seyedeh Maryam
collection PubMed
description Propranolol HCl is a beta blocker commonly used worldwide; however, it shows a low bioavailability due to its extensive first-pass metabolism. To overcome this problem, a novel drug delivery system such as buccoadhesive system might be helpful. The aim of the present investigation is to prepare the buccoadhesive tablet of propranolol HCl using different mucoadhesive polymers. Buccoadhesive tablets containing drug, lactose, and polymers such as HPMC K4M, carbomer 934P, PEO 8000000 and PEG 6000, in various concentrations, were prepared. The tablets were evaluated in terms of weight variation, thickness, hardness, friability, and mucoadhesive strength. Among thirteen prepared formulations, seven of them which had better physicochemical properties and mucoadhesive strength were undergone the release and swelling tests. Finally, two formulations were selected and uniformity, drug content, duration of mucoadhesion, and kinetic studies were performed for them. All polymers except PEG 6000 were appropriate for being used in buccal mucoadhesive systems. Formulation F(1) was considered as the most desirable formulation as it exhibited appropriate mucoadhesive strength (43.93 ± 12.4 g), extended duration of mucoadhesion (19.15 ± 0.29 h) and suitable swelling ability while having a prolonged drug release over 12 h. Although the efficiency and mucosal irritation of propranolol HCl buccoadhesive tablets should be monitored under the in-vivo conditions, however, based on the results, it seems that such tablets can be considered as an alternative route to bypass the first pass metabolism of propranolol HCl.
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spelling pubmed-76675412020-11-20 Propranolol Hydrochloride Buccoadhesive Tablet: Development and In-vitro Evaluation Mortazavi, Seyedeh Maryam Mortazavi, Seyed Alireza Iran J Pharm Res Original Article Propranolol HCl is a beta blocker commonly used worldwide; however, it shows a low bioavailability due to its extensive first-pass metabolism. To overcome this problem, a novel drug delivery system such as buccoadhesive system might be helpful. The aim of the present investigation is to prepare the buccoadhesive tablet of propranolol HCl using different mucoadhesive polymers. Buccoadhesive tablets containing drug, lactose, and polymers such as HPMC K4M, carbomer 934P, PEO 8000000 and PEG 6000, in various concentrations, were prepared. The tablets were evaluated in terms of weight variation, thickness, hardness, friability, and mucoadhesive strength. Among thirteen prepared formulations, seven of them which had better physicochemical properties and mucoadhesive strength were undergone the release and swelling tests. Finally, two formulations were selected and uniformity, drug content, duration of mucoadhesion, and kinetic studies were performed for them. All polymers except PEG 6000 were appropriate for being used in buccal mucoadhesive systems. Formulation F(1) was considered as the most desirable formulation as it exhibited appropriate mucoadhesive strength (43.93 ± 12.4 g), extended duration of mucoadhesion (19.15 ± 0.29 h) and suitable swelling ability while having a prolonged drug release over 12 h. Although the efficiency and mucosal irritation of propranolol HCl buccoadhesive tablets should be monitored under the in-vivo conditions, however, based on the results, it seems that such tablets can be considered as an alternative route to bypass the first pass metabolism of propranolol HCl. Shaheed Beheshti University of Medical Sciences 2020 /pmc/articles/PMC7667541/ /pubmed/33224208 http://dx.doi.org/10.22037/ijpr.2019.13866.13346 Text en This is an Open Access article distributed under the terms of the Creative Commons Attribution License, (http://creativecommons.org/licenses/by/3.0/) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Original Article
Mortazavi, Seyedeh Maryam
Mortazavi, Seyed Alireza
Propranolol Hydrochloride Buccoadhesive Tablet: Development and In-vitro Evaluation
title Propranolol Hydrochloride Buccoadhesive Tablet: Development and In-vitro Evaluation
title_full Propranolol Hydrochloride Buccoadhesive Tablet: Development and In-vitro Evaluation
title_fullStr Propranolol Hydrochloride Buccoadhesive Tablet: Development and In-vitro Evaluation
title_full_unstemmed Propranolol Hydrochloride Buccoadhesive Tablet: Development and In-vitro Evaluation
title_short Propranolol Hydrochloride Buccoadhesive Tablet: Development and In-vitro Evaluation
title_sort propranolol hydrochloride buccoadhesive tablet: development and in-vitro evaluation
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7667541/
https://www.ncbi.nlm.nih.gov/pubmed/33224208
http://dx.doi.org/10.22037/ijpr.2019.13866.13346
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