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Formulation and evaluation of carvedilol melt-in-mouth tablet using mucoadhesive polymer and PEG-6-stearate as hydrophilic waxy binder

PURPOSE: The demand for melt-in-mouth tablets (MMTs) has been rapidly growing during the last decade, especially for the elderly and children who have swallowing difficulties, to avoid first-pass metabolism and quick drug entry into the systemic circulation. MATERIALS AND METHODS: In this work, a ne...

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Autores principales: Dangi, Amish Ashvinkumar, Zalodiya, Prakash Bhikhabhai
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Medknow Publications & Media Pvt Ltd 2012
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3618634/
https://www.ncbi.nlm.nih.gov/pubmed/23580934
http://dx.doi.org/10.4103/2230-973X.106989
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author Dangi, Amish Ashvinkumar
Zalodiya, Prakash Bhikhabhai
author_facet Dangi, Amish Ashvinkumar
Zalodiya, Prakash Bhikhabhai
author_sort Dangi, Amish Ashvinkumar
collection PubMed
description PURPOSE: The demand for melt-in-mouth tablets (MMTs) has been rapidly growing during the last decade, especially for the elderly and children who have swallowing difficulties, to avoid first-pass metabolism and quick drug entry into the systemic circulation. MATERIALS AND METHODS: In this work, a new approach has been tried to prepare MMTs using a hydrophilic waxy binder [polyethylene glycol (PEG)-6-stearate]. Carvedilol MMTs were prepared by direct compression method using different mucoadhesive polymers such as hydroxypropyl methylcellulose (HPMC), chitosan, and sodium carboxymethyl cellulose (Na-CMC) at various concentrations (range: 0.5–5%) to reduce the flushing action of saliva and to increase mucosal absorption. All the formulations were evaluated for various physiochemical parameters, and the formulations containing the maximum amount of polymer (F4, F7, and F10) were selected for further stability study. RESULTS: The deaggregation time of the tablets was found to be rapid, and the dissolution test revealed that carvedilol was dissolved from the formulation within the compendia limits. This data confirmed that the polymer concentration (0.5–5%) was within acceptable limits. It was also concluded that avicel PH101, pearlitol SD 200, and croscarmellose sodium (CCS) were the appropriate excipients and formulated in the right proportion. CONCLUSION: As a result, mouth dissolving administration of carvedilol formulated with appropriate excipients and especially with chitosan seems a promising alternative to traditional routes.
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spelling pubmed-36186342013-04-11 Formulation and evaluation of carvedilol melt-in-mouth tablet using mucoadhesive polymer and PEG-6-stearate as hydrophilic waxy binder Dangi, Amish Ashvinkumar Zalodiya, Prakash Bhikhabhai Int J Pharm Investig Original Research Article PURPOSE: The demand for melt-in-mouth tablets (MMTs) has been rapidly growing during the last decade, especially for the elderly and children who have swallowing difficulties, to avoid first-pass metabolism and quick drug entry into the systemic circulation. MATERIALS AND METHODS: In this work, a new approach has been tried to prepare MMTs using a hydrophilic waxy binder [polyethylene glycol (PEG)-6-stearate]. Carvedilol MMTs were prepared by direct compression method using different mucoadhesive polymers such as hydroxypropyl methylcellulose (HPMC), chitosan, and sodium carboxymethyl cellulose (Na-CMC) at various concentrations (range: 0.5–5%) to reduce the flushing action of saliva and to increase mucosal absorption. All the formulations were evaluated for various physiochemical parameters, and the formulations containing the maximum amount of polymer (F4, F7, and F10) were selected for further stability study. RESULTS: The deaggregation time of the tablets was found to be rapid, and the dissolution test revealed that carvedilol was dissolved from the formulation within the compendia limits. This data confirmed that the polymer concentration (0.5–5%) was within acceptable limits. It was also concluded that avicel PH101, pearlitol SD 200, and croscarmellose sodium (CCS) were the appropriate excipients and formulated in the right proportion. CONCLUSION: As a result, mouth dissolving administration of carvedilol formulated with appropriate excipients and especially with chitosan seems a promising alternative to traditional routes. Medknow Publications & Media Pvt Ltd 2012 /pmc/articles/PMC3618634/ /pubmed/23580934 http://dx.doi.org/10.4103/2230-973X.106989 Text en Copyright: © International Journal of Pharmaceutical Investigation 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 Original Research Article
Dangi, Amish Ashvinkumar
Zalodiya, Prakash Bhikhabhai
Formulation and evaluation of carvedilol melt-in-mouth tablet using mucoadhesive polymer and PEG-6-stearate as hydrophilic waxy binder
title Formulation and evaluation of carvedilol melt-in-mouth tablet using mucoadhesive polymer and PEG-6-stearate as hydrophilic waxy binder
title_full Formulation and evaluation of carvedilol melt-in-mouth tablet using mucoadhesive polymer and PEG-6-stearate as hydrophilic waxy binder
title_fullStr Formulation and evaluation of carvedilol melt-in-mouth tablet using mucoadhesive polymer and PEG-6-stearate as hydrophilic waxy binder
title_full_unstemmed Formulation and evaluation of carvedilol melt-in-mouth tablet using mucoadhesive polymer and PEG-6-stearate as hydrophilic waxy binder
title_short Formulation and evaluation of carvedilol melt-in-mouth tablet using mucoadhesive polymer and PEG-6-stearate as hydrophilic waxy binder
title_sort formulation and evaluation of carvedilol melt-in-mouth tablet using mucoadhesive polymer and peg-6-stearate as hydrophilic waxy binder
topic Original Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3618634/
https://www.ncbi.nlm.nih.gov/pubmed/23580934
http://dx.doi.org/10.4103/2230-973X.106989
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