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Design, development and evaluation of clopidogrel bisulfate floating tablets

OBJECTIVE: The objective of the present work was to formulate and to characterize a floating drug delivery system for clopidogrel bisulphate to improve bioavailability and to minimize the side effects of the drug such as gastric bleeding and drug resistance development. MATERIALS AND METHODS: Clopid...

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Autores principales: Rao, K. Rama Koteswara, Lakshmi, K. Rajya
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/PMC3944613/
https://www.ncbi.nlm.nih.gov/pubmed/24678458
http://dx.doi.org/10.4103/2230-973X.127736
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author Rao, K. Rama Koteswara
Lakshmi, K. Rajya
author_facet Rao, K. Rama Koteswara
Lakshmi, K. Rajya
author_sort Rao, K. Rama Koteswara
collection PubMed
description OBJECTIVE: The objective of the present work was to formulate and to characterize a floating drug delivery system for clopidogrel bisulphate to improve bioavailability and to minimize the side effects of the drug such as gastric bleeding and drug resistance development. MATERIALS AND METHODS: Clopidogrel floating tablets were prepared by direct compression technique by the use of three polymers xanthan gum, hydroxypropyl methylcellulose (HPMC) K15M and HPMC K4M in different concentrations (20%, 25% and 30% w/w). Sodium bicarbonate (15% w/w) and microcrystalline cellulose (30% w/w) were used as gas generating agent and diluent respectively. Studies were carried out on floating behavior and influence of type of polymer on drug release rate. All the formulations were subjected to various quality control and in-vitro dissolution studies in 0.1 N hydrochloric acid (1.2 pH) and corresponding dissolution data were fitted to popular release kinetic equations in order to evaluate release mechanisms and kinetics. RESULTS AND DISCUSSION: All the clopidogrel floating formulations followed first order kinetics, Higuchi drug release kinetics with diffusion as the dominant mechanism of drug release. As per Korsmeyer-Peppas equation, the release exponent “n” ranged 0.452-0.654 indicating that drug release from all the formulations was by non-Fickian diffusion mechanism. The drug release rate of clopidogrel was found to be affected by the type and concentration of the polymer used in the formulation (P < 0.05). As the concentration of the polymer was increased, the drug release was found to be retarded. CONCLUSION: Based on the results, clopidogrel floating tablets prepared by employing xanthan gum at concentration 25% w/w (formulation F2) was the best formulation with desired in-vitro floating time and drug dissolution.
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spelling pubmed-39446132014-03-27 Design, development and evaluation of clopidogrel bisulfate floating tablets Rao, K. Rama Koteswara Lakshmi, K. Rajya Int J Pharm Investig Original Research Article OBJECTIVE: The objective of the present work was to formulate and to characterize a floating drug delivery system for clopidogrel bisulphate to improve bioavailability and to minimize the side effects of the drug such as gastric bleeding and drug resistance development. MATERIALS AND METHODS: Clopidogrel floating tablets were prepared by direct compression technique by the use of three polymers xanthan gum, hydroxypropyl methylcellulose (HPMC) K15M and HPMC K4M in different concentrations (20%, 25% and 30% w/w). Sodium bicarbonate (15% w/w) and microcrystalline cellulose (30% w/w) were used as gas generating agent and diluent respectively. Studies were carried out on floating behavior and influence of type of polymer on drug release rate. All the formulations were subjected to various quality control and in-vitro dissolution studies in 0.1 N hydrochloric acid (1.2 pH) and corresponding dissolution data were fitted to popular release kinetic equations in order to evaluate release mechanisms and kinetics. RESULTS AND DISCUSSION: All the clopidogrel floating formulations followed first order kinetics, Higuchi drug release kinetics with diffusion as the dominant mechanism of drug release. As per Korsmeyer-Peppas equation, the release exponent “n” ranged 0.452-0.654 indicating that drug release from all the formulations was by non-Fickian diffusion mechanism. The drug release rate of clopidogrel was found to be affected by the type and concentration of the polymer used in the formulation (P < 0.05). As the concentration of the polymer was increased, the drug release was found to be retarded. CONCLUSION: Based on the results, clopidogrel floating tablets prepared by employing xanthan gum at concentration 25% w/w (formulation F2) was the best formulation with desired in-vitro floating time and drug dissolution. Medknow Publications & Media Pvt Ltd 2014 /pmc/articles/PMC3944613/ /pubmed/24678458 http://dx.doi.org/10.4103/2230-973X.127736 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
Rao, K. Rama Koteswara
Lakshmi, K. Rajya
Design, development and evaluation of clopidogrel bisulfate floating tablets
title Design, development and evaluation of clopidogrel bisulfate floating tablets
title_full Design, development and evaluation of clopidogrel bisulfate floating tablets
title_fullStr Design, development and evaluation of clopidogrel bisulfate floating tablets
title_full_unstemmed Design, development and evaluation of clopidogrel bisulfate floating tablets
title_short Design, development and evaluation of clopidogrel bisulfate floating tablets
title_sort design, development and evaluation of clopidogrel bisulfate floating tablets
topic Original Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3944613/
https://www.ncbi.nlm.nih.gov/pubmed/24678458
http://dx.doi.org/10.4103/2230-973X.127736
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