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Formulation and Pharmacokinetic Evaluation of Microcapsules Containing Pravastatin Sodium Using Rats

Pravastatin Sodium has a cholesterol lowering agent. It has shorter half-life and undergoes first-pass metabolism. Frequent dose is required in case of conventional dosage form. The purpose of the study is to formulate and evaluate microcapsules containing Pravastatin Sodium by complex with cholesty...

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Autores principales: Puttegowda, Venkatesh Dinnekere, Karki, Roopa, Goli, Divakar, Jha, Sajal kumar, Mudagal, Manjunatha Panduranga
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Hindawi Publishing Corporation 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4993944/
https://www.ncbi.nlm.nih.gov/pubmed/27595040
http://dx.doi.org/10.1155/2016/7623193
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author Puttegowda, Venkatesh Dinnekere
Karki, Roopa
Goli, Divakar
Jha, Sajal kumar
Mudagal, Manjunatha Panduranga
author_facet Puttegowda, Venkatesh Dinnekere
Karki, Roopa
Goli, Divakar
Jha, Sajal kumar
Mudagal, Manjunatha Panduranga
author_sort Puttegowda, Venkatesh Dinnekere
collection PubMed
description Pravastatin Sodium has a cholesterol lowering agent. It has shorter half-life and undergoes first-pass metabolism. Frequent dose is required in case of conventional dosage form. The purpose of the study is to formulate and evaluate microcapsules containing Pravastatin Sodium by complex with cholestyramine resins coated with Eudragit RLPO and Eudragit RSPO polymers for achieving control release. Complexation of drug on resin was carried out by batch method. Microencapsulation was carried out by nonaqueous solvent evaporation method. Pharmacokinetic studies were done by using rats. The intermediate stability studies were carried out on the most satisfactory formulations. FTIR, X-ray diffraction, and DSC spectra of drug, drug-resinates, and polymers revealed no chemical interaction. The % DEE and % yield were observed for formulations of f1 to f7 that were varied from 97.1 ± 0.8 to 98.9 ± 0.5% and 95.0 ± 3.25 to 98.8 ± 7.1%, respectively. Most satisfactory formulation, f6, showed drug release up to 72.6%. No changes in % DEE and % CDR were observed after stability studies. Microcapsules of f6 formulation achieved best performance regarding in vitro drug release and from pharmacokinetic evaluation mean residence time was found to be 6.3 h, thus indicated, Pravastatin Sodium microcapsules were released and absorbed slowly over a prolonged period of time.
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spelling pubmed-49939442016-09-04 Formulation and Pharmacokinetic Evaluation of Microcapsules Containing Pravastatin Sodium Using Rats Puttegowda, Venkatesh Dinnekere Karki, Roopa Goli, Divakar Jha, Sajal kumar Mudagal, Manjunatha Panduranga Scientifica (Cairo) Research Article Pravastatin Sodium has a cholesterol lowering agent. It has shorter half-life and undergoes first-pass metabolism. Frequent dose is required in case of conventional dosage form. The purpose of the study is to formulate and evaluate microcapsules containing Pravastatin Sodium by complex with cholestyramine resins coated with Eudragit RLPO and Eudragit RSPO polymers for achieving control release. Complexation of drug on resin was carried out by batch method. Microencapsulation was carried out by nonaqueous solvent evaporation method. Pharmacokinetic studies were done by using rats. The intermediate stability studies were carried out on the most satisfactory formulations. FTIR, X-ray diffraction, and DSC spectra of drug, drug-resinates, and polymers revealed no chemical interaction. The % DEE and % yield were observed for formulations of f1 to f7 that were varied from 97.1 ± 0.8 to 98.9 ± 0.5% and 95.0 ± 3.25 to 98.8 ± 7.1%, respectively. Most satisfactory formulation, f6, showed drug release up to 72.6%. No changes in % DEE and % CDR were observed after stability studies. Microcapsules of f6 formulation achieved best performance regarding in vitro drug release and from pharmacokinetic evaluation mean residence time was found to be 6.3 h, thus indicated, Pravastatin Sodium microcapsules were released and absorbed slowly over a prolonged period of time. Hindawi Publishing Corporation 2016 2016-08-09 /pmc/articles/PMC4993944/ /pubmed/27595040 http://dx.doi.org/10.1155/2016/7623193 Text en Copyright © 2016 Venkatesh Dinnekere Puttegowda et al. https://creativecommons.org/licenses/by/4.0/ This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Research Article
Puttegowda, Venkatesh Dinnekere
Karki, Roopa
Goli, Divakar
Jha, Sajal kumar
Mudagal, Manjunatha Panduranga
Formulation and Pharmacokinetic Evaluation of Microcapsules Containing Pravastatin Sodium Using Rats
title Formulation and Pharmacokinetic Evaluation of Microcapsules Containing Pravastatin Sodium Using Rats
title_full Formulation and Pharmacokinetic Evaluation of Microcapsules Containing Pravastatin Sodium Using Rats
title_fullStr Formulation and Pharmacokinetic Evaluation of Microcapsules Containing Pravastatin Sodium Using Rats
title_full_unstemmed Formulation and Pharmacokinetic Evaluation of Microcapsules Containing Pravastatin Sodium Using Rats
title_short Formulation and Pharmacokinetic Evaluation of Microcapsules Containing Pravastatin Sodium Using Rats
title_sort formulation and pharmacokinetic evaluation of microcapsules containing pravastatin sodium using rats
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4993944/
https://www.ncbi.nlm.nih.gov/pubmed/27595040
http://dx.doi.org/10.1155/2016/7623193
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