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Formulation Development and Dissolution Rate Enhancement of Efavirenz by Solid Dispersion Systems
The aim of this study was to enhance the dissolution rate of efavirenz using solid dispersion systems (binary and ternary). A comparison between solvent and fusion method was also investigated. Solid dispersions of efavirenz were prepared using polyethylene glycol 8000, polyvinylpyrrolidone K30 alon...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Medknow Publications & Media Pvt Ltd
2013
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3783747/ https://www.ncbi.nlm.nih.gov/pubmed/24082345 http://dx.doi.org/10.4103/0250-474X.117434 |
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author | Koh, P. T. Chuah, J. N. Talekar, Meghna Gorajana, A. Garg, S. |
author_facet | Koh, P. T. Chuah, J. N. Talekar, Meghna Gorajana, A. Garg, S. |
author_sort | Koh, P. T. |
collection | PubMed |
description | The aim of this study was to enhance the dissolution rate of efavirenz using solid dispersion systems (binary and ternary). A comparison between solvent and fusion method was also investigated. Solid dispersions of efavirenz were prepared using polyethylene glycol 8000, polyvinylpyrrolidone K30 alone and combination of both. Tween 80 was incorporated to obtain a ternary solid dispersion system. Dissolution tests were conducted and evaluated on the basis of cumulative percentage drug release and dissolution efficiency. Physicochemical characterizations of the solid dispersions were carried out using differential scanning calorimetric, powder X-ray diffraction, Fourier transform infrared spectroscopy, and scanning electron microscopy. Dissolution was remarkably improved in both systems compared to pure efavirenz (P<0.05). An optimum ratio was identified at a drug:polymer of 1:10. Incorporation of Tween 80 to 1:10 formulations formed using solvent method showed further improvement in the dissolution rate. Physicochemical characterization results suggested that efavirenz existed in the amorphous form in all the solid dispersion systems providing evidence of improvement in dissolution. No statistically significant difference (P>0.05) in dissolution was observed between the two methods. Binary and ternary solid dispersion systems both have showed a significant improvement in the dissolution rate of efavirenz. Formulations with only polyvinylpyrrolidone K30 showed best dissolution profile and 1:10 was identified as an optimum drug-polymer weight ratio. |
format | Online Article Text |
id | pubmed-3783747 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2013 |
publisher | Medknow Publications & Media Pvt Ltd |
record_format | MEDLINE/PubMed |
spelling | pubmed-37837472013-09-30 Formulation Development and Dissolution Rate Enhancement of Efavirenz by Solid Dispersion Systems Koh, P. T. Chuah, J. N. Talekar, Meghna Gorajana, A. Garg, S. Indian J Pharm Sci Research Paper The aim of this study was to enhance the dissolution rate of efavirenz using solid dispersion systems (binary and ternary). A comparison between solvent and fusion method was also investigated. Solid dispersions of efavirenz were prepared using polyethylene glycol 8000, polyvinylpyrrolidone K30 alone and combination of both. Tween 80 was incorporated to obtain a ternary solid dispersion system. Dissolution tests were conducted and evaluated on the basis of cumulative percentage drug release and dissolution efficiency. Physicochemical characterizations of the solid dispersions were carried out using differential scanning calorimetric, powder X-ray diffraction, Fourier transform infrared spectroscopy, and scanning electron microscopy. Dissolution was remarkably improved in both systems compared to pure efavirenz (P<0.05). An optimum ratio was identified at a drug:polymer of 1:10. Incorporation of Tween 80 to 1:10 formulations formed using solvent method showed further improvement in the dissolution rate. Physicochemical characterization results suggested that efavirenz existed in the amorphous form in all the solid dispersion systems providing evidence of improvement in dissolution. No statistically significant difference (P>0.05) in dissolution was observed between the two methods. Binary and ternary solid dispersion systems both have showed a significant improvement in the dissolution rate of efavirenz. Formulations with only polyvinylpyrrolidone K30 showed best dissolution profile and 1:10 was identified as an optimum drug-polymer weight ratio. Medknow Publications & Media Pvt Ltd 2013 /pmc/articles/PMC3783747/ /pubmed/24082345 http://dx.doi.org/10.4103/0250-474X.117434 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 | Research Paper Koh, P. T. Chuah, J. N. Talekar, Meghna Gorajana, A. Garg, S. Formulation Development and Dissolution Rate Enhancement of Efavirenz by Solid Dispersion Systems |
title | Formulation Development and Dissolution Rate Enhancement of Efavirenz by Solid Dispersion Systems |
title_full | Formulation Development and Dissolution Rate Enhancement of Efavirenz by Solid Dispersion Systems |
title_fullStr | Formulation Development and Dissolution Rate Enhancement of Efavirenz by Solid Dispersion Systems |
title_full_unstemmed | Formulation Development and Dissolution Rate Enhancement of Efavirenz by Solid Dispersion Systems |
title_short | Formulation Development and Dissolution Rate Enhancement of Efavirenz by Solid Dispersion Systems |
title_sort | formulation development and dissolution rate enhancement of efavirenz by solid dispersion systems |
topic | Research Paper |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3783747/ https://www.ncbi.nlm.nih.gov/pubmed/24082345 http://dx.doi.org/10.4103/0250-474X.117434 |
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