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Efavirenz Dissolution Enhancement I: Co-Micronization
AIDS constitutes one of the most serious infectious diseases, representing a major public health priority. Efavirenz (EFV), one of the most widely used drugs for this pathology, belongs to the Class II of the Biopharmaceutics Classification System for drugs with very poor water solubility. To improv...
Autores principales: | , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2012
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3834943/ https://www.ncbi.nlm.nih.gov/pubmed/24300394 http://dx.doi.org/10.3390/pharmaceutics5010001 |
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author | da Costa, Maíra Assis Seiceira, Rafael Cardoso Rodrigues, Carlos Rangel Hoffmeister, Cristiane Rodrigues Drago Cabral, Lucio Mendes Rocha, Helvécio Vinícius Antunes |
author_facet | da Costa, Maíra Assis Seiceira, Rafael Cardoso Rodrigues, Carlos Rangel Hoffmeister, Cristiane Rodrigues Drago Cabral, Lucio Mendes Rocha, Helvécio Vinícius Antunes |
author_sort | da Costa, Maíra Assis |
collection | PubMed |
description | AIDS constitutes one of the most serious infectious diseases, representing a major public health priority. Efavirenz (EFV), one of the most widely used drugs for this pathology, belongs to the Class II of the Biopharmaceutics Classification System for drugs with very poor water solubility. To improve EFV’s dissolution profile, changes can be made to the physical properties of the drug that do not lead to any accompanying molecular modifications. Therefore, the study objective was to develop and characterize systems with efavirenz able to improve its dissolution, which were co-processed with sodium lauryl sulfate (SLS) and polyvinylpyrrolidone (PVP). The technique used was co-micronization. Three different drug:excipient ratios were tested for each of the two carriers. The drug dispersion dissolution results showed significant improvement for all the co-processed samples in comparison to non-processed material and corresponding physical mixtures. The dissolution profiles obtained for dispersion with co-micronized SLS samples proved superior to those of co-micronized PVP, with the proportion (1:0.25) proving the optimal mixture. The improvements may be explained by the hypothesis that formation of a hydrophilic layer on the surface of the micronized drug increases the wettability of the system formed, corroborated by characterization results indicating no loss of crystallinity and an absence of interaction at the molecular level. |
format | Online Article Text |
id | pubmed-3834943 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2012 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-38349432013-11-21 Efavirenz Dissolution Enhancement I: Co-Micronization da Costa, Maíra Assis Seiceira, Rafael Cardoso Rodrigues, Carlos Rangel Hoffmeister, Cristiane Rodrigues Drago Cabral, Lucio Mendes Rocha, Helvécio Vinícius Antunes Pharmaceutics Article AIDS constitutes one of the most serious infectious diseases, representing a major public health priority. Efavirenz (EFV), one of the most widely used drugs for this pathology, belongs to the Class II of the Biopharmaceutics Classification System for drugs with very poor water solubility. To improve EFV’s dissolution profile, changes can be made to the physical properties of the drug that do not lead to any accompanying molecular modifications. Therefore, the study objective was to develop and characterize systems with efavirenz able to improve its dissolution, which were co-processed with sodium lauryl sulfate (SLS) and polyvinylpyrrolidone (PVP). The technique used was co-micronization. Three different drug:excipient ratios were tested for each of the two carriers. The drug dispersion dissolution results showed significant improvement for all the co-processed samples in comparison to non-processed material and corresponding physical mixtures. The dissolution profiles obtained for dispersion with co-micronized SLS samples proved superior to those of co-micronized PVP, with the proportion (1:0.25) proving the optimal mixture. The improvements may be explained by the hypothesis that formation of a hydrophilic layer on the surface of the micronized drug increases the wettability of the system formed, corroborated by characterization results indicating no loss of crystallinity and an absence of interaction at the molecular level. MDPI 2012-12-20 /pmc/articles/PMC3834943/ /pubmed/24300394 http://dx.doi.org/10.3390/pharmaceutics5010001 Text en © 2013 by the authors; licensee MDPI, Basel, Switzerland. http://creativecommons.org/licenses/by/3.0/ This article is an open-access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/). |
spellingShingle | Article da Costa, Maíra Assis Seiceira, Rafael Cardoso Rodrigues, Carlos Rangel Hoffmeister, Cristiane Rodrigues Drago Cabral, Lucio Mendes Rocha, Helvécio Vinícius Antunes Efavirenz Dissolution Enhancement I: Co-Micronization |
title | Efavirenz Dissolution Enhancement I: Co-Micronization |
title_full | Efavirenz Dissolution Enhancement I: Co-Micronization |
title_fullStr | Efavirenz Dissolution Enhancement I: Co-Micronization |
title_full_unstemmed | Efavirenz Dissolution Enhancement I: Co-Micronization |
title_short | Efavirenz Dissolution Enhancement I: Co-Micronization |
title_sort | efavirenz dissolution enhancement i: co-micronization |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3834943/ https://www.ncbi.nlm.nih.gov/pubmed/24300394 http://dx.doi.org/10.3390/pharmaceutics5010001 |
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