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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...

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Autores principales: da Costa, Maíra Assis, Seiceira, Rafael Cardoso, Rodrigues, Carlos Rangel, Hoffmeister, Cristiane Rodrigues Drago, Cabral, Lucio Mendes, Rocha, Helvécio Vinícius Antunes
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2012
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.
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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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