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...
| Main Authors: | , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2012-12-01
|
| Series: | Pharmaceutics |
| Subjects: | |
| Online Access: | http://www.mdpi.com/1999-4923/5/1/1 |
| _version_ | 1811185197233733632 |
|---|---|
| author | Helvécio Vinícius Antunes Rocha Cristiane Rodrigues Drago Hoffmeister Rafael Cardoso Seiceira Carlos Rangel Rodrigues Maíra Assis da Costa Lucio Mendes Cabral |
| author_facet | Helvécio Vinícius Antunes Rocha Cristiane Rodrigues Drago Hoffmeister Rafael Cardoso Seiceira Carlos Rangel Rodrigues Maíra Assis da Costa Lucio Mendes Cabral |
| author_sort | Helvécio Vinícius Antunes Rocha |
| collection | DOAJ |
| 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. |
| first_indexed | 2024-04-11T13:25:21Z |
| format | Article |
| id | doaj.art-179898888800424490e379861c47df68 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-04-11T13:25:21Z |
| publishDate | 2012-12-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-179898888800424490e379861c47df682022-12-22T04:22:05ZengMDPI AGPharmaceutics1999-49232012-12-015112210.3390/pharmaceutics5010001Efavirenz Dissolution Enhancement I: Co-MicronizationHelvécio Vinícius Antunes RochaCristiane Rodrigues Drago HoffmeisterRafael Cardoso SeiceiraCarlos Rangel RodriguesMaíra Assis da CostaLucio Mendes CabralAIDS 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.http://www.mdpi.com/1999-4923/5/1/1efavirenzdissolutionmicronizationpoorly soluble drugssodium lauryl sulfatepolyvinylpyrrolidone |
| spellingShingle | Helvécio Vinícius Antunes Rocha Cristiane Rodrigues Drago Hoffmeister Rafael Cardoso Seiceira Carlos Rangel Rodrigues Maíra Assis da Costa Lucio Mendes Cabral Efavirenz Dissolution Enhancement I: Co-Micronization Pharmaceutics efavirenz dissolution micronization poorly soluble drugs sodium lauryl sulfate polyvinylpyrrolidone |
| 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 | efavirenz dissolution micronization poorly soluble drugs sodium lauryl sulfate polyvinylpyrrolidone |
| url | http://www.mdpi.com/1999-4923/5/1/1 |
| work_keys_str_mv | AT helvecioviniciusantunesrocha efavirenzdissolutionenhancementicomicronization AT cristianerodriguesdragohoffmeister efavirenzdissolutionenhancementicomicronization AT rafaelcardososeiceira efavirenzdissolutionenhancementicomicronization AT carlosrangelrodrigues efavirenzdissolutionenhancementicomicronization AT mairaassisdacosta efavirenzdissolutionenhancementicomicronization AT luciomendescabral efavirenzdissolutionenhancementicomicronization |