Efavirenz Dissolution Enhancement I Co-Micronization.docVIP

Pharmaceutics 2013, 5, 1-22; doi:10.3390/pharmaceutics5010001 OPEN ACCESS pharmaceutics ISSN 1999-4923 /journal/pharmaceutics Article Efavirenz Dissolution Enhancement I: Co-Micronization Maíra Assis da Costa , Rafael Cardoso Seiceira , Carlos Rangel Rodrigues 1, 1,2 3 2 1 Cristiane Rodrigues Drago Hoffmeister , Lucio Mendes Cabral and Helvécio Vinícius Antunes Rocha 1,2, * 1 Laboratory of Industrial Pharmaceutical Technology (LabTIF), Faculty of Pharmacy, Federal University of Rio de Janeiro, Rio de Janeiro, Brazil; E-Mails: mairacosta@far.fiocruz.br (M.A.C.); rangel@pharma.ufrj.br (C.R.R.); lmcabral@pharma.ufrj.br (L.M.C.) 2 Laboratory of Advanced Pharmaceutical Systems (LaSiFA), Farmanguinhos, FIOCRUZ, Rio de Janeiro, Brazil; E-Mail: cristianedrago@ 3 Laboratory of Solid State Studies (LEES), Farmanguinhos, FIOCRUZ, Rio de Janeiro, Brazil; E-Mail: rcseiceira@far.fiocruz.br * Author to whom correspondence should be addressed; E-Mail: helveciorocha@far.fiocruz.br; Tel.: +55-213-348-5319; Fax: +55-213-348-5050. Received: 23 August 2012; in revised form: 8 November 2012 / Accepted: 3 December 2012 / Published: 20 December 2012 Abstract: 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 d