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Influence of the Efavirenz Micronization on Tableting and Dissolution
Laboratory of Antibiotics, Biochemistry, Institute of Biology, Universidade Federal Fluminense, Campus of Valonguinho, Niterói, RJ, CEP: 24.210-130, Brazil
Institute of Drug Technology, Fundação Oswaldo Cruz, Av. Comandante Guaranys, 447, Curicica, Rio de Janeiro, RJ, CEP: 22.775-903, Brazil
* Author to whom correspondence should be addressed.
Received: 8 August 2012; in revised form: 2 September 2012 / Accepted: 2 September 2012 / Published: 12 September 2012
Abstract: The purpose of this study was to propose an analytical procedure that provides the effects of particle size and surface area on dissolution of efavirenz. Five different batches obtained by different micronization processes and with different particle size distribution and surface area were studied. The preformulation studies and dissolution curves were used to confirm the particle size distribution effect on drug solubility. No polymorphic variety or amorphization was observed in the tested batches and the particle size distribution was determined as directly responsible for the improvement of drug dissolution. The influence of the preparation process on the tablets derived from efavirenz was observed in the final dissolution result in which agglomeration, usually seen in non-lipophilic micronized material, was avoided through the use of an appropriate wet granulation method. For these reasons, micronization may represent one viable alternative for the formulation of brick dust drugs.
Keywords: AIDS; size distribution; surface area; bioavailability; brick dust drug
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MDPI and ACS Style
Pinto, E.C.; Carmo, F.A.; Honório, T.S.; Barros, R.C.S.A.; Castro, H.C.R.; Rodrigues, C.R.; Esteves, V.S.D.; Rocha, H.V.A.; Sousa, V.P.; Cabral, L.M. Influence of the Efavirenz Micronization on Tableting and Dissolution. Pharmaceutics 2012, 4, 430-441.
Pinto EC, Carmo FA, Honório TS, Barros RCSA, Castro HCR, Rodrigues CR, Esteves VSD, Rocha HVA, Sousa VP, Cabral LM. Influence of the Efavirenz Micronization on Tableting and Dissolution. Pharmaceutics. 2012; 4(3):430-441.
Pinto, Eduardo Costa; Carmo, Flávia Almada do; Honório, Thiago da Silva; Barros, Rita de Cássia da Silva Ascenção; Castro, Helena Carla Rangel; Rodrigues, Carlos Rangel; Esteves, Valéria Sant'Anna Dantas; Rocha, Helvécio Vinícius Antunes; Sousa, Valeria Pereira de; Cabral, Lucio Mendes. 2012. "Influence of the Efavirenz Micronization on Tableting and Dissolution." Pharmaceutics 4, no. 3: 430-441.