title: Influence of the efavirenz micronization on tableting and dissolution.
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.
authors.affiliation: Laboratory of Antibiotics, Biochemistry, Institute of Biology, Universidade Federal Fluminense, Campus of Valonguinho, Niterói, RJ, CEP: 24.210-130, Brazil. facarmo@pharma.ufrj.br.
authors.forename: Eduardo Costa
authors.initials: EC
authors.lastname: Pinto
authors.forename: Flávia Almada do
authors.initials: FA
authors.lastname: Carmo
authors.forename: Thiago da Silva
authors.initials: Tda S
authors.lastname: Honório
authors.forename: Rita de Cássia da Silva Ascenção
authors.initials: Rde C
authors.lastname: Barros
authors.forename: Helena Carla Rangel
authors.initials: HC
authors.lastname: Castro
authors.forename: Carlos Rangel
authors.initials: CR
authors.lastname: Rodrigues
authors.forename: Valéria Sant'anna Dantas
authors.initials: VS
authors.lastname: Esteves
authors.forename: Helvécio Vinícius Antunes
authors.initials: HV
authors.lastname: Rocha
authors.forename: Valeria Pereira de
authors.initials: VP
authors.lastname: Sousa
authors.forename: Lucio Mendes
authors.initials: LM
authors.lastname: Cabral