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Arch Pharm Res ; 33(7): 1009-17, 2010 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-20661710

RESUMO

Itraconazole (ITZ) solid complex using hydroxypropyl-beta-cyclodextrin (ITZ-HP-beta-CD) with 20% polyvinylpyrrolidone was prepared by a co-evaporation method. The complex improved antifungal activity against C. parapasilosis and C. albicans. The complex demonstrated good flow and compressibility characteristics. The complex was formulated as a capsule dosage form and drug release was evaluated. Capsules containing ITZ-HP-beta-CD at a molar ratio of 1:3 with 20% polyvinylpyrrolidone have a faster dissolution rate than commercial capsules (Sporanox). About 88% of ITZ was released in less than 30 min and the initial dissolution rate exhibited a 3.5-fold increase compared to the commercial product. UV spectrophotometeric, HPLC, and antimicrobial methods were used to determine ITZ concentration in the release medium and the results obtained by these methods are reported. It was found that HPLC analysis is a suitable and reliable method for determination of the drug concentration with a coefficient of variation less than 10%. The intraday precision showed a coefficient of variation less than 3.96%, and that for interday was less than 4.99%. The HPLC method was more accurate and precise than the antimicrobial and UV-spectrophotometric methods for determination of ITZ concentration present in the release medium.


Assuntos
Antifúngicos/farmacologia , Química Farmacêutica/métodos , Ciclodextrinas/síntese química , Ciclodextrinas/farmacologia , Itraconazol/síntese química , Itraconazol/farmacologia , Anti-Infecciosos/síntese química , Anti-Infecciosos/farmacologia , Antifúngicos/síntese química , Candida albicans/efeitos dos fármacos , Candida albicans/fisiologia , Cápsulas , Formas de Dosagem , Testes de Sensibilidade Microbiana/métodos
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