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Drug Dev Ind Pharm ; 35(1): 73-82, 2009 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-18821153

RESUMO

Commercial tablets of glyburide exhibit unsatisfactory dissolution profiles and, consequently, problems of bioinequivalence and poor bioavailability. The aim of this work was to develop glyburide fast-dissolving tablets by exploiting the solubilizing effect of different cyclodextrins (CDs), alone or in combination with hydrophilic polymers. Drug-CD and drug-CD-polymer systems, prepared by different techniques, were characterized by differential scanning calorimetry (DSC), X-ray diffractometry, and Fourier transform infra-red (FT-IR) spectroscopy. Tablets containing binary and ternary systems were prepared by direct compression and evaluated for technological properties and dissolution behavior in comparison with a reference formulation containing the plain drug. A significant improvement of the drug dissolution profile was achieved from tablets containing drug-CD systems (coevaporated products doubled drug dissolution efficiency [DE]), but 100% drug dissolution was never reached. Better results were obtained with ternary systems. In particular, polyvinylpyrrolidone (PVP) emerged as the most effective polymer, and tablets with drug-PVP-hydroxypropyl-betaCD coevaporated products showed the best dissolution profiles, reaching 100% dissolved drug within only 15 min.


Assuntos
Ciclodextrinas/química , Glibureto/farmacocinética , Hipoglicemiantes/farmacocinética , Polímeros/química , Disponibilidade Biológica , Varredura Diferencial de Calorimetria , Química Farmacêutica , Glibureto/química , Hipoglicemiantes/química , Povidona/química , Solubilidade , Espectroscopia de Infravermelho com Transformada de Fourier , Comprimidos , Tecnologia Farmacêutica , Equivalência Terapêutica , Difração de Raios X
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