Studies on the characterization and polymorphic stability of Fosamprenavir



Título del documento: Studies on the characterization and polymorphic stability of Fosamprenavir
Revista: Anais da Academia Brasileira de Ciencias
Base de datos: PERIÓDICA
Número de sistema: 000436193
ISSN: 0001-3765
Autores: 1
1
1
Instituciones: 1Universidade Federal de Alfenas, Instituto de Quimica, Alfenas, Minas Gerais. Brasil
Año:
Volumen: 92
Número: 1
País: Brasil
Idioma: Inglés
Tipo de documento: Artículo
Enfoque: Experimental, aplicado
Resumen en inglés Fosamprenavir calcium is an amprenavir prodrug of the protease inhibitors class used in the treatment of patients with acquired immunodeficiency syndrome (AIDS). Different solid forms of this drug are described in patents, in this sense studies on the physico-chemical characterization and stability are relevant for the selection of a solid form with adequate features for pharmaceutical purposes. In the present work form I (commercial) and amorphous of fosamprenavir calcium were characterized by the techniques of Differential Scanning Calorimetry (DSC), Thermogravimetry (TGA), Powder X-ray Diffraction (PXRD), Fourier-Transform Infrared Spectroscopy (FTIR) and Scanning Electron Microscopy (SEM). Furthermore, the chemical and polymorphic stability of the commercial form were evaluated by DSC, PXRD, FTIR and High-Performance Liquid Chromatography (HPLC). In the studies of characterization, thermal analyses allied to spectroscopic methods (PXRD and FTIR) demonstrated that the presence of water in the crystalline structure of Form I is fundamental for maintaining its crystallinity. In studies of accelerated stability the techniques of DSC, PXRD and FTIR showed that Form I does not suffer phase change when submitted to controlled conditions of temperature and humidity. Moreover, HPLC and FTIR proved the chemical stability of this solid form of fosamprenavir, thus demonstrating its suitability for pharmaceutical purposes
Disciplinas: Medicina
Palabras clave: Farmacología,
Inmunología,
SIDA,
Inhibidores enzimáticos,
Proteasas,
Estabilidad química,
Polimorfismo,
Fosamprenavir
Keyword: Pharmacology,
Immunology,
AIDS,
Enzymatic inhibitors,
Proteases,
Chemical stability,
Polymorphism,
Fosamprenavir
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