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Eur J Pharm Biopharm ; 65(1): 85-93, 2007 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-16971097

RESUMEN

The purpose of this work was to develop hollow calcium pectinate beads for floating-pulsatile release of diclofenac sodium intended for chronopharmacotherapy. Floating pulsatile concept was applied to increase the gastric residence of the dosage form having lag phase followed by a burst release. To overcome limitations of various approaches for imparting buoyancy, hollow/porous beads were prepared by simple process of acid-base reaction during ionotropic crosslinking. The floating beads obtained were porous (34% porosity), hollow with bulk density<1 and had Ft50% of 14-24 h. In vivo studies by gamma scintigraphy determined on rabbits showed gastroretention of beads up to 5 h. The floating beads provided expected two-phase release pattern with initial lag time during floating in acidic medium followed by rapid pulse release in phosphate buffer. This approach suggested the use of hollow calcium pectinate microparticles as promising floating-pulsatile drug delivery system for site- and time-specific release of drugs acting as per chronotherapy of diseases.


Asunto(s)
Calcio/química , Cronoterapia , Portadores de Fármacos , Microesferas , Pectinas/química , Tecnología Farmacéutica , Animales , Antiinflamatorios no Esteroideos/química , Antiinflamatorios no Esteroideos/farmacocinética , Química Farmacéutica , Cronoterapia/métodos , Fuerza Compresiva , Preparaciones de Acción Retardada , Diclofenaco/química , Diclofenaco/farmacocinética , Tracto Gastrointestinal/diagnóstico por imagen , Tránsito Gastrointestinal , Masculino , Microscopía Electrónica de Rastreo , Tamaño de la Partícula , Porosidad , Conejos , Cintigrafía , Solubilidad , Espectroscopía Infrarroja por Transformada de Fourier , Propiedades de Superficie , Tecnología Farmacéutica/métodos , Factores de Tiempo
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