Development and in vivo evaluation of gastroretentive delivery systems for cefuroxime axetil

头孢呋辛酯胃滞留给药系统的研制及体内评价

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Abstract

The purpose of this investigation was to design and develop gastroretentive dosage form for cefuroxime axetil using floating tablet approach with various grades of hydroxypropyl methyl cellulose. Cefuroxime axetil is known to have low bioavailability, short half-life and is absorbed largely from upper GIT. Sodium bicarbonate was used in the dosage form as a source of carbon-di-oxide to maintain buoyancy. In vitro dissolution study results indicated non-Fickian diffusion controlled drug release mechanism and was best fitted into Korsmeyer-Peppas equation. In vivo radiographic studies conducted in five healthy human volunteers for optimized formulation indicated over 6 h retention of tablet in the stomach region. Reproducible physical parameters indicated that the current formulation could be easily scaled-up.

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