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

机译:头孢呋辛酯胃阻滞性递送系统的开发和体内评估

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摘要

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.
机译:这项研究的目的是使用浮动级片剂方法和各种等级的羟丙基甲基纤维素设计和开发头孢呋辛酯的胃滞留剂型。已知头孢呋辛酯的生物利用度低,半衰期短,并且主要从上消化道吸收。剂型中使用碳酸氢钠作为二氧化碳的来源,以保持浮力。体外溶出研究结果表明,非菲克扩散控制的药物释放机制,最适合Korsmeyer-Peppas方程。在五名健康人类志愿者中进行的体内放射学研究表明,该制剂具有最佳配方,可将药片保留在胃区域超过6小时。可重现的物理参数表明,当前的配方很容易扩大规模。

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