开发和体内评价头孢呋辛酯的胃滞留给药系统。
Development and in vivo evaluation of gastroretentive delivery systems for cefuroxime axetil.
机构信息
Pharmacy Department, Pragati Pharmacy College, Janagaon, Warangal (Dist.), Andhra Pradesh, India.
出版信息
Saudi Pharm J. 2013 Jan;21(1):53-9. doi: 10.1016/j.jsps.2012.01.003. Epub 2012 Jan 14.
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.
摘要
本研究旨在通过使用不同等级的羟丙甲纤维素设计和开发头孢呋辛酯的胃滞留剂型的漂浮片。头孢呋辛酯的生物利用度低，半衰期短，主要在上消化道被吸收。碳酸氢钠被用作该剂型中的二氧化碳源以维持漂浮性。体外溶出研究结果表明，药物释放机制是非菲克扩散控制，并最好拟合到 Korsmeyer-Peppas 方程中。在五名健康志愿者中进行的优化配方体内放射影像学研究表明，片剂在胃区域的滞留时间超过 6 小时。可重现的物理参数表明，当前的配方可以很容易地放大。
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