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复方二甲双胍/格列吡嗪双层缓释片: 设计与体外释放

欧阳德方, 聂淑芳, 孟晋, 杨星钢, 宋志全, 潘卫三*   

  1. 沈阳药科大学药剂教研室122号信箱, 辽宁 沈阳 110016
  • 收稿日期:2005-02-04 修回日期:2005-08-10 出版日期:2005-09-15 发布日期:2005-09-15
  • 通讯作者: 潘卫三*

Compound Metformin/Glipizide Bilayer Extended Release Tablets: Development and in Vitro Release

OUYANG De-fang, NIE Shu-fang, MENG Jin, YANG Xing-gang, SONG Zhi-quan, PAN Wei-san*   

  1. Department of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China
  • Received:2005-02-04 Revised:2005-08-10 Online:2005-09-15 Published:2005-09-15
  • Contact: PAN Wei-san*

摘要: 目的 本文为了解决2型糖尿病中的多药治疗问题, HPMC进行湿法制粒制备了复方二甲双胍格列吡嗪双层缓释片。方法 由于二甲双胍的压缩成型性较差, 高剂量的二甲双胍很难压制成片。在实验中, 采用十八醇克服了这一问题。研究了HPMC的黏度、用量和填充剂的用量对药物释放的影响。优化的处方具有较好的物理化学性质, 其中二甲双胍和格列吡嗪缓释时间为10小时。结果 二甲双胍的体外释放符合Higuchi方程, 而格列吡嗪的体外释放符合零级方程。结论 本文成功地设计了一种新型的复方二甲双胍格列吡嗪双层缓释片。

关键词: 二甲双胍, 二甲双胍, 二甲双胍, 格列吡嗪, 格列吡嗪, 格列吡嗪, 缓释, 缓释, 缓释, 双层片, 双层片, 双层片, 十八醇, 十八醇, 十八醇

Abstract: Aim In this study, compound metformin/glipizide bilayer extended release tablets were formulated with hydroxypropyl methylcellulose (HPMC) by wet granulation technique in order to tackle the problems associated with the multidrug therapy of non-insulin dependent diabetes mellitus. Methods High-dose metformin is difficult to formulate into a tablet dosage form due to its poor compressibility and compactibility. In this study, the way to overcome the difficulty was to utilize stearic alcohol to prepare the tablet formulation. The influences of viscosity, amount of HPMC, and weight of fillers were investigated. The optimal formulation had acceptable physicochemical properties and released metformin and glipizide over 10 h. Results The data of metformin obtained from in vitro release fitted Higuchi kinetics best, while the release of glipizide in vitro was found to follow zero kinetics. Conclusion Compound metformin/glipizide bilayer extended release tablets have been successfully developed.

Key words: metformin, metformin, glipizide, glipizide, extended release, extended release, bilayer tablet, bilayer tablet, stearic alcohol, stearic alcohol

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Supporting: *Corresponding author. Tel.: 86-24-23986313; fax: 86-24-23953241