中国药物警戒 ›› 2014, Vol. 11 ›› Issue (7): 394-397.

• 质量与工艺研究 • 上一篇    下一篇

全因子实验筛选盐酸二甲双胍缓释片处方及其释药机制研究

陈叶明, 周志亮2, 张学农1*, 李先俊2   

  1. 1苏州大学,江苏 苏州215123;
    2润泽制药有限公司,江苏 苏州 215126
  • 收稿日期:2016-02-03 修回日期:2016-02-03 出版日期:2014-07-08 发布日期:2016-03-02
  • 通讯作者: 张学农,男,教授·博导,药物新技术与新剂型研究。 E-mail：zhangxuenong@163.com
  • 作者简介:陈叶明,男,硕士,制药工程。

Full-factorial Design for Optimizing Formulation of Metformin Hydrochloride Extended-release Tablets and Investigation of Release Mechanism in Vitro

CHEN Ye-ming1, ZHOU Zhi-liang2, ZHANG Xue-nong1, *, LI Xian-jun2   

  1. 1Soochow University, Jiangsu Suzhou 215123,China;
    2Runze Pharmaceutical Co.Ltd, Jiangsu Suzhou 215126, China
  • Received:2016-02-03 Revised:2016-02-03 Online:2014-07-08 Published:2016-03-02

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摘要： 目的优化盐酸二甲双胍缓释片的处方并对释药机制进行研究。方法采用高速湿法制粒制备颗粒,然后压片,硬度控制在80~100N。以相似因子f2为主要评价指标,辅以10小时的累计释放百分率Q10为评价指标,用Design Expert软件进行全因子试验设计及分析,筛选最优处方。获取的最优处方进行释放度试验,进行释放机制研究。结果最佳处方是盐酸二甲双胍100 g,壳聚糖2.5 g,HPMC（K100M）47.5 g,硬脂酸镁1.5 g,相似因子f2与预测值偏差小于4%。该样品释放数据经拟合,符合一级释放模型,释药机制为Fick's扩散。结论用Design Expert软件进行全因子试验设计及分析,能够有效优化盐酸二甲双胍缓释片处方,其药物释放机制为Fick's扩散。

关键词: 盐酸二甲双胍, 缓释片, 全因子实验, Design Expert软件

Abstract: ObjectiveTo obtain an optimized formulation of metformin hydrochloride extended-release tablets, and investigate the release mechanism of the optimized formulation. MethodsMetformin hydrochloride extended-release tablets were prepared by high shear wet granulation route. The formulation was optimized using full-factorial design by Design Expert software. Responses were measured in this study, including the f2 factor of drug release profiles in vitro and the cumulative release percentages of 10 hours(Q10). The release mechanism of optimized formulation was investigated. ResultsOptimal prescription contained metformin hydrochloride 100 g, chitosan 2.5 g, HPMC(K100 M)47.5 g, magnesium stearate 1.5 g. The predicted value of deviation was less than 4%. The drug release followed the first-order kinetics, via mechanism of Fickian diffusion. ConclusionFull-factorial design by Design Expert software is an effective and feasible method for screening metformin hydrochloride extended-release tablets formulation. The drug release follows the mechanism of Fickian diffusion.

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