甲硝唑结肠定位缓释片的工艺研究

目的：研制甲硝唑结肠定位缓释片。方法：通过羟丙甲基纤维素（HPMC）骨架缓释材料制备甲硝唑缓释片芯，再采用S100包肠溶衣，制备甲硝唑结肠定位缓释片，并进行体外释放度和药动学研究。结果：所制得的片剂体外释放度符合结肠释放并缓释的特征，犬的药动学研究以及大鼠的消化道药物分布研究表明，药物口服后主要在结肠中释放，胃和小肠中几乎无药物释放。结论：采用本工艺制备的甲硝唑结肠定位缓释片可达到结肠定位和缓释的效果。

Optimal process of metronidazole colon-targeted sustained-release tablets

Objective:To prepare metronidazole colon-targeted sustained-release tablets.Meth- ods:Metronidazole sustained-released tablets were prepared by mixing with HPMC as matrix materials followed by coating with S_(100).The release behavior in vitro and pharmacokinetic parameters were evalu- ated in animal tests.Results:The sustained-release tablets produced a relatively flat,sustained drug concentration in colon.The pharmacokiuetic research in dogs and drug distribution test at alimentary tract of rats further confirmed the sustained release of metronidazole at colon tissues other than stomach and intestine tissues.Conclusion:The metronidazole colon-targeted sustained-release tablets were a- chieved.