硝苯地平缓释微丸片的制备与体外释放度考察  

Preparation of Nifedipine Sustained-Release Pellet Tablets and Study of Its Release Behavior in vitro

作　　者：张怡[1] 袁中文[2] 关世侠[1] 李庆国[1] 周祥萍[1] 

机构地区：[1]广州中医药大学中药学院,广州510006 [2]澳门科技大学中药质量研究国家重点实验室

出　　处：《医药导报》2014年第6期790-793,共4页Herald of Medicine

摘　　要：目的制备硝苯地平缓释微丸片及其体外释放度考察。方法首先筛选载体的种类和用量,确定以新型辅料Soluplus作为载体材料(硝苯地平∶Soluplus=1∶1),用热熔融挤出法制备硝苯地平固体分散体,采用差式扫描量热法对其进行验证;用挤出-滚圆法制备含药微丸,并以EudragitRS 30D为包衣材料制备缓释微丸,再将缓释微丸压制成片剂。结果体外释放度表明,所制备的硝苯地平缓释微丸片在24 h内释药平稳且完全,释药规律符合一级释放模型。结论该法制备的硝苯地平缓释微丸片,载药量高,工艺简便,易于操作。Objective To prepare nifedipine （NF） sustained-release pellet tablets, and study of its release behavior in vitro. Methods Soluplus was selected as a carrier to prepare solid dispersion of NF by hot melt extrusion technique （ HME）, and the ratio of the drug to carrier was 1： 1. The samples were validated as the solid dispersion by differential scanning calorimetry （DSC）. Extrusion-spheronization technique was introduced to prepare NF pellets and EudragitRS 30D was used as the coating material. The NF sustained-release tablets were prepared by direct compression of the coated pellets and suitable excipients. Results The release data in vitro proved that the drug release from the tablets was steady and complete over 24 hours. Conclusion The release of NF from sustained-release tablets is slow and steady. The method is easy to operate. The in vitro drug release pattern follows first-order kinetics.

关 键 词：硝苯地平 热熔融挤出法 挤出-滚圆法 微丸片 释放度 体外 

分 类 号：R972.4[医药卫生—药品] TQ460.6[医药卫生—药学]