摘要
目的:制备硝苯地平骨架型和膜控型两种24小时缓释微丸,以释放度为指标比较两者优劣,并研究其释放机理。方法:以硬脂酸和乙基纤维素为材料,挤出滚圆法制备硝苯地平骨架型缓释微丸;以液相层积空白丸芯上药法制备载药速释丸芯,以苏丽丝E-7-19040为包衣材料,用流化床制备硝苯地平膜控型缓释微丸;并研究其释放机制。以综合评分P=|P2h-20%|+|P12h-60%|+|P24h-100%|评价两种微丸的释放行为优劣。结果:两种方法制备的微丸都能达到24小时缓释的效果;释放机制均为药物扩散与骨架溶蚀协同作用。结论:膜控型缓释微丸的释放行为略优于骨架型缓释微丸,但骨架型缓释微丸的制备工艺较膜控型简单可行。
Objective：To prepare Nifedipine matrix and coated sustained-release pellets,compare their release profile and mechanism.Methods：Nifedipine matrix sustained-release pellets were prepared by extrusion-spheronisation method using ethylcellulose and stearic acid as matrix material,and nifedipine coated sustained-release pellets were prepared in a fluidized bed coating system,using Surelease-7-19040 R as coated material.Simulated equation and relative coefficient were calculated and compared after data of drug release were input.Comprehensive score P=｜P2h-20%｜＋｜P12h-60%｜＋｜P24h-100%｜was used to compare the release profile of two types of pellets.Result：Both the two types of prepared pellets had significant effect of sustained-releasing.Drug release from the two types of pellets was controlled by both diffusion and matrix corrosion.Conclusion：The release profile of nifedipine coated sustained-release pellets was superior to nifedipine matrix sustained-release pellets.But the preparation of nifedipine matrix sustained-release pellets was more applicable than coated sustained-release pellets.
出处
《药学与临床研究》
2010年第3期235-238,共4页
Pharmaceutical and Clinical Research
基金
国家新药创制科技重大专项(NO2009zx09310-004)
国家科技支撑计划项目(No2008BA155B03)
关键词
硝苯地平
缓释微丸
挤出滚圆
流化床包衣
固体分散体
Nifedipine
Sustained-release pellets
Extrusion-spheronisation
Fluidized bed coating
Solid dispersions
