摘要
目的:制备间尼索地平微孔渗透泵微丸,并探讨其释药机制。方法:以磺丁基醚-β-环糊精(SBE-β-CD)为渗透压物质,采用挤出滚圆法制备丸芯,流化床包衣法包衣;以累积释放度为指标,通过单因素法考察增塑剂癸二酸二丁酯(DBS)用量、包衣增重、包衣液(醋酸纤维素的丙酮-异丙醇溶液)浓度对微丸释放的影响,优选包衣处方。按最优处方制备3批微丸并以累积释放度与时间进行零级、一级、Higuchi方程拟合来考察其释药特征。结果:增塑剂用量为15%,包衣增重为4%,包衣液浓度为1%;所制备的间尼索地平微孔渗透泵微丸12h内释药具有零级释放特征(r=0.9996,0.9995,0.9989),释放动力以渗透压为主。结论:该制备工艺稳定、重现性良好,12h内释药恒定。
OBJECTIVE：To prepare m-nisoldipine（m-Nis） controlled porosity-osmotic pump pellets,and to study the release mechanism.METHODS：Sulfobutylether-β-cyclodextrin（SBE-β-CD） was used as a solubilizing and osmotic agent.The extrusion-spheronisation method was used to prepare the core of pellets which then coated by fluid-bed coating technology.The single factor design was applied to review the influence of the amount of DBS,coating weight and the concentration of acetone-isopropyl alcohol on the dissolution of pellets.3 batches of pellets were prepared in a ccordance with the optimal prescription and zero and first-order,Higuchi equation of cumulative release with time were fitted to study its release characteristics.RESULTS：The formula of coating was optimized as follows：DBS of 15%,coating weight of 4%,cellulose acetate（CA） acetone-isopropanol solution of 1%.Zero-order kinetics existed in the release of the pellets in 12 h（r=0.999 6,0.999 5,0.998 9）.Moreover,the osmotic pressure-controlled delivery was greatly responsible for drug release.CONCLUSION：The preparation technique is stable with a good repeatability in a constant release within 12 h.
出处
《中国药房》
CAS
CSCD
2012年第33期3102-3105,共4页
China Pharmacy
基金
河北省自然科学基金资助项目(C2010000488)
关键词
间尼索地平
微丸
制备
磺丁基醚-Β-环糊精
渗透泵
零级释放
渗透压
m-Nisoldipine
Pellets
Preparation
Sulfobutylether-β-cyclodextrin
Osmotic pump
Zero-order release
Osmotic pressure
