盐酸普罗帕酮结肠定位释药微丸的研制  

Preparation of propafenone hydrochloride colon-specific release pellets

作　　者：尹飞[1] 王彩霞[2] 张雪竹[2] 李巧云[2] 谭一宁 邹梅娟[2] 

机构地区：[1]辽宁省肿瘤医院药剂科,沈阳110042 [2]沈阳药科大学药学院,沈阳110016

出　　处：《中国新药杂志》2014年第6期711-715,共5页Chinese Journal of New Drugs

摘　　要：目的：针对心律失常明显的“日高夜低”的昼夜节律特点，研制盐酸普罗帕酮结肠定位释药微丸，以期按照生理和治疗需择时、定量给药，实现最佳疗效。方法：以MCC丸芯为母核采用粉末层积法制备盐酸普罗帕酮含药微丸。使用流化床包衣技术，选择L—HPC作为内层溶胀包衣材料，EudragitNE30D作为外层控释包衣材料制备盐酸普罗帕酮结肠定位释药微丸。结果：确定了含药微丸的处方。并以药物开始释放时间（时滞）和时滞后90rain释放度为指标，考察了溶胀层包衣材料类型、溶胀层包衣增重、溶胀层添加剂的种类、控释层包衣增重、抗黏剂用量和老化时间等因素对药物释放的影响，确定了最终包衣的处方。结论：制备了延迟3～4h释药的结肠定位释药系统。Objective： To develop a kind of propafenone hydrochloride （PPH） colon-specific release pel- lets for chronotherapy of arrhythmia. Methods：The propafenone hydrochloride pellets were prepared by centrifugal granulator using MCC beads by powder layer technology. A fluid bed spray processor was adopted for coating the pellets prepared by centrifugal granulator with L-HPC as swelling layer and Eudragit NE 30D aqueous dispersion as controlling layer. Results：Centrifugal granulation technology was suitable to prepare propafenone hydrochloride pel- lets. Coating factors including type of swelling layer, coating amounts of swelling layer and controlling layer, additive in the swelling layer, talc amount and curing time were investigated with accumulative release percentages as the in- dex. Conclusion： PPH was released from the pellets after a lag time of 3 - 4 h.

关 键 词：盐酸普罗帕酮 结肠定位释药 微丸 

分 类 号：R943.4[医药卫生—药剂学] R972.2[医药卫生—药学]