离心造粒包衣技术制备姜黄素pH依赖-时控型结肠靶向小丸  

Preparation of pH-based and time-lag type pellets of curcumin for colon-targeted by centrifugal granulation coating technology

作　　者：倪文娟[1] 张永生[1] 章文红[2] 王彬辉[2] 张晓芬[2] 

机构地区：[1]浙江中医药大学药学院,浙江杭州310053 [2]台州学院医学院附属市立医院药剂科,浙江台州318000

出　　处：《中国现代医生》2014年第6期71-73,76,共4页China Modern Doctor

基　　金：浙江省中医药科学研究基金计划(2011ZB160);浙江省台州市椒江区科技计划(10284)

摘　　要：目的探讨制备姜黄素pH依赖-时控型结肠靶向小丸制备工艺。方法采用离心造粒包衣技术,以粉末层积法制备载姜黄素素丸,再分别包衣EC(时控内层)及Eudragit FS30D(pH依赖外层),得到姜黄素pH依赖-时控型结肠靶向小丸,并优化最佳制备工艺。结果时控层包衣液由3.0%EC、0.6%邻苯二甲酸二乙酯、25%滑石粉乙醇溶液组成,包衣增重2.0%;pH依赖层包衣液由Eudragit FS30D、40%滑石粉和3.0%柠檬酸三乙酯组成,包衣增重4.0%。此小丸在人工胃液2、3 h后累积释放百分率<15%,在人工结肠液5 h后累积释放百分率>85%,有显著的结肠定位及释药特性。结论以EC作为时控内层,Eudragit FS30D作为pH依赖外层,可制备姜黄素结肠靶向释药系统。Objective To prepare pH-based and time-lag type pellets of curcumin for colon-targeted. Methods The pH-based and time-lag type pellets of curcumin for colon-targeted were prepared by Centrifugal granulation coating technology and by means of powder layering. Pellets were coated EC （time-lag type inner layer） and Eudragit FS30D （pH-based outer layer）, then optimize the best preparation. Results The coating liquid of time-lag type inner layer was controlled by the 3.0% EC, 0.6% diethyl phthalate, and 25% ethanol solution composition talc, coating weight more 2.0%; The coating liquid of pH-based outer layer was controlled by the Eudragit FS30D, 40% talc and 3.0% triethyl citrate composition, coating weight more 4.0%. The accumulated release rates of the pellets were less than 15% in artificial succus gastricus and intestinal juice, The accumulated release rates of the pellets were more than 85% in the artificial colonic juice within 5 h with indicated a significant feature of colon-targeted. Conclusion EC as time-lag type inner layer, Eudragit FS30D as a pH-based outer layer can be prepared pellets of curcumin for colon-targeted.

关 键 词：姜黄素 PH依赖 时控型 结肠 体外释药 

分 类 号：R460.6[医药卫生—临床医学]