白头翁总皂苷-羟丙基-β-环糊精包合物结肠靶向微丸的制备  

Preparation of colon target pellets of Pulsatilla total saponinshydroxypropyl-β-cyclodextrin inclusion

作　　者：陈振华[1] 管咏梅[2] 朱卫丰[2] 杨明[2] 刘红宁[2] 杨世林[2] 

机构地区：[1]江西科技师范大学药学院,江西南昌330013 [2]江西中医药大学现代中药制剂教育部重点实验室,江西南昌330004

出　　处：《中国中药杂志》2013年第24期4292-4297,共6页China Journal of Chinese Materia Medica

基　　金：国家"重大新药创制"科技重大专项(2013ZX09103-002-001);江西省自然科学基金项目(20122BAB215041);江西科技师范大学重点科研课题项目(KY2011ZZ05);江西省教育厅科技落地计划项目(赣财教[2011]243号);江西省卫生厅中医药科研项目(2012A152)

摘　　要：目的:制备白头翁总皂苷结肠靶向微丸。方法:采用水溶液-搅拌法制备白头翁总皂苷-羟丙基-β-环糊精包合物,再以制粒-滚圆法制备微丸,利用Glatt流化床进行包衣。结果:白头翁总皂苷微丸2 h溶出度为16.0%,而包合物微丸0.5h溶出度达91.9%。以Eudragit S100为包衣材料、TEC为增塑剂、滑石粉为抗黏剂、包衣增重为12%时,包衣效率高,几乎无黏结现象,包衣微丸在人工胃液中2 h几乎无药物释放,人工小肠液4 h药物累积释放度小于15%,人工结肠液4 h药物累积释放度大于90%。结论:白头翁总皂苷-羟丙基-β-环糊精包合物包衣微丸具有良好的体外结肠靶向释药特征,可进一步研制成口服结肠靶向制剂。Objective： To prepare colon target pellets of Pulsatilla total saponins. Method： Pulsatilla total saponinshydmxypropyl-β-cyclodextrin inclusion was prepared by the water solution-mixing method. Then plain piUs of inclusion were prepared by the granulation-spheronization method, and coated by GIatt fluid bed. Result： The dissolution of plain pills of Pulsatilla total saponins at 2 h was 16. 0%, while that of plain pills of inclusion at 0. 5 h was 91.9%. With Eudragit S100 as the coating material, TEC as the plasticizer and talcum power as the anti-adherent, when the coating weight was 12% , the coating efficiency was high, with almost no bonding and drug release of coated pellets in artificial gastric juice for 2 h. The accumulated drug release in artificial intestinal fluid for 4 h was less than 15%, and that in artificial colon fluid for 4 h was more than 90%. Conclusion： Coated pellets of Pulsatilla total saponins-hydroxypropyl-fl-cyclodextrin inclusion showed a good colon targeted drug release in vitro, thus could be further developed to be oral colon targeted preparations.

关 键 词：白头翁总皂苷 包合物 结肠靶向 微丸 

分 类 号：TQ461[化学工程—制药化工]