采用螺旋CT技术研究pH敏感双层型苦参微丸的-中国实验方剂学杂志.docVIP

pH敏感双层型苦参结肠靶向微丸的体内外释药性能评价 谢兴亮1，杨 明2，韩 丽3，陈 诚1，刘金秀1，胡文娟1 （1成都医学院药学院，成都，610083；2江西中医学院中药制剂教育部重点实验室，南昌；3成都中医药大学药学院，成都，611137） ［摘要］目的 评价pH敏感双层型苦参结肠靶向微丸的体内外结肠靶向性能。方法 采用桨法对微丸的体外释药性能进行评价，采用多层螺旋CT扫描技术，实时监测微丸在人体消化道内的运转情况。结果 该微丸在人工胃液2 h、小肠液4 h中共累积释药26.18%，而在人工结肠液中2 h后，累积释药达99.52%，基本释放完全。微丸口服后1h，完全自胃部排空，5h后所有微丸均到达结肠。在胃、小肠各部均未检测到微丸的崩解，进入结肠后开始检测到崩解溶散现象，10 h后检测到明显崩解，24 h后微丸在结肠完全崩解溶散。结论 该微丸在体内外均具有良好的结肠靶向释药性能。 ［关键词］苦参；pH敏感双层型结肠靶向微丸；多层螺旋CT；释药性能 In vivo / in vitro evaluation of pH-triggered double layer Colon Target Pellets of Sophora Flavescens XIE Xing-liang，Chen Cheng，Liu Jin-xiu，Hu Wen-juan (Pharmaceutical College，Chengdu Medical College, Chengdu 610083) YANG Ming（Jiangxi University of Traditional Chinese Medicine, Key Lab. of Modern Preparation of TCM, Ministry of Education, Nanchang 330004，China） Han Li（Pharmaceutical College，Chengdu University of Traditional Chinese Medcine, Chengdu Sichuan，611173，China） [Abstract] Objective：To evaluate the drug release in colon targeting of pH-triggered double layer colon target pellets in vivo and in vitro. Method：Evaluate the drug release of the pellets in vitro with paddle method. With multi-slice spiral CT scanning，detect the conveying of pellets in the digestive canal of human body. Result：The pellets altogether release 26.18% of the drug in artificial gastric juice for two hours and in artificial intestinal juice for four hours, and accumulate to release 99.52% of the drug in artificial colon juice for two hours. The pellets are all emptied from stomach one hour afer taking orally,and after five hours all reach colon. Do not detect the disintegration of the pellets in stomach and small intestine, which start to disintegration afer entering colon, disaggregate obviously afer ten hours,and completely disaggregate in colon afer twenty-four hours. Conclusion：The pellets possess well the drug release of colon targeting in vivo/in vitro. [Key words]Sophora flavescens；pH-triggered double layer colon target pellets；multi-slice spiral CT；drug