pH敏感双层型苦参结肠靶向微丸的体内外释药性能评价

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1 h,完全自胃部排空,5 h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。

Evaluation In vivo / in vitro of pH-triggered Double Layer Colon Target Pellets of Sophora flavescens

Objective: To evaluate the drug release in colon targeting of pH-triggered double layer colon target pellets of Sophora flavescens in vivo and in vitro. Method: Evaluate the drug release of the pellets in vitro with paddle method. Multi-slice spiral CT scanning was applied to detect the conveying of pellets in the digestive canal of human body in real time. Result: The pellets altogether released 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 were all emptied from stomach one hour after taking orally and all reached to colon after five hours. The disintegration of the pellets was not detected in stomach and small intestine, which started to disintegration after entering colon, disaggregated obviously after ten hours and completely disaggregated in colon after twenty-four hours. Conclusion: The pellets possess well drug release of colon targeting in vivo and in vitro.