pH敏感双层型苦参结肠靶向微丸在大鼠体内的药代动力学研究

Pharmacokinetic Study in Rats on pH-triggered Double Layer Colon Target Pellets of Sophora Flavescens

目的:比较苦参结肠靶向微丸与苦参溶液中苦参碱的药动学行为差异,以明确该靶向制剂在体内的药动学特征。方法:采用反相高效液相法,检测给药后血浆、结肠内容物中苦参碱含量;用DAS药动学软件统计程序处理,提取PK参数。结果:微丸与溶液中苦参碱在血浆及结肠内容物中tmax,Cmax,AUC等参数均有明显差异,微丸中苦参碱吸收存在明显的迟滞效应,且大部分未被吸收进入体循环,而在结肠中显示出高浓度分布。结论:制备的苦参微丸具有良好结肠靶向分布特征,达到了预期设计目标。

Objective：To compare pharmacokinetics of matrine between colon target pellets of Sophora Flavescens and solution,make clear the pharmacokinetic character of the targeted agents in vivo.Method：RP-HPLC was applied to determine the content of matrine in plasma and colon contents after the administration and DAS pharmacokinetic software was used for calculating the acquired PK parameters.Result：The parameters of matrine contained in pellets in plasma and colon contents were all differed from those in solution,such as tmax,Cmax,AUC ad.There was obviously delay effect on absorbability of matrine in pellet,and most of that was not absorbed into systemic circulation,and then high concentration distribution was found in colon.Conclusion：The pellets of Sophora Flavescens prepared show good colon-specific distribution characteristics,and achieve the expected design goal.