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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 the pharmacokinetic behavior of matrine in kushen colon-targeting pellets with kushen solution to clarify the pharmacokinetic characteristics of the targeted preparation in vivo. Methods: The contents of matrine in plasma and colon were determined by reversed-phase high-performance liquid chromatography. PK parameters were extracted by DAS pharmacokinetic software. Results: The parameters of tmax, Cmax, AUC and other parameters of matrine in plasma and colon contents were significantly different between the pellets and the solution. There was a significant hysteresis effect of matrine absorption in the pellets, and most of them were not absorbed into the systemic circulation , While in the colon showed a high concentration profile. Conclusion: The prepared kushen pellets have good distribution characteristics of colon targeting, reaching the expected design goals.