薏苡素包合物的药动学及组织分布研究

Pharmacokinetics and tissue distribution of coixol-HP-β-CD clathrate

目的:研究薏苡素-羟丙基-β-环糊精(coixol-hydroxypropyl-β-cyclodextrin,薏苡素-HP-β-CD)包合物在大鼠体内的药动学及组织分布,为其新剂型的研发提供依据。方法:采用HPLC法测定血浆及组织中薏苡素的含量,药动学分析软件DAS 2.0计算药动学参数。结果:药动学实验中,制剂组的AUC_(0-10)是原药组的2.38倍,末端消除半衰期t_(1/2)由0.83 h延长到1.97 h。药物在各组织中分布随着时间而变化,薏苡素及包合物在各组织器官中药物浓度大小依次为:肾>肝>脾>心>肺>脑。制剂组各组织的分布浓度均有显著提高。结论:薏苡素制成包合物后可延缓其在体内的代谢消除,达到了提高生物利用度的效果。

Objective:To study the pharmacokinetics and tissue distribution of coixol-HP-β-CD clathrate in rats and provide reference for the development of new coixol formulations.Methods:The contents of coixol in plasma and tissues were determined by HPLC.The pharmacokinetic parameters were calculated using DAS 2.0 program.Results:In pharmacokinetic study,results show that the AUC_((0-10))of the preparation group was 2.38-fold of the original drug group,and t_(1/2)was extended from 0.83 to 1.97 h.The issue distribution results show that the distribution of the drug in each tissue changes with time.The levels of drug and clathrate in organs rank:kidney>liver>spleen>heart>lung>brain.The distribution concentrations in each tissue of the preparation group was significantly increased.Conclusion:The complex packaged by HP-β-CD could delay the metabolic elimination of coixol in body and prolong the half-life,achieving slow release and increased bioavailability.