血竭中血竭素在大鼠体内药动学和组织分布研究

Study on pharmacokinetics and tissue distribution of hemorrhoet in import of dragon′s blood in rats

研究大鼠口服给药(ig)血竭(IDB)后药动学和组织分布特征.建立大鼠血浆和各组织中血竭素的HPLC测定方法,SD大鼠分别单次igIDB(1.0 g/kg)后,测定不同时间点大鼠血浆和各组织中的血竭素质量浓度,血药浓度采用药动学程序软件DAS 2.0计算药动学参数.主要药动学参数:血竭素t_(1/2)=4.86 h,α=0.54,β=0.01,AUC_((0-t))=146434.27μg/L/h,MRT_((0-t))=4.19 h,组织分布特征为在肝、肾、心组织中分布较高.igIDB后药效物质血竭素符合药动学二室模型,起效快,生物利用度高.血竭素在肝肾中分布最多,心中次之,提示与其归心、肝经有关.

To study the pharmacokinetics and tissue distribution characteristics of rats after oral administration(ig)intragastrous blood(IDB).HPLC method was established for the determination of serum and tissues of rats.After single intragastrically administration of IDB(1.0 g/kg),the plasma and tissues of SD rats were determined at different time points.Pharmacokinetic parameters were calculated by using pharmacokinetic program DAS 2.0.The main pharmacokinetic parameters were t_(1/2)=4.86 h,α=0.54,β=0.01,AUC_((0-t))=146434.27μg/L/h,MRT_((0-t))=4.19 h.Tissue distribution characteristics:higher distribution in liver、kidney and heart tissues.After iGIDB,the pharmacodynamic substance hemorrhoetin was in line with the pharmacokinetic two-compartment model,with quick onset and high bioavailability.The distribution of hemorrhoetin in the liver and kidney is the most,followed by the heart,suggesting that it is related to the heart and liver meridian.