齐墩果酸磷酸酯二钠盐的药物动力学与生物利用度研究

Studies on the pharmacokinetics and bioavailability of disodium oleanolic acid phosphate

采用高效液相色谱法对齐墩果酸磷酸酯二钠盐 (disodiumoleanolicacidphosphate,以下简称为OLANa2 )进行了大鼠体内的药物动力学与生物利用度研究。大鼠静脉注射 3种不同剂量 ( 4 0、5 0、6 0mg/kg)的OLANa2 注射液后 ,其药物动力学行为均符合二室开放模型特征 ,且在实验剂量范围内其药时过程为线性动力学。大鼠灌胃及肝门静脉给药后 ,其药时过程符合单室开放一级吸收模型特征。大鼠经灌胃、肝门静脉、颈静脉交叉给药后 ,灌胃的绝对生物利用度为 2 2 0 3% ,肝门静脉注射的绝对生物利用度为 88 89% ,胃肠道代谢或未吸收部分共为 6 6 9%。

This paper was focused on the studies of pharmacokinetics and bioavailability of disodium oleanolic acid phosphate(OLANa 2)in rats by the HPLC method. The experimental results showed that the concentration time curves of OLANa 2 after iv of 40,50, 60 mg/kg fitted in a two compartment open model, and the elimination of OLANa 2 from plasma was in accordance with liner kinetics. The concentration time curve of OLANa 2 in rats fitted in a one compartment open model with first order absorption after oral administration and hepatic portal vein injection. The drug was administrated to the rats via ig, iv and hepatic portal vein injection crossly, the absolute bioavailability was 22 03%, the first pass effect of the liver was 11 11% and about 66 86% of the drug was not absorbed or was metabolized in the gastrointestinal tract.