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采用RP-HPLC法,测定给药后不同时刻大鼠血浆中雷公藤内酯酮的浓度。大鼠iv0.7,1.4,2.8mg·k-1雷公藤内酯酮后,血浓数据用PKBP-NI程序拟合,药物动力学模型为两室开放模型,T1/2α为0.167~0.195h,T1/2β为4.95~6.49h,曲线下面积(AUC)与剂量成正比,清除率(CLs)与剂量无关。非房室模型统计矩计算的结果表明,3剂量平均驻留时间MRT为3.26~5.14h。大鼠iv雷公藤内酯酮后,在大鼠体内分布广泛,其中以肺和肝药物浓度最高,心、肾、脾和肌肉次之,宰丸、胃肠道和脑中最低。iv雷公藤内酯酮后,经尿和胆汁排泄的原型药物较少。雷公藤内酯酮的血浆蛋白结合率约为75%。
The plasma concentrations of triptolide were determined by RP-HPLC at different time points after administration. Rat iv 0.7, 1.4, 2.8 mg · k-1 triptolide, blood concentration data were fitted by PKBP-NI program, the pharmacokinetic model for the two-compartment open model, T1 / 2α 0. 167 ~ 0.195h, T1 / 2β was 4.95 ~ 6.49h. The area under the curve (AUC) was proportional to the dose, and the clearance rate (CLs) was independent of dose. The calculation results of the statistical moments of non-atrioventricular model showed that the average MRT of 3 doses was 3.26-5.14h. Rat iv triptolide, widely distributed in rats, with the highest concentration of pulmonary and hepatic drugs, followed by heart, kidney, spleen and muscle, slaughter pill, the lowest in the gastrointestinal tract and brain. After triptolide iv, less urinary and biliary excretion of the prototype drug. Triptolide plasma protein binding rate of about 75%.