解热药YL2000中蛇床子素在正常和发热大鼠体内药物代谢动力学比较

Comparison for Pharmacokinetics of Osthole Contained in Antifebrile Complex YL2000 Between Normal and Febrile Rats

目的 :探讨中药有效部位新药YL2 0 0 0中蛇床子素在正常和发热大鼠体内的代谢动力学。方法 :采用高效液相色谱技术分别测定正常大鼠和干酵母致发热大鼠血浆中蛇床子素的含量 ,使用 3P87软件处理蛇床子素的时量数据 ,计算各药代动力学参数。结果 :在正常和发热大鼠体内 ,蛇床子素的达峰时间分别为 1 6 2h和 4 0 2h ,峰值血药浓度分别达 0 0 3ug ml和0 0 4ug ml,t1 2 (ke)分别长达 2 98h和 2 0 0h ,t1 2 (ka)分别为 0 4 3h和 1 0 9h ,CL F值分别为 4 2 2 1(mg kg) h (ug ml)和 2 715 (mg kg) h (ug ml) ,AUC( 0 -T) 值分别为 0 189(ug ml) h和 0 2 9(ug ml) h。结论 :发热对蛇床子素的药动学有一定的影响 ,可以延缓它的吸收 ,增加它的吸收率 ,最终导致模型组的AUC( 0 -T) 增大。

Objective:To explore pharmacokinetics for osthole of YL2000 in normal and febrile rats. Methods:The levels of osthole in plasma were measured through HPLC and the secondary parameters were obtained by fitting the osthole concentration-time data using 3P87 software. Results:In normal and febrile rats,the plasma concentration of osthole was peaked at 1.62h vs.4.02h with a level of 0.03ug/ml vs. 0.04ug/ml,and the t 1/2(ke), t 1/2(ka), CL/F and AUC (0-T) of osthole was 2.98h vs. 2.00h, 0.43h vs. 1.09h, 4221(mg/kg)/h/(ug/ml) vs.2715(mg/kg)/h/(ug/ml) and 0.189(ug/ml)*h vs. 0.29(ug/ml)*h, respectively. Conclusion:Fever induced effects on pharmacokinetics of osthole,including delay of absorption and increas in AUC (0-T).