来氟米特活性代谢产物A771726在小鼠体内的药动学研究

Pharmacokinetics of A771726 the metabolite of leflunomide in mice

目的研究A771726在小鼠体内的药代动力学过程。方法单剂量尾静脉注射三个剂量的A771726,根据小鼠体内血药浓度经时过程,估算相应的药代动力学参数。结果A771726(4,12,36 mg.kg-1)的血药经时过程均符合一级吸收的一房室模型,其主要药动学参数为:t1/2Ke(h):(18.63±1.78),(31.07±7.33),(25.41±2.76);C0(mg.L-1):(19.92±1.20),(49.58±9.00),(182.14±22.98);AUC(mg.h-1.L-1):(533.99±41.49),(2173.88±440.21),(6621.97±584.25)。结论单剂量尾静脉注射A771726三个剂量组的药物代谢均成线性关系,其血药浓度-时间曲线符合一级吸收的一房室模型。

Aim To study the pharmacokinetics of A771726, metabolite of leflunomide, in mice. Methods Caudal vein injection of single dose of A771726（4, 12, 36 mg · kg^-1）, then calculate corresponding pharmacokinetic parameters based on the time process of blood drug concentration. Results The serum concentration-time curve of A771726 conformed to one compartment model of the first order absorption. The main pharmacokinetic parameters of A771726 （4, 12, 36 mg · kg^-1） were t 1/2ke （h） ： （18.63 1.78） , （31.07 7. 33）, （25.41 2,76）; C0（mg·L^-1）： （19.92 1.20）, （49.58 9.00）, （182.14 22.98）; AUC（mg. h^-1 ·L^-1）： （533.9941.49）, （ 2173.88 440.21 ）, （6621.97 584.25 ）. Conclusion The metabolite of A771726 following caudal vein injection accords with the linear relation, and its serum concentration-time curve consists with the first - order kinetics of one-compartment model.