^(125)I标记白眉蝮蛇毒精氨酸酯酶代谢动力学研究

Study on the pharmacokinetics of ^(125)I-labelled arginine esterase from Agkistrodon halys ussuriensis venom in rabbits

研究白眉蝮蛇(Agkistrodon halys ussuriensis)毒精氨酸酯酶的代谢动力学,为临床应用提供依据。125I标记的精氨酸酯酶对大鼠一侧颈静脉给药,不同时间从另一测颈静脉取血。5h后处死动物,取各组织、尿液、胆汁和粪便,对各样本的放射性进行测定并拟合时间-放射性关系曲线。代谢动力学拟合曲线符合一室模型,其中生物半衰期T1/2为55.9min,K值为0.0124min-1。125I标记的精氨酸酯酶在体内各组织广泛分布,但有血脑屏障存在,肝、肾和尿液中的放射性比其它组织要高很多,主要通过肝脏降解,肾脏排泄。

To study the pharmacokinetics and distribution of arginine esterase from Agkistrodon halys ussuriensis venom for its clinical application in the future, ^125I-arginine esterase was given to rabbits by intravenous injection and blood was taken at different time. Rabbits were killed 5 h later and their various tissues, bile, urine and feces were samoled. The radioactivity of all the samples was assayed. The radioactivity - time curve for blood was simulated by computer and the pharmacokinetic parameters were calculated. For pharmacokinetics, simulated curve corresponded to one compartment model. Biological half-life （T1/2） was 55.9 min, and K was 0. 0124 min^-1. The result indicated that ^125I-arginine esterase distributed broadly in tissues. Blood brain barrier existed. The radioactivity in liver, kidney and urine was much higher than that in other organs and it was degraded liver and eliminated fast mainly from kidney.