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蛇毒纤溶酶的体内过程及药物代谢动力学研究

Pharmacokinetic Studies of Nevin Fibrinolytic Enzyme

  • 摘要: 以125I-蛇毒纤溶酶作示踪剂对蛇毒纤溶酶的体内过程及药代动力学进行了研究。实验结果表明,静脉注射后,大鼠体内血药浓度时程曲线为二房室模型,T1/2β分别为6.1h(低剂量),6.3h(中剂量)和5.6h(高剂量)。小鼠尾静脉注射后3h,各脏器中放射性活性达到峰值,其值(%)大小顺序如下:肾(1.34)>肺((1.09)>肝(0.90)=脾(0.90)>心(0.51)>肌肉(0.45)>脑(0.29)。125I-蛇毒纤溶酶主要从尿排泄,静脉注射后,72h内尿排泄率达85.6%,而粪排泄仅为5.4%,胆汁排泄率为12%。

     

    Abstract: The pharmacokinetics of nevin fibrinolytic enzyme (NFE) was studied by 125I-NFE as a tracer. Experiment results have showed that the time-concentration curve mainly was fitted to a two-compartment model after i.v , and its T1/2β were 6.1h(0.02u/kg),6.3h(0.04u/kg)and 5.6h(0.08u/kg) respectively. The 125I-NFE was found to be distributed w idely in organs of mice after iv , the peak concentration of 125I-NFE in organs appeared at 3h , and its values were as follows: 1.34%(kidney) , 1.09%(lung) , 0.90%(liver) , 0.90%(spleen) , 0.51%(heart) , 0.45%(muscle) and 0.29%(brain). The 85.6% of 125I-NFE was excreted in urine and only 5.4% in feces in 72h after iv. The percentage of gall excretion in rats was 12 in 8h after iv.

     

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