一种类凝血酶制剂人体药动学探究.docVIP

一种类凝血酶制剂人体药动学探究[摘要] 目的：研究单次静注注射用尖吻蛇毒血凝酶（HCA）的人体药代动力学规律。方法：30例男性健康志愿者随机分组至1 U、2 U、4 U 3个剂量组，每组 10例，采用放射免疫分析法对受试血清检测HCA的含量，用DAS软件计算其药代动力学参数。结果：受试者给药后，药-时曲线符合二室模型，主要药代动力学参数：t1/2α为34~55 min；t1/2β为301~351 min；CL分别为0.001 1、0.001 2、0.000 9 L/(minkg)，Vd分别为1.357 0、0.593 4、0.410 1 L/kg，AUC0-tn分别为16 518.38、22 405.67和29 531.41 μU/(minml)，呈明显的剂量依赖关系。结论：单次静注注射用HCA体内药代动力学特征符合一级线性动力学二室模型。 [关键词] 类凝血酶；药动学；放射免疫分析法 [中图分类号] R917[文献标识码] A [文章编号]1673-7210（2011）04（a）-059-04 Pharmacokinetics of a thrombin-like enzyme injection in chinese healthy volunteers SHEN Wenyu1, DI Weiqing1, LIU Hongda1, ZHANG Jingchao1，NIU Huisheng2, LI Huaifen2 1. Liaoning Nuokang Biological pharmaceuticalLimited Liability Company, Shenyang 110171; 2. Chinese Academy of Medical Sciences Radiology Institute of Radiological Medicine Research, Tianjin 300000 [Abstract] Objective： To study the pharmacokinetics of heamocoagulase agkistrodon (HCA) injection after a single dose in chinese healthy volunteers. Methods: 30 male healthy volunteers were randomly allocated into three groups, receiving 1 U,2 U, 4 U HCA injection, respectively. Every group had ten volunteers. The drug concentration in human serum were determined by radioimmunoassay method, and the pharmacokinetic parameters were calculated by DAS software. Results: The serum concentration-time curve fit the two-compartment model after iv 1 U, 2 U, 4 U HCA. The pharmacokinetic parameters were as follows: its t1/2α required 34-55 min, t1/2β required 301-351 min. CL were 0.001 1, 0.001 2, 0.000 9 L/(min?kg), respectively. Vdwere 1.357 0, 0.593 4, 0.410 1 L/kg, respectively. AUC0-tn were 16 518.38, 22 405.67 and 29 531.41 μU/(min?ml), respectively, in a dose-dependent manner. Conclusion: The characters of in vivo pharmacokinetics of a single dose administration of HCA fit the first-order dynamics equation and two-compartment model. [Key words] Thrombin-like enzyme; Pharmacokinetics; Radioimmunoasssy 蛇毒类凝血酶(Snake Venom Thrombin-like Enzyme, SVT