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,药一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0.0011、0.0012、0.000 9L/(min·kg),Vd分别为1.357 0、0.593 4、0.410 1 L/kg,AUC0-th分别为16 518.38、22 405.67和29 531.41 μU/(min·ml),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.%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 t 1/2α required 34-55 min,t1/2α required 301-351 min. CL were 0.001 1, 0.001 2, 0.000 9L/(min·kg),respectively. Vd were 1357 0, 0593 4, 0.410 1 1L/kg, respectively. A UC0-tn were 16 51838, 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.
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