一种类凝血酶制剂的人体药动学研究  

Pharmacokinetics of a thrombin-like enzyme injection in chinese healthy volunteers

作　　者：沈文彧 邸伟庆 刘宏大 张竞超 牛惠生[2] 李怀芬[2] 

机构地区：[1]辽宁诺康生物制药有限责任公司,辽宁沈阳110171 [2]中国医学科学院放射医学研究所,天津300000

出　　处：《中国医药导报》2011年第10期59-61,70,共4页China Medical Herald

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/(min.kg),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29 531.41μU/(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 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.Vd were 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.

关 键 词：类凝血酶 药动学 放射免疫分析法 

分 类 号：R917[医药卫生—药物分析学]