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1、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1U、2U、4U3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：tl/2a为34~55min；tl/2B为30广351min；CL分别为0.001l、0.0012.0.0009L/(min•kg),Vd分别为1.3570、0.5934、0.4
2、101L/kg,AUCO-tn分别为16518.38、22405.67和29531.41uU/(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。［关键词］类凝血酶；药动学；放射免疫分析法［中图分类号］R917E文献标识码］A［文章编号11673-7210(2011)04(a)-059-04Pharmacokineticsofathrombin-likeenzymeinjectioninChinesehealthyvolunteersSHEN
3、Wenyul,DIWeiqingl,LIUHongdal,ZHANGJingchaol,NIUHuisheng2,LIHuaifen21.LiaoningNuokangBiologicalpharmaceuticalLimitedLiabilityCompany,Shenyang110171；2.ChineseAcademyofMedicalSciencesRadiologyInstituteofRadiologicalMedicineResearch,Tianjin300000_Abstract]O
4、bjective:Tostudythepharmacokineticsofheamocoagulaseagkistrodon(HCA)injectionafterasingledoseinChinesehealthyvolunteers・Methods：30malehealthyvolunteerswererandomlyallocatedintothreegroups,receiving1U,2U,4UHCAinjection,respectively.Everygrouphadtenvolunte
5、ers・Thedrugconcentrationinhumanserumweredeterminedbyradioimmunoassaymethod,andthepharmacokineticparameterswerecalculatedbyDASsoftware・Results：Theserumconcentration-timecurvefitthetwo-compartmentmodelafteriv1U,2U,4UHCA.Thepharmacokineticparameterswereasf
6、ollows：itstl/2arequired34~55min,tl/2Brequired301-351min.CLwere0.0011,0.0012,0.0009L/(min•kg),respectively・Vdwere1.3570,0.5934,0.4101L/kg,respectively.AUC0-tnwere16518.38,22405.67and29531.41uU/(min•ml),respectively,inadose-dependentmanner・Conclusion：Thec
7、haractersofinvivopharmacokineticsofasingledoseadministrationofHCAfitthefirst-orderdynamicsequationandtwo-compartmentmodel..Keywords]Thrombin-likeenzyme；Pharmacokinetics；Radioimmunoasssy蛇毒类凝血酶(SnakeVenomThrombin-likeEnzyme,SVTLE)是蛇毒中与血浆凝血酶性质相似的一类酶的总称[1-2
8、]o注射用尖吻蛇毒血凝酶是蛇毒类凝血酶的一种冻干粉针剂[3-4],是从尖吻蝮蛇蛇毒中采用现代生物化学分离提取技术分离纯化得到的，经药效试验证明具有良好促凝血作用及止血效果[5-6]o放射免疫分析(RIA)方法[7-8]具有灵敏度高、特异性强、重复性好特点，广泛应用于生物医学研究和临床诊断领域中各种蛋白质、激素、小分子药物和肿瘤标志物的定量分析。本实验采用放射免疫分析(RIA)方法测定单次静注注射用HCA后的血药浓度，考察其在健康人体内的代谢规律。1仪器与
