头孢克洛在中国健康志愿者体内的群体药代动力学研究  

Population pharmacokinetics of cefaclor in healthy Chinese adult male volunteers

作　　者：黄继汉[1] 黄晓晖[2] 王鲲[1] 李俊[2] 郑青山[1] 

机构地区：[1]上海中医药大学药物临床研究中心,上海201203 [2]安徽医科大学药学院基础与临床药理学教研室

出　　处：《中国临床药理学与治疗学》2012年第6期659-665,共7页Chinese Journal of Clinical Pharmacology and Therapeutics

基　　金：国家科技支撑计划项目(2008BAI51B03);安徽省优秀青年科技基金(08040106813);上海市教委创新项目(10YZ61)

摘　　要：目的:建立头孢克洛口服给药在健康志愿者体内的群体药代动力学模型,探讨个体因素对代谢反应的影响。方法:基于头孢克洛生物等效性试验数据,应用非线性混合效应模型的群体方法分析头孢克洛口服给药的生物等效性试验数据,估算相关药代动力学参数及变异。结果:头孢克洛在健康志愿者中符合一级吸收的二室模型。药物表观清除率(CL)、中央分布容积(V2)、中央分布容积(V3)、吸收速率常数(KA)的群体典型值分别为0.219L/min、35.9L、598L和0.042min-1。体重对清除率(CL)有显著影响。结论:群体药代动力学最终模型可对个体药代参数做出精确的估计,体重对表观清除率有影响。AIM： To develop a population pharmacokinetic model of cefaclor in healthy volunteers and evalute the effect of individual factors on the pharmacokinetics of cefaclor. METHODS： A nonlinear mixed-effect modeling was developed to analyze the data of cefaclor bioequivalence studies in healthy volunteers and calculate the related parameters and interand intra variabilties. RESULTS： two-compartment model with first order absorption was fitted to the cefaclor concentration data. The population value of CL, V2, V3, KA were 598 L , 0.042 min^-1, 0. 219 L/min, 35.9 L, respectively. CL was found to be significantly related to the covariate of weight. CONCLUSION. The population pharmacokinetic model can be used to provide accu- rate individual pharmacokinetic parameters. CL was significantly influenced by the covariate of weight, which showed that it is better to administer drug according to the per kilogram of body weight in clinical practice.

关 键 词：头孢克洛 健康志愿者 群体药代动力学 

分 类 号：R969[医药卫生—药理学]