法罗培南钠多剂量静脉滴注在中国健康人体的药代动力学  

Pharmacokinetics of faropenem after multiple intravenous infusion administration in Chinese healthy volunteers

作　　者：苏克剑[1] 孙黎[1] 杨娟[1] 刘瑾[1] 

机构地区：[1]上海交通大学医学院附属仁济医院临床药理研究室,上海200001

出　　处：《中国临床药理学杂志》2011年第2期110-113,共4页The Chinese Journal of Clinical Pharmacology

基　　金：国家科技部"重大新药创制"科技重大专项基金资助项目(2008ZX09312-007)

摘　　要：目的研究多剂量静脉滴注法罗培南钠(β内酰胺类抗生素)在中国健康人体的药代动力学。方法 11名健康志愿者接受多剂量静脉滴注法罗培南钠(600 mg,tid×7 d),用高效液相色谱-紫外检测法,测定法罗培南的血药浓度、尿药浓度,用3P87软件计算药代动力学参数。结果血药浓度-时间曲线符合二房室模型,体内过程呈线性动力学特征。主要的药代动力学参数:单剂量给药后,Cmax为(62.54±10.58)μg.mL-1;t1/2α为(0.39±0.12)h;t1/2β为(1.40±0.68)h;AUC0-8为(67.34±11.80)μg.h.mL-1;尿药累积排泄率为(26.24±10.48)%。多剂量给药达稳态后,Csmsin为(0.13±0.05)μg.mL-1;Cmssax为(58.13±9.93)μg.mL-1;Cav为(7.14±1.00)μg.mL-1;t1/2α为(0.31±0.05)h;t1/2β为(1.09±0.11)h;AUCs0s-t为(57.15±8.01)μg.h.mL-1;尿药累积排泄率为(30.21±15.94)%。结论多剂量给药后,法罗培南在体内的分布和消除速度较单剂量给药有所加快。Objective To study the pharmacokinetics of faropenem after multiple intravenous infusion administration in Chinese healthy volunteers.Methods Eleven healthy volunteers received faropenem at multiple dose（600 mg,tid 7 d）.The concentrations of faropenem in plasma and urine were assayed by HPLC-UV method.The pharmacokinetic parameters of faropenem were calculated by 3P87 software.Results It was found that the plasma concentration-time curves of faropenem were fitted to a two-compartment model,and physiological dispositions were assumed by linear kinetics characteristics.The main pharmacokinetic parameters were as follows：obtained from the single dose study,Cmax was（62.54±10.58） μg·mL^-1;t1/2αwas（0.39±0.12） h;t1/2βwas（1.40±0.68） h;AUC0-8 was（67.34±11.80） μg·h·mL^-1;urinary recovery rate was（26.24±10.48）%.The steady-state pharmacokinetic parameters were as follows： Cmin^ss was（0.13±0.05） μg·mL^-1;Cmax^ss was（58.13±9.93） μg·mL^-1;Cav was（7.14±1.00） μg·mL^-1;t1/2α was（0.31±0.05） h;t1/2β was（1.09±0.11） h;AUC0-t^ss was（57.15±8.01） μg·h·mL^-1;urinary recovery rate was（30.21±15.94）%.Conclusion The results of multiple dose study showed that the absorption and elimination rate of faropenem was acceleratedcompared with single dose.

关 键 词：法罗培南 药代动力学 高效液相色谱 

分 类 号：R969.1[医药卫生—药理学] R978.11[医药卫生—药学]