注射用比阿培南单剂量及多剂量静脉滴注给药的人体药动学研究

目的:研究注射用比阿培南单剂量及多剂量静脉滴注的人体药动学过程。方法:采用单中心、开放、随机自身对照设计,12名健康受试者单剂量恒速静脉滴注注射用比阿培南300mg;单剂量试验结束后进入多剂量给药试验,q12h,连续给药5d。采用高效液相色谱法测定血浆和尿液中比阿培南的浓度,并采用DAS药动学软件对试验数据进行处理,求算有关药动学参数。结果:12名健康受试者单剂量静脉滴注注射用比阿培南后,主要药动学参数分别为cma(x13.74±4.40)μg.mL-1,tma(x0.51±0.11)h,t1/2β(1.34±0.41)h,t1/2(z1.18±0.23)h,AUC0～(t15.60±2.95)μg.h.mL-1,12h平均尿液累积排泄率为(33.04±13.54)%。多剂量静脉滴注达稳态后的主要药动学参数cssmin因低于定量下限而未检测出,cssmax为(15.12±3.27)μg.mL-1,cssav为(1.43±0.23)mg.L-1,tssmax为(0.49±0.05)h,t1/2β为(1.33±0.39)h,t1/2z为(1.02±0.18)h,AUC0～t为(17.18±2.73)μg.h.mL-1,血药浓度波动系数DF为(10.56±1.55)%。结论:注射用比阿培南静脉滴注给药300mg,q12h,连续给药5d,药物在体内无蓄积,安全性好。

Pharmacokinetics of Single and Multiple Doses of Biapenem for Injection in Chinese Healthy Volunteers with Intravenous Administration

OBJECTIVE:To investigate the pharmacokinetics of Biapenem for injection with a single and multiple dose administration in Chinese healthy volunteers.METHODS:In single-center open randomized controlled design,12 healthy volunteers received a single dose intravenous infusion of 300 mg biapenem,and then they were repeatedly administrated with 300 mg biapenem every 12 hour for 5 days.The concentrations of biapenem in plasma and urine were determined by HPLC.DAS pharmacokinetics software was used for data proces...