【摘要】 目的:通过健康志愿者口服法罗培南进行药动学研究,了解药物在人体内分布、消除规律,为制定合理给药方案提供依据。方法:选择9名健康成人按拉丁方随机分组,分别单剂口服100,200,300 mg三个剂量的法罗培南后,应用微生物法测定血药和尿药浓度,采用3P87软件进行数据处理,求出药动学参数。结果: 血清和尿液中法罗培南分别在0．05-6．4 mg·L-1浓度范围内呈良好的线性关系,日内、日间变异系数及回收率均符合临床药动学研究的要求。受试者单剂口服法罗培南100,200,300 mg后,药-时曲线符合二室模型, 主要药动学参数cmax分别为(2．2±s 0．4),(3．8±1．0),(6．0±0．5)mg·L-1;t1/2β为(0．72±0．22),(0．67±0．24), (0．92±0．19)h;AUC分别为(3．4±1．0),(6±3),(8．8±1．5)mg·h·L-1。24 h尿药累积排泄率分别为(2．1± 0．7),(3．2±1．0),(4．2±0．7)％。结论:法罗培南药-时曲线符合二室模型,cmax和AUC与剂量成正比,而t1/2β基本相同,该药具有线性动力学特征。更多还原

【Abstract】 AIM: To investigate the pharmacokinetics of faropenera after a single dose administration in healthy volunteers. METHODS: Nine selected volunteers after passing health and laboratory examination were divided into 3 groups randomly by Latin square. The drug concentration in serum and urine of the volunteers after taking single oral doses of 100,200,300 mg faropenem separately for each groups member were determined by microbiological analysis.The pharmacokinetic parameters were calculated by 3P87 software. RESULTS:Serum and urine concentrations of 0.05-6.4 mg·L-1 were found in well linearity .The precisions of within-days and the recovery rate were all coincided with the study on the clinical pharmacokinetics.The serum concentration-time curve showed coincidence with the two compartment model after administration of single oral doses of faropenem tablets 100,200,300 mg. The main pharmacokinetic parameters of cmax,t1/2β and AUC were (2.2 ± 0.4), (3.8 ± 1.0), (6.0 ±0.5) mg·L-1; (0.72 ±0.22), (0.67 ±0.24), (0.92 ±0.19) h and (3.4 ± 1.0), (6 ± 3), (8.8 ± 1.5) mg· h·L-1 respectively. The amount of cumulative recovery of faropenem in urine within 24 h were(2.1 ± 0.7), (3.2 ± 1.0), (4.2 ± 0.7) % respectively after singe dose administration of 100,200,300 mg. CONCLUSION: The serum concentration-time curve of faropenem coincides with the two compartment model. The cmax and A UC are in direct proportion with the dosage of drug. There is no significant difference in pharmacokinetic parameters between t1/2β of the three groups.Faropenem has linear linear dynamic feature.更多还原