法罗培南钠片在健康人体中的药代动力学研究

Pharmacokinetics of faropenem sodiumin tablets in healthy volunteers

目的研究健康志愿者单次口服3个剂量法罗培南钠片的药代动力学。方法 12名健康志愿者,男女各半,随机分为3组,分别口服150、300和600 mg法罗培南钠片后,采用HPLC法测定血浆和尿液中法罗培南的浓度,应用DAS软件计算其药代动力学参数。结果单次口服3个剂量组(150、300和600 mg)法罗培南钠片,血浆中法罗培南的主要药代动力学参数:AUC0～t分别为(3.73±2.77)、(6.72±4.12)和(13.1±8.04)μg.h/mL;Cmax分别为(1.89±0.93)、(3.19±1.14)和(6.95±3.37)μg/mL;Tmax分别为(0.97±0.54)、(0.83±0.38)和(0.93±0.45)h;t1/2分别为(0.92±0.26)、(0.94±0.14)和(0.98±0.15)h。累积尿药排泄率分别为(6.23±7.09)%、(4.69±4.32)%和(4.14±2.95)%。结论健康人口服150～600 mg法罗培南钠片后,法罗培南在体内符合线性药代动力学特征。

Objective To investigate the pharmacokinetic characteristics of faropenem in healthy volunteers. Methods Twelve healthy volunteers（6 male,6 female）were randomly divided into 3 groups and administrated a single oral dose（150,300,600 mg）of faropenem sodiumin tablets.The concentration of faropenem in plasma was determined by HPLC.The pharmacokinetic parameters were calculated by DAS software. Results The main pharmacokinetics parameters after administration with a single oral dose（150,300,600 mg）were as follows：AUC0～t were（3.73±2.77）,（6.72±4.12）and（13.1±8.04）μg·h/mL;Cmax were（1.89±0.93）,（3.19±1.14）and（6.95±3.37）μg/mL;Tmax were（0.97±0.54）,（0.83±0.38）and（0.93±0.45）h;t1/2 were（0.92±0.26）,（0.94±0.14）and（0.98±0.15）h.The urinary amounts of cumulative recovery were（6.23±7.09）%,（4.69±4.32）% and（4.14±2.95）%. Conclusion The pharmacokinetics of faropenem by oral administration of 150 to 600 mg faropenem sodiumin tablets in human body nearly fits linear dynamic feature.