【作者】 朱燕； 肖永红； 吕媛； 魏敏吉； 张朴； 康子胜； 刘燕； 梁军； 张薇； 张曼； 李天云；

【Author】 Zhu yan,Xiao yonghong~*,Lu yuan,Wei minji,Zhang pu,Kang Zisheng Liu yan,Li tianyun Institute of Clinical Pharmacology,First Hospital,Peking University,Beijing 100191

【机构】 北京大学第一医院临床药理研究所；

【摘要】 目的研究注射用比阿培南在健康人群单次给药药代动力学特征,为临床用药提供参考。方法采用分层随机、三交叉、拉丁方设计、空腹给药的试验方法,在12名健康受试者（男女各半）中单次静脉滴注150mg、300mg、600mg比阿培南,HPLC法测定给药后不同时间点的血、尿药物浓度,DAS软件计算药代动力学参数。结果共12名受试者完成试验,结果显示静脉滴注比阿培南后药代动力学符合二室开放模型,受试者静脉点滴1 50mg,300mg,600mg后,比阿培南血药峰浓度(C_max)分别是8.49±1.02,16.31±1.83、34.51±3.74mg/L;消除半衰期(T_1/2β)分别为1.08±0.80;0.89±0.14;0.93±0.08h;药时曲线下面积AUC_（0-∞）分别13.83±2.36,29.23±5.03,61.23±8.75 mg/L*h;清除率（CL）分别是11.09±1.58,10.54±1.85,9.98±1.39L/h/kg。12小时尿排出率分别为61.31%,62.82%,62.79%。男女受试者药代动力学参数差异不明显。受试者对注射用比阿培南的耐受性良好。结论注射用比阿培南药代动力学符合二室开放模型,药代动力学参数与剂量呈线性相关,受试者耐受性良好。更多还原

【Abstract】 Objective To study the pharmacokinetic of Biapenem Injection in healthy volunteers and provide reference for clinical application.Methods 12 healthy volunteers were enrolled and a single dose of 150,300,600mg of biapenem was administered intravenously in Latin square design.The drug concentrations of Biapenem in plasma and in urine were determined by HPLC method.Phamarcokinetic parameters of biapenem were generated with DAS software.Results The plasma concentration-time curves of biapenem conformed to a 2-compartment pharmarcokinetic model.The plasma peak concentrations(C_max) of biapenem after single doses of 150,300 and 600mg intravenous administration were 8.49±1.02,16.31±1.83,34.51±3.74mg/L;the elimination half lives(T_1/2β) were 1.08±0.80,0.89±0.14,0.93±0.08h;the areas under the concentration-time curve(AUC_0-∞) were 13.83±2.36,29.23±5.03,61.23±8.75mg/L*h;and the tatol clearance（CLs） were 11.09±1.58,10.54±1.85,9.98±1.39L/h/kg,respectively.Urinary recoveries were 61.31%,62.82%,62.79%in 12h after drug administration,respectively.No gender difference were detected in the phamarcokinetic parameters.All subjects were well tolerance to the study medicine.Conclusion The plasma concentration-time curve of biapenem fits two compartment model in 12 healthy volunteers after a single dose（150,300 or 600mg） intravenous administration,the pharmacokinetic parameters proportionate linearly to the dosages.All the subjects are well-tolerant.更多还原