【摘要】 目的研究注射用比阿培南(碳青霉烯类抗生素)在健康人群单次给药药代动力学。方法用分层随机、三交叉、拉丁方设计、空腹给药的试验方法,12名健康受试者单次静脉滴注比阿培南150,300,600 mg,HPLC法测定给药后血、尿药物浓度,DAS软件计算药代动力学参数。结果受试者静滴比阿培南150,300,600 mg后药代动力学参数如下,Cmax分别是(8.49±1.03),(16.31±1.83),(34.51±3.74)mg.L-1;Tmax均为(1.00±0.00)h;t1/2β分别为(1.08±0.80),(0.89±0.14),(0.93±0.08)h;AUC0-t分别(13.49±2.29),(28.91±4.92),(60.85±8.72)mg.L-1.h;CL分别是(11.09±1.58),(10.54±1.85),(9.98±1.39)L.h-1.kg-1。12 h尿排出率分别为61.9%,62.1%,62.8%。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 Twelve healthy volunteers were enrolled and a single dose of 150,300,600 mg of biapenem was administered intravenously in Latin square design.The drug concentrations of biapenem in plasma and in urine were determined by HPLC method.Pharmacokinetic parameters of biapenem were generated with DAS software.Results The plasma concentration-time curves of biapenem conformed to a 2-compartment pharmarcokinetic model.The main pharmacokinetics parameters of three different dosages(150,300,600 mg) were as follows:Cmax were(8.49±1.03),(16.31±1.83),(34.51±3.74)mg·L-1;Tmax were(1.00±0.00)h;t1/2β were(1.08±0.80),(0.89±0.14),(0.93±0.08)h;AUC0-t were(13.49±2.29),(28.91±4.92),(60.85±8.72) mg·L-1·h and CL were(11.09±1.58),(10.54±1.85),(9.98±1.39)L·h-1·kg-1,respectively.Urinary recoveries were 61.9%,62.1%,62.8% in 12 h after drug administration,respectively.Conclusion The plasma concentration-time curve of biapenem fits two compartment model,the pharmacokinetic parameters proportionate linearly to the dosages.All the subjects are well-tolerant.更多还原