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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。
Objective To study the pharmacokinetics of biapenem (carbapenem antibiotics) for injection in healthy individuals. Methods A total of 12 healthy volunteers received a single intravenous infusion of biapenem 150,300,600 mg by stratified randomized, triple crossover, Latin square design and fasting drug delivery method. The blood and urine drug concentrations, DAS software calculates pharmacokinetic parameters. Results The pharmacokinetic parameters of biapenem 150, 300 and 600 mg were (8.49 ± 1.03), (16.31 ± 1.83) and (34.51 ± 3.74) mg.L-1, respectively 1.00 ± 0.00) h and t1 / 2β were (1.08 ± 0.80), (0.89 ± 0.14) and (0.93 ± 0.08) h, respectively; AUC0-t were (13.49 ± 2.29), (28.91 ± 4.92) and (60.85 ± 8.72 ) mg.L-1.h; CL were (11.09 ± 1.58), (10.54 ± 1.85), (9.98 ± 1.39) Lh-1.kg-1.12 h urinary excretion rates were 61.9%, 62.1% 62.8%. Conclusions The biapenem injection pharmacokinetics conforms to the two-compartment open model. The pharmacokinetic parameters are dose-dependently linear and the subjects are well tolerated.