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目的评价单剂量头孢他啶/他唑巴坦注射剂(3∶1)在中国健康人体的药代动力学。方法 12名健康男性受试者先后接受单方头孢他啶1800 mg、他唑巴坦600 mg和复方头孢他啶/他唑巴坦1800/600 mg,用高效液相色谱-紫外检测法测定血药浓度、尿液浓度,用DAS程序求药代动力学参数。结果血药浓度-时间曲线符合二房室模型。主要药代动力学参数分别如下:给药后单方和复方头孢他啶的Cmax为(130.64±12.05),(136.03±15.27)mg.L-1;t1/2β为(1.50±0.25),(1.36±0.62)h;AUC0-t为(271.26±44.23),(285.36±42.87)mg.h.L-1。单方和复方他唑巴坦的Cmax为(23.72±8.06),(24.52±6.86)mg.L-1;t1/2β为(0.85±0.36),(0.89±0.45)h;AUC0-t为(28.06±12.18),(30.41±13.74)mg.h.L-1。单方和复方头孢他啶24 h累积排泄率分别为(73.8±18.5)%和(79.0±23.0)%;单方和复方他唑巴坦24 h尿药累积排泄率分别为(66.1±27.0)%和(66.2±36.5)%。结论头孢他啶与他唑巴坦两药联合应用,并不影响它们各自的体内过程。
Objective To evaluate the pharmacokinetics of single dose ceftazidime / tazobactam injections (3: 1) in Chinese healthy volunteers. Methods Twelve healthy male subjects received ceftazidime 1800 mg, tazobactam 600 mg, and ceftazidime / tazobactam 1800/600 mg sequentially. Plasma concentrations were determined by high performance liquid chromatography - ultraviolet detection. Urine Concentration, pharmacokinetic parameters were determined using the DAS program. Results The plasma concentration-time curve conformed to the two-compartment model. The main pharmacokinetic parameters were as follows: Cmax (130.64 ± 12.05), (136.03 ± 15.27) mg.L-1 for monotherapy and compound ceftazidime after administration and t1 (1.50 ± 0.25) and (1.36 ± 0.62 ) h; AUC0-t was (271.26 ± 44.23), (285.36 ± 42.87) mg.hL-1. The Cmax for unilateral and tazobactam was (23.72 ± 8.06) and (24.52 ± 6.86) mg.L-1, respectively. The t1 / 2β was (0.85 ± 0.36) and (0.89 ± 0.45) ± 12.18), (30.41 ± 13.74) mg.hL-1. The cumulative excretion rates of monotherapy and compound ceftazidime for 24 h were (73.8 ± 18.5)% and (79.0 ± 23.0)%, respectively. The cumulative urinary excretion rates of monotherapy and compound tazobactam for 24 h were (66.1 ± 27.0)% and ± 36.5)%. Conclusion Ceftazidime combined with tazobactam did not affect their respective in vivo processes.