注射用头孢他啶/他唑巴坦(5∶1)在中国健康人体的单次给药的药代动力学

Pharmacokinetics of ceftazidime/tazobactam (5 ∶ 1) after single intravenous infusion administration in Chinese health volunteers

目的评价单剂量头孢他啶/他唑巴坦注射剂(5∶1)在中国健康人体的药代动力学。方法 11名健康男性受试者先后接受单方头孢他啶2000 mg、他唑巴坦400 mg和复方头孢他啶/他唑巴坦2000/400 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程序处理求药代动力学参数。结果血药浓度-时间曲线符合二房室模型。给药后主要药代动力学参数如下。单方和复方头孢他啶:C max分别为(127.45±18.60),(129.3±16.32)mg·L-1;t1/2β分别为(1.58±0.55),(1.583±0.31)h;AUC0-t分别为(238.23±0.69),(241.09±28.9)mg·h·L-1。单方和复方他唑巴坦:C max分别为(17.39±4.01),(18.73±2.64)mg·L-1;t1/2β分别为(0.91±0.46),(0.87±0.44)h;AUC0-t分别为(18.33±5.9),(18.48±3.25)mg·h·L-1。24 h尿药累积排泄率:单方和复方头孢他啶分别为(71.94±28.43)%,(70.04±22.53)%;单方和复方他唑巴坦分别为(68.52±25.2)%,(67.35±40.11)%。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 investigate pharmacokinetics of eeftazidime/ tazobactam （5：1 ） after single intravenous infusion administration in Chi-nese healthy volunteers. Methods Eleven healthy male volunteers re-ceived ceftazidime 2000 mg, tazobactam 400 mg and ceflazidime/ tazobactam 2000/400 mg. The concentrations of eeftazidime and tazobac-tam in serum and urine were assayed by HPLC - UV methods. The phar-macokinetic parameters of ceftazidime and tazobactam were caculated by DAS software. Results It was found that concentrations - time curves of ceftazidime and tazobactam were fitted to two compartment model. The main pharmacokinetic parameters were as follows： ceftazidime in single and combination preparations, Cmax were（ 127.45 ± 18.60）, （ 129.3 ± 16.32） mg·L^-1; t1/2βwere （1.58 ±0.55）, （1.583 ±0.31） h; AUC0-t, were （238. 23 ± 0. 69）, （241.09 ± 28.9） mg · h · L^-1. Tazobactam in single and combination preparations, Cmax were （ 17.39 ± 4.01 ）, （18.73 ±2. 64） mg · L^-1 ; t1/2β were （0. 91±0.46）, （0. 87 ± 0.44） h; AUC0-t,were （18.33 ±5.9）, （18.48 ±3.25） mg· h · L^-1. Urinary recovery rate of ceftazidime in single and combination prepara-tions were （71.94 ± 28.43 ） % and （70. 04 ± 22. 53 ） %, respectively.Urinary recovery rate of tazobactam in single and combination preparations were （68.52 ± 25.2 ） % and （ 67.35 ± 40. 11 ） %, respectively. Conclusion The results of single dose study showed that the combination of ceftazidime and tazobactam did not affect their respective disposition.