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目的评价多剂量头孢他啶/他唑巴坦注射剂(3∶1)在中国健康人体的药代动力学。方法 10名健康男性受试者接受头孢他啶/他唑巴坦连续给药(1800/600 mg q12h,6 d),用高效液相色谱-紫外检测法测定血药浓度,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。多剂量给药血药浓度在第4 d达稳态,稳态后头孢他啶和他唑巴坦的Cmax分别为(135.28±25.46),(27.37±3.69)mg.L-1;Cmin分别(1.75±0.49),(0.02±0.26)mg.L-1;AUC0-t分别为(254.12±35.98),(36.26±11.26)mg.h.L-1;Css分别为(21.29±2.97),(3.16±1.03)mg.L-1。单次给予头孢他啶/他唑巴坦1800/600 mg和连续6 d给予头孢他啶/他唑巴坦1800/600 mg后,2组头孢他啶和他唑巴坦的Cmax、t1/2β、AUC0-t、AUC0-∞、CL/F、V/F均无显著性差异(P>0.05)。结论连续给予头孢他啶/他唑巴坦与单次给药相比在体内的消除过程也无明显改变,无体内蓄积作用。
Objective To evaluate the pharmacokinetics of multidose ceftazidime / tazobactam injection (3: 1) in Chinese healthy volunteers. Methods Ten healthy male subjects were given continuous ceftazidime / tazobactam (1800/600 mg q12h, 6 d), and plasma concentrations were determined by high performance liquid chromatography - ultraviolet detection. Pharmacokinetics were determined by DAS program Learning parameters. Results The plasma concentration-time curve conformed to the two-compartment model. The plasma concentration of multidose administration reached the steady state on the 4th day, and the Cmax of ceftazidime and tazobactam was (135.28 ± 25.46) and (27.37 ± 3.69) mg.L-1 respectively after steady state; the Cmin were (1.75 ± 0.21); AUC0-t was (254.12 ± 35.98) and (36.26 ± 11.26) mg.hL-1, respectively; Css was (21.29 ± 2.97) and (3.16 ± 1.03) mg.L-1. After a single dose of 1800/600 mg ceftazidime / tazobactam and 1800/600 mg ceftazidime / tazobactam for 6 consecutive days, Cmax, t1 / 2β, AUC0-t, AUC0 -∞, CL / F, V / F had no significant difference (P> 0.05). Conclusions Continuous ceftazidime / tazobactam treatment showed no significant change in vivo compared with single administration, and no accumulation was observed in vivo.