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目的评价多剂量头孢他啶/他唑巴坦注射剂(5∶1)在中国健康人体的药代动力学。方法 10名受试者接受了复方头孢他啶/他唑巴坦连续给药(2000/400 mg q12 h,6 d),用高效液相色谱-紫外检测法测定头孢他啶和他唑巴坦的血药浓度,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。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药代动力学参数如下。C max分别为(130.93±30.6),(21.89±7.73)mg·L-1;C min分别为(1.29±0.37),(0.09±0.28)mg·L-1;AUC0-t分别为(242.92±34.81),(21.52±6.49)mg·h·L-1;C ss分别为(20.24±2.90),(1.79±0.54)mg·L-1。单次给予头孢他啶/他唑巴坦2000/400 mg和连续6 d给予头孢他啶/他唑巴坦2000/400 mg,C max、t1/2β、AUC0-t、AUC0-∞、CL/F及V/F差异均无统计学意义(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无明显改变,无体内蓄积作用。
Objective To evaluate the pharmacokinetics of multidose ceftazidime / tazobactam injection (5: 1) in Chinese healthy volunteers. Methods Ten subjects received continuous ceftazidime / tazobactam (2000/400 mg q12 h, 6 d), and the plasma concentrations of ceftazidime and tazobactam were determined by high performance liquid chromatography - ultraviolet detection , Using the DAS program for pharmacokinetic parameters. Results The plasma concentration-time curve conformed to the two-compartment model. Multidose administration of plasma drug concentration reached steady state on the 4th day. The pharmacokinetic parameters of ceftazidime and tazobactam after steady state were as follows. Cmax were (130.93 ± 30.6) and (21.89 ± 7.73) mg · L-1, respectively; C min was (1.29 ± 0.37) and (0.09 ± 0.28) mg · L-1, respectively; AUC0-t was (242.92 ± 34.81), (21.52 ± 6.49) mg · h · L-1, respectively; Css was (20.24 ± 2.90) and (1.79 ± 0.54) mg · L-1, respectively. Ceftazidime / tazobactam 2000/400 mg and ceftazidime / tazobactam 2000/400 mg, Cmax, t1 / 2β, AUC0-t, AUC0- ∞, CL / F and V / F were no significant difference (P> 0.05). Conclusions Continuous ceftazidime / tazobactam treatment showed no significant change in vivo and no accumulation in vivo compared with single administration.