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目的观察司帕沙星在肾功能异常患者体内的药代动力学特征。方法用高效液相色谱法测定10例住院患者单剂量和多剂量口服司帕沙星后血清和尿药物浓度,并计算药代动力学参数。结果经PKBP -N1 药代动力学软件模拟和计算,司帕沙星的药物动力学符合一级吸收二室开放模型,主要药动学参数 :单剂量T1/2(ka)=(1.02±0.22)h,T1/2(β)=(15.73±3.20)h,Tpeak=(3.88±0.75)h,Cmax =(0.59±0.17)mg·L-1,AUC0 -∞=(11.25±2.13)mg·h·L -1,尿中24h原形药物排除率为(10.58±1.47) %;多剂量T1/2(ka) =(1.25±0.27)h,T1/2(β)=(16.90±4.13)h,Tpeak=(4.18±0.78)h,Cmax =(0.79±0.21)mg·L-1,AUC0～∞=(13.34±2.25)mg·h·L-1,尿中24h原形药物排出率为(11.08±1.94) %。多剂量Cmax 和AUC明显高于单剂量(P<0.05),蓄积因子为1.19。结论中度肾功能异常不改变司帕沙星的药代动力学参数。
Objective To investigate the pharmacokinetics of sparfloxacin in patients with renal dysfunction. Methods Serum and urinary concentrations of single and multiple doses of sparfloxacin in 10 hospitalized patients were determined by high performance liquid chromatography (HPLC). Pharmacokinetic parameters were calculated. Results Pharmacokinetics of sparfloxacin was simulated and calculated by PKBP-N1 pharmacokinetic software. The pharmacokinetics of sparfloxacin was in accordance with the two-compartment open model of primary absorption. The main pharmacokinetic parameters were: single dose T1 / 2 (ka) = (1.02 ± 0.22 ), Tmax = (3.88 ± 0.75) h, Cmax = (0.59 ± 0.17) mg · L-1 and AUC0 -∞ = (11.25 ± 2.13) mg · h · L -1, urinary 24h prototype drug exclusion rate was (10.58 ± 1.47)%; multiple dose T1 / 2 (ka) = (1.25 ± 0.27) h and T1 / 2 (β) = (16.90 ± 4.13) h , Tpeak = (4.18 ± 0.78) h, Cmax = (0.79 ± 0.21) mg · L-1 and AUC0 ~ ∞ = (13.34 ± 2.25) mg · h · L-1 respectively. ± 1.94)%. Cmax and AUC of multiple doses were significantly higher than those of single dose (P <0.05), and accumulation factor was 1.19. Conclusions The moderate renal dysfunction does not change the pharmacokinetic parameters of sparfloxacin.