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目的 观察司帕沙星在慢性肾衰患者血液透析时的药物动力学特征.方法 用高效液相色谱法测定透析和非透析住院患者单剂量口服司帕沙星后血清和尿药物浓度,并计算药物动力学参数.结果 经PKNP-N_1药代动力学软件摸拟和计算,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:透析时T_(1/2(ka))=(1.25±0.57)h,T_(1/2β)=(11.88±4.13)h,T_(peak)=(4.18±0.78)h,C_(max)=(0.80±0.17)mg·L~(-1),AUC_(0~∞)=(6.90±3.25)mg·h·L~(-1)尿中24h原形药物排除率为(8.98±3.92)%;未透析时T_(1/2(ka))=(1.12±0.42)h,T_(1/2β)=(15．93±5．20)h,T_(peak)=(3.88±0.75)h,C_(max)=(0.69±0.37)mg·L~(-1),AUC_(0~∞)=(10.05±4.13)mg·h·L~(-1),尿中24h原形药物排出率为(10.58±5.64)%.结论 司帕沙星在慢性肾衰患者血液透析时消除加快.
Objective To investigate the pharmacokinetics of sparfloxacin in hemodialysis patients with chronic renal failure.Methods Serum and urinary drug concentrations of sparfloxacin in dialysis and non-dialysis inpatients were determined by high performance liquid chromatography Pharmacokinetic parameters.Results Pharmacokinetics of sparfloxacin was in accordance with the first-order absorption two-compartment open model by PKNP-N 1 pharmacokinetic software. The main pharmacokinetic parameters were T 1/2 (ka) = (1.25 ± 0.57) h, T 1 / 2β = 11.88 ± 4.13 h, T peak = 4.18 ± 0.78 h, C max = 0.80 ± 0.17 mg · (8.98 ± 3.92)% in urine and T_ (1) of untreated dialysis group at L ~ (-1) and AUC_ (0 ~ ∞) = 6.90 ± 3.25 mg · h · L -1 / (Ka) = (1.12 ± 0.42) h, T 1 / 2β = 15.93 ± 5.20 h, T peak = 3.88 ± 0.75 h, C max = 0.69 ± 0.37) mg · L -1, AUC 0 ~ ∞ = 10.05 ± 4.13 mg · h · L -1, and the urinary excretion rate of prototype drug in 24h was (10.58 ± 5.64)% Conclusion Sparfloxacin is expedited in hemodialysis patients with chronic renal failure.