慢性肾衰患者血液透析时司帕沙星的药物动力学

Effect of hemodialysis on pharmacokinetics of sparfIoxacin in the patients with chronic renal failure

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.

Aim To observe the effect of hemodialysis on pharmacokinetics of sparfloxacin in thepatients contracting chronic renal failure. Methods Sparfloxacin concentrations inserum and urine of hemodialysis and non-dialysis patients were measured with a highperformance liquid chromatography method after administration a single oral dose of 200mg sparfloxacin. The pharmacokinetic parameters were computed with the programPKBP-N1.Results The main pharmacokinetic parameters in hemodialysis group wereT1/2(ka) - (1. 25 ±0. 57) h, T1/2(β) = (11. 88±4. 13) h, Tpeak = (4. 18 ± 0. 78) h,Cmax = (0.80 ± 0. 17) mg· L-1 and AUC0-= (6. 90 ± 3. 25) mg·h·L-1, while innon-dialysis group were T1/ 2(ka) = (1. 12 ± 0. 42) h, T1/ 2(β) = (15. 93 ± 5. 20) h, Tpeak =(3. 88 ± 0. 75) h, Cmax = (0. 69 ± 0. 37) mg·L -1, AUC0-= (10.05 ± 4. 13) mg·h·L-l. The original sparfloxacin discharge rats in urine within 24 h were (8. 98 ± 3. 92) % and(10. 58 ± 5. 64) % separately. T1/2(β) and AUC in hemodialysis group were markedly lowerthan in non-dialysis group (P< 0. 05) .Conclusion The pharmacokinetics ofsparfloxacin in patients contracting chronic renal failure is not changed by hemodialysis.