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中国临床药理学与治疗学 ›› 1999, Vol. 4 ›› Issue (2): 108-111.

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肾功能异常患者司帕沙星的药代动力学

梁竹, 张颖伟, 潘菡清, 张爱萍, 袁成   

  1. 解放军济南军区总医院, 济南 250031
  • 收稿日期:1999-04-05 出版日期:1999-06-26 发布日期:2020-12-04
  • 作者简介:梁竹,女,37岁,主管药师,主要从事医院临床药学工作;袁成,男,37岁,副主任药师,主要从事抗菌药物和抗癌药物临床药理学工作

Pharmacokinetics of sparfloxacin in the patients with abnormal kidney function

LIANG Zhu, ZHANG Ying-Wei, PAN Han-Qing, ZHANG Ai-Ping, YUAN Cheng   

  1. General Hospital of Jinan Military Region of The PLA, Jinan 250031
  • Received:1999-04-05 Online:1999-06-26 Published:2020-12-04

摘要: 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24 h 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24 h 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。

关键词: 司帕沙星, 药代动力学, 肾功能, 高效液相色谱法

Abstract: Aim To observe pharmaco kinetics of sparfloxacin in the patients with abnormal kidney function.Methods Sparfloxacin concent ration in serum and urine of ten patients were measured by a reversed phase high performance liquid chromatography method after having a single dose and multiple dose of 200 mg sparfloxacin tablet.The Pharmacokinetics parameters were computed with program PKBP-N1.Results The main pharmacokinetics parameters at single dose of sparfloxacin were 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 and AUC0-∞=(11.25±2.13)mg·h·L-1, while at multiple dose were 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 and AUC0-∞=(13.34±2.25)mg·h·L-1.The discharge rate in 24h of original sparfloxacin in urine were (10.58±1.47)% and (11.08±1.94)% separately.Cmax and AUC in multiple dose were marked higher than in single dose(P<0.05).The retainfactor was 1.19. Conclusion The pharmacokinetics parameters of sparfloxacin are not signi ficantly changed in patients with middle-abnormal kidney function had not change.

Key words: sparfloxacin, pharmaco kinetics, kidney function, high performance liquid chromatography

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