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中国临床药理学与治疗学 ›› 2002, Vol. 7 ›› Issue (2): 130-133.

• 基础研究 • 上一篇    下一篇

不同剂量丙磺舒对头孢克罗药物动力学的影响

汪长生, 刘晓平, 马张庆, 宋建国   

  1. 皖南医学院药理教研室, 芜湖 241001
  • 收稿日期:2002-02-02 修回日期:2002-02-28 出版日期:2002-04-26 发布日期:2020-11-27
  • 通讯作者: 汪长生, 男, 硕士研究生。Tel:0553-3832468-6264 Email:wangchangsh@sina.com
  • 作者简介:宋建国, 男, 博士, 教授, 院长。

Influence of probenecid on pharmacokinetics of cefaclor

WANG Chang-Sheng, LIU Xiao-Ping, MA Zhang-Qing, SONG Jian-Guo   

  1. Department of Pharmacology, Wannan Medical College, Wuhu241001
  • Received:2002-02-02 Revised:2002-02-28 Online:2002-04-26 Published:2020-11-27

摘要: 目的: 观察不同剂量丙磺舒(Pro) 对头孢克罗(Cef) 药动学的影响, 为两者联用提供依据。 方法: 家兔 30 只随机分成 5 组;Cef 50 mg·kg-1 组, Cef50 mg·kg-1+Pro 50 mg·kg-1 组, Cef 50 mg·kg-1+Pro 100 mg·kg-1组, Cef 50 mg·kg-1+ Pro200 mg·kg-1组, Cef 25 mg·kg-1 +Pro 100 mg·kg-1组。灌胃给药后于不同时间股静脉取血,HPLC 法测定Cef 血药浓度, NDST 程序计算药动学参数。 结果: 在给予Cef 50 mg·kg-1 条件下, 随 Pro 联用剂量的增大, Cef 的 Cmax、AUC 增高而 Cl/F、V/F 减少;Cef 25 mg·kg-1 +Pro 100 mg·kg-1 组各参数(除 Cl/F 外)与Cef 50 mg·kg-1 组差异不显著。 结论: Pro 可明显改变 Cef 的药动学, 在实验剂量范围内其影响程度与丙 磺 舒 剂 量 有 关。 Cef 25 mg·kg-1联 用 Pro100 mg·kg-1 可产生 Cef 50 mg·kg-1 的血药水平。

关键词: 头孢克罗, 丙磺舒, 药物代谢动力学, HPLC

Abstract: AIM: To observe the effects of proben-e-cid of different doses on pharmacokinetics of cefaclor and to provide the basis of their co-adiministration. METHODS: 30 rabbits were randomly divided into 5 groups: Cef 50 mg·kg-1, Cef 50 mg·kg-1 +Pro 50 mg·kg-1, Cef 50 mg·kg-1 +Pro 100 mg·kg-1, Cef 50 mg·kg-1 + Pro 200 mg·kg-1, Cef 25 mg·kg-1 +Pro 100 mg·kg-1. The blood samples were drawn from thigh vein after IG and the concentrations of cefaclor were determined by HPLC. Pharmacokinetics parameters were calculated by NDST procedure.RESULTS: In groups with Cef 50 mg·kg-1, Cmax and AUC of cefaclor increased, and Vd/F and Cl/F decreased progressively with the adding probenecid. There was no significant difference between Cef 25 mg +Pro 100 mg and Cef 50 mg·kg-1 in each parameter except Cl/F.CONCLUSION: Probenecid can remarkably alter the pharmacokinetics of cefaclor and the magnitude of the effects of probenecid is dependent on its dose in this trial.Cef 25 mg·kg-1 with Pro 100 mg·kg-1 can reach the same blood concentration as Cef 50 mg· kg-1 alone.

Key words: cefaclor, probenecid, pharmacokinetics

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