丙磺舒对大鼠体内头孢克罗药动学的影响

中国临床药理学与治疗学 ›› 2004, Vol. 9 ›› Issue (5): 523-526.

丙磺舒对大鼠体内头孢克罗药动学的影响

张秀红, 马张庆, 桂常青, 宋建国

皖南医学院药理学教研室, 芜湖241000, 安徽

收稿日期:2003-10-20 修回日期:2003-12-19 发布日期:2020-11-22

Effects of probenecid on pharmacokinetics of cefaclor in rats

ZHANG Xiu-Hong, MA Zhang-Qing, GUI Chang-Qing, SONG Jian-Guo

Department of Pharmacology, Wannan Medical College, Wuhu 241000, Anhui, China

Received:2003-10-20 Revised:2003-12-19 Published:2020-11-22
Contact: SONG Jian-Guo, male, professor, postgraduate tutor,engaged in chronopharmacology and mathematical pharmacology.Tel:0553-3832468-6264 Fax:0553-3811994 E-mail:zhxh66 @hotmail.com
About author:ZHANG Xiu-Hong, female, postgraduat e.

摘要/Abstract

摘要： 目的观察不同剂量丙磺舒对大鼠体内头孢克罗药动学的影响。方法大鼠24 只随机分成4组, Ⅰ 组:单用头孢克罗100 mg·kg^-1;Ⅱ组:头孢克罗100mg·kg^-1联用丙磺舒300 mg·kg^-1;Ⅲ组:头孢克罗100 mg·kg^-1联用丙磺舒600 mg·kg^-1;Ⅳ组:头孢克罗100 mg·kg^-1联用丙磺舒900 mg·kg^-1。各组动物灌胃给药后不同时间取血,HPLC 法测头孢克罗血药浓度,DAS 程序计算药动学参数。结果联用剂量在300 ~ 600 mg·kg^-1范围内, 随丙磺舒联用剂量增大, 头孢克罗的Cmax、AUC 增高而CL/F、V/F 减少;当丙磺舒联用剂量达900 mg·kg^-1时, 头孢克罗的C_max 反而降低, 而AUC、CL/F 则稳定于联用丙磺舒600 mg·kg^-1时的水平。结论丙磺舒可明显改变头孢克罗的药动学, 在本实验剂量范围内其影响程度与丙磺舒剂量有关, 随丙磺舒联用剂量增大, 头孢克罗的C_max 先升高后降低, 该现象可能与大剂量丙磺舒抑制头孢克罗的肠吸收有关。

关键词: 头孢克罗, 丙磺舒, 药物动力学, HPLC

Abstract: AIM: To investigate the effect of concurrent probenecid administration with different dosages on pharmacokinetics of cefaclor in rats. METHODS: Cefaclor (100 mg·kg^-1, ig) was given alone or in the presence of probenecid (300, 600 and 900 mg·kg^-1, ig) to rats.Serial blood samples were drawn according to the exact time schedule and concentrations of cefaclor were determined by HPLC method. RESULTS: Under the dosages of probenecid ranged from 300 to 600 mg·kg^-1, Cmax and AUC of cefaclor increased, while Vd/F and Cl/F of cefaclor decreased.However, when a still higher dosage (900 mg·kg^-1) of probenecid was used, Cmax of cefaclor decreased, while AUC, Vd F and Cl/F maintained at the levels of those with probenecid 600 mg·kg^-1. CONCLUSION: Probenecid can markedly alter pharmacokinetics of cefaclor and the influential magnitude for each parameter is dependent on the dose of probenecid used in the trial.The Cmax of cefaclor increases with proper dosage of probenecid, while decreases with over dose of probenecid, and this phenomenon may be related to the inhibition of cefaclor intestinal absorption attained with over dose of probenecid.

Key words: cefaclor, probenecid, pharmacokinetics, HPLC

中图分类号:

R969.1

张秀红, 马张庆, 桂常青, 宋建国. 丙磺舒对大鼠体内头孢克罗药动学的影响[J]. 中国临床药理学与治疗学, 2004, 9(5): 523-526.

ZHANG Xiu-Hong, MA Zhang-Qing, GUI Chang-Qing, SONG Jian-Guo. Effects of probenecid on pharmacokinetics of cefaclor in rats[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2004, 9(5): 523-526.

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