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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 2 4只随机分成 4组 ,Ⅰ组 :单用头孢克罗 10 0mg·kg-1;Ⅱ组 :头孢克罗 10 0mg·kg-1联用丙磺舒 30 0mg·kg-1;Ⅲ组 :头孢克罗 10 0mg·kg-1联用丙磺舒 6 0 0mg·kg-1;Ⅳ组 :头孢克罗 10 0mg·kg-1联用丙磺舒 90 0mg·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 30 0～ 6 0 0mg·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 90 0mg·kg-1时 ,头孢克罗的Cmax反而降低 ,而AUC、CL F则稳定于联用丙磺舒6 0 0mg·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Cmax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。
Objective: To observe the effects of different doses of probenecid on the kinetics of cefaclor in rats. METHODS: Twenty-four rats were randomly divided into 4 groups: group Ⅰ: cefaclor 10 mg · kg-1 alone; group Ⅱ: cefaclor 10 mg · kg-1 with probenecid 30 0 mg · kg-1 ; Group Ⅲ: cefaclor 100 mg · kg-1 with probenecid 600 mg · kg-1; group Ⅳ: cefaclor 100 mg · kg-1 probenecid 90 0 mg · kg-1. Blood samples were taken from the rats in different groups at different times after gavage, and the plasma concentrations of cefaclor were determined by HPLC. The pharmacokinetic parameters were calculated by DAS program. Results: The combination dose of 300 ~ 600mg · kg-1, with dose of probenecid increased, cefaclor Cmax, AUC increased CL F, VF decreased; when probenecid combined Cefploxacol reduced Cmax, but AUC and CLF were stable at the level of 600 mg · kg-1 when probe dose was 90 mg · kg-1. Conclusion: Probenecid can significantly change the pharmacokinetics of cefaclor, the extent of the impact of this test dose and probenecid dose, with probenecid combined with increased doses, cefaclor Cmax first increased After the reduction, the phenomenon may be high dose probenecid inhibit cefaclor intestinal absorption related.