【摘要】 目的 研究克拉霉素胶囊在健康人体的药动学及相对生物利用度。方法 20名健康受试者随机交叉单剂量口服克拉霉素胶囊被试制剂和标准参比制剂500mg，采用微生物法测定不同时间的血清中药物浓度。结果 两制剂的体内过程均符合—房室开放模型，其主要药动学参数，达峰时间Tmax分别为(1.93±0.18)h和(1.90±0.21)h，峰浓度Cmax分别为(2.55±0.47)mg/L和(2.61±0.57)mg/L，消除半衰期T1/2ke分别为(5.63±0.90) h和(5.61±0.79) h，AUCt0分别为(20.99±4.01)mg/h·L和(21.61±4.84) mg/h·L，AUC∞0分别为(22.17±3.65)mg/h·L和(23.22±4.83) mg/h·L，被试制剂的相对生物利用度Ft0为(99.88±21.92)%，F∞0为(97.98±20.15)%。结论 对两制剂间的AUCt0、AUC∞0、Cmax、Tmax等进行双向单侧t检验，证明两种制剂具有生物等效性。

    【关键词】 克拉霉素； 药动学；生物利用度；生物等效性

    Relative bioavailability and pharmacokinetics of clarithromycin in healthy volunteers.

    GUO Yu-zhong, JIA Lin-jing, ZHANG Li-rong,et al. Department of Clinical Pharmacology, Zhengzhou University, Zhengzhou 450052

    【Abstract】 Objective To study the pharmacokinetics and relative bioavailability of clarithromycin in healthy volunteers. Methods The serum concentrations of clarithromycin of two formulations were determined in 20 healthy volunteers after an oral dose of 500 mg in crossways. The serum were collected at various periods after oral administration. The serum concentrations of clarithromycin were determined by microbiological method. Results The concentration-time curves of clarithromycin were fitted to the one-compartment open model. The Cmax values were(2.55±0.47)mg/L and (2.61±0.57) mg/L ......