克拉霉素颗粒剂人体相对生物利用度  

Relative bioavailability of clarithromycin granules in healthy volunteers

作　　者：马小亚[1] 王美纳[1] 王信隆 王玉虎[1] 梁维薇 芦燕青 

机构地区：[1]西安医科大学第二附属医院,陕西西安710004

出　　处：《中国医院药学杂志》2000年第12期712-714,共3页Chinese Journal of Hospital Pharmacy

摘　　要：目的 :研究克拉霉素颗粒剂在健康人体内的药动学和相对生物利用度。方法 :8名健康男性受试者 ,采用随机交叉试验设计 ,单剂量口服克拉霉素颗粒剂和片剂 5 0 0mg ,用微生物检定法测定血药浓度。经 3p97程序拟合 ,计算药动学参数。 结果 :克拉霉素颗粒剂和片剂的药 时曲线均符合二室模型 ,主要药动学参数 :t1/ 2 β分别为 (6 .9± 4.0 )h和 (7.9± 3.8)h ;tmax分别为 (1.4± 0 .3)h和 (1.4± 0 .4)h ;Cmax分别为 (2 .1± 0 .3)mg·L-1和 (2 .0± 0 .4)mg·L-1;AUC0→∞ 分别为 (11.6± 1.6 )h·mg·L-1和 (11.3± 1.4)h·mg·L-1。经统计学分析 ,两制剂的tmax、Cmax、AUC0→∞ 差异均无显著性 (P >0 .0 5 ) ,克拉霉素颗粒剂的相对生物利用度为 (10 4.1± 2 1.3) %。结论OBJECTIVE:To study the pharmacokinetics and relative bioavailability of clarithromycin granules.METHODS:A single oral dose of 500 mg clarithromycin granules and tablets were given to 8 healthy male volunteers in an open randomized crossover design. The clarithromycin concentrations in serum were determined by microbioassay. The pharmacokinetic parameters of clarithromycin were calculated with 3p97 program.RESULTS:The concentration time curves of clarithromycin granules and tablets were fitted to two compartment open model.The t 1/2β were (6.9±4.0) h and (7.9±3.8) h;the t max (1.4±0.3) h and (1.4±0.4) h;the C max (2.1±0.3) mg·L -1 and (2.0±0.4) mg·L -1 ; the AUC 0→∞ (11.6±1.6) h· mg·L -1 and (11.3±1.4) h·mg·L -1 ,respectively.There are no significant differences in pharmacokinetic parameters above between clarithromycin granules and tablets. The relative bioavailability of clarithromycin granules to the tablets was (104.1±21.3)%.CONCLUSIONS:The two formulations were bioequivalent. [

关 键 词：克拉霉素 药动学 生物利用度 微生物检定法 

分 类 号：R978.15[医药卫生—药品] R969.1[医药卫生—药学]