克拉霉素分散片在健康人体内的相对生物利用度

Relative bioavailability of clarithromycin in healthy volunteers

目的 :研究克拉霉素分散片在健康人体内的相对生物利用度 ,评价其生物等效性。方法 :采用微生物法测定 9名受试者单剂量交叉口服 5 0 0mg克拉霉素分散片和片剂后不同时间血清中药物浓度 ,用 3P87程序软件处理血药浓度 时间数据。结果 :2制剂体内过程均符合一室模型 ,Cmax分别为 (3.0 9± 0 .2 9)mg·L-1和 (2 .98± 0 .37)mg·L-1;Tmax分别为 (1 .37± 0 .35 )h和 (1 .5 6± 0 .42 )h ;T1/ 2 分别为 (4.0 7± 0 .92 )h和 (4.0 9± 0 .71 )h ;AUC为 (2 2 .6± 3.6 )mg·h·L-1和 (2 3.0 0± 3.90 )mg·h·L-1,被试制剂的相对生物利用度为 (98.7± 1 0 .9) % (82 .5 %～ 1 1 7.4% )。结论 :2种制剂具有生物等效性。

Aim:To study the relative bioavailability of clarithromycin disperse tablet. Methods: The clarithromycin concentration in serum were determined by microbiology method after a single oral dose of clarithromycin disperse tablet and clarithromycin tablet were respectively given to 9 volunteers in an open randomized cross over test. Data of serum level time were processed with 3P87 software. Results:The concentration time curves of clarithromycin disperse tablet and tablet fitted to one compartment open model. The C max was (3.09±0.29) mg·L -1 and (2.98±0.37) mg·L -1 , T max was (1.37±0.35) h and (1.56± 0.42 ) h, T 1/2 was ( 4.07±0.92) h and (4.09±0.71) h, AUC was (22.6±3.6) mg·h·L -1 and (23.0±3.90) mg·h·L 1 of clarithromycin disperse tablet and clarithromycin tablet, respectively. The pharmacokinetic parameters obtained from our studies showed no significant difference between two formulations. Compared with reference formulation, the relative bioavailability was (98.7±10.9)%(82.5%～117.4%)of clarithromycin disperse tablet. Conclusion: The results suggest that the two formulations were bioequivalent.