中国志愿者口服克拉霉素片剂的药代动力学与相对生物利用度研究

健康志愿者 9名采用三交叉设计分别口服 50 0 mg国产西安制药厂克拉霉素片剂 A,丽珠制药厂克拉霉素片剂 B(2 50 mg/片 )及进口克拉霉素片 (KL ACID,2 50 mg/片 )。克拉霉素的血药浓度用微生物法进行测定。这三种制剂血药药浓度 -时间过程十分相似 ,符合开放二室模型。片剂 A、B与 KAL CID的药动学参数如下 :Tmax分别为 (2 .0 6± 0 .3 0 )、(2 .11± 0 .42 )及 (1.89±0 .3 3 ) h;Cmax分别为 (2 .47± 0 .3 0 )、(2 .63± 0 .2 5)及 (2 .64± 0 .3 3 ) mg/ L;AUC分别为 (2 1.50± 3 .53 )、(19.10± 2 .3 9)及 (19.92±2 .63 ) mg· h/ L。以 KL ACD作为参考标准 (生物利用度为 10 0 % ) ,A、B片剂的相对生物利用度分别为 10 7.9%与 95.9%。本试验的药动学参数与文献报道日本志愿者相仿 ,但与西方志愿者相比存在很大差异 ,值得进一步研究

Studies on the pharmacokietics and relative biovailability of clarithromycin tablets in healthy Chinese volunteers

The pharmacokinetics of domestic clarithromycin tablet A (Xian Pharmaceuticals,250mg/tab), B (Lizhu Pharmaceutical Factory, 250mg/tab), and Italy-made clarithromycin (KLACID,250mg/tab) were determined after triple cross over administration 500mg orally in 9 healthy Chinese volunteers. The serum drug concentrations were measured by microbiological assay. The serum drug course of tablet A, B and KLACID were very similar and could be best described by an open two compartment model.The main pharmacokinetics parameters of A, B and KLACID were as follows: Tmax= (2. 06±0. 30), (2. 11 ±0.42) and (1.89±0. 33)h; Cmax= (2.47±0. 30), (2.63±0. 25) and (2.64±0. 33)mg/L; AUC = (21.50±were 107.9% and 95.9% compared with KLACID (100%, as reference standard). The Cmax and AUC data presented here were twice higher than that of the western volunteers, but generally in agreement with that of the Japanese volunteers. Such a big difference between eastern and western volunteers were worthy to be investigated.