国产罗红霉素胶囊的人体生物利用度和药代动力学

Bioavailability and pharmacoloinetics of domestic roxithromycin capsule

目的 以法国罗赛尔公司生产的罗力得片为参比制剂 ,比较国产罗红霉素胶囊的人体生物利用度和生物等效性。方法 选择 10名男性成年健康志愿者 ,用自身交叉对照试验方法 ,分别单剂量一次口服罗红霉素胶囊和罗力得片两种制剂 30 0mg ,血药浓度采用微生物法测定。罗红霉素的血药浓度 时间数据用 3p87程序处理得药代动力学参数。结果 口服国产和进口两种制剂的血药浓度 曲线符合二室模型 ,Cmax分别为 (7.5 9± 1.43)mg/L和(7.5 4± 0 .93)mg/L ;Tmax分别为 (1.45± 0 .6 1)h和 (1.32± 0 .42 )h ;T β分别为 (13.37± 2 .4)h和 (13.6 5± 1 0 6 )h ;AUC分别为每小时 (98.89± 14.85 )mg·L-1和 (98.2 8± 19.49)mg·L-1。国产胶囊与进口片剂比较相对生物利用度为10 0 6 2 %。结论 经方差分析表明两种制剂的药代动力学参数间无显著性差异 (P >0 .0 5 ) ,经双单侧t检验 ,国产罗红霉素胶囊生物利用度与进口罗力得片比 ,具有生物等效性。

Objective To compare the bioavailability of domestic roxithromycin capsule with those of France roxithromycin tablet.Methods A single oral dose of 300mg roxithromycin was given according to a crossover design in 10 healthy Chinese volunteers.Plasma concentration of roxithromycin was measured by bioassay method.The concentration time curver of roxithromycin was fitted to a two compartment open model by using 3P87 program.Results The pharmacokinetic parameter C max ,T max ,T 1/2 β and AUC 0～48 of domestic and imported roxithromycin were (7.59±1.43)mg·L -1 and (7.54±0.93)mg·L -1 ,(1.45±0.61)h and (1.32±0.42)h,(13.37±2.4)h and (13.65±1.06)h,(98.89±14.85)mg·L -1 ·h -1 and (98.28±19.49)mg·L -1 ·h -1 respectively.The relative bioavailability of domestic capsule was 100.62% as compared with imported tablet.Conclusion The result by two one sided test show that the two formulation of domestic and imported products are bioequivalent.