地红霉素片的人体药代动力学及生物利用度研究

目的　考察国产与进口地红霉素片的药代动力学及生物等效性。方法　采用随机单剂二交叉试验设计,18名健康男性志愿者单剂口服国产与进口地红霉素片 75 0mg,微生物法测定地红霉素血浓度。对二种制剂的主要药代动力学参数进行方差分析、双向单侧t检验,评价试验制剂与参比制剂的生物等效性。结果　国产和进口地红霉素片主要药代动力学参数t1/2ke分别为 19 77± 4 5 1h和 18 5 7± 3 39h,Tpeak分别为 3 89± 0 76h和 3 83± 0 5 1h,Cmax分别为 1 6 12± 0 176 μg·ml-1和1 6 85± 0 10 8μg·ml-1,AUC0～ 96h分别为 11 4 0± 1 88μg·ml-1·h和 11 0 5± 1 84 μg·ml-1·h,AUC0～∞ 分别为 12 14± 2 11μg·ml-1·h和 11 6 6± 1 88μg·ml-1·h,国产地红霉素片相对生物利用度F为 10 3 79%± 10 5 2 %。结论　国产与进口地红霉素片为生物等效制剂。

Study on pharmacokinetics and bioavailability of Dirithromycin Tablets with microbiological assay

Objective To study the pharmacokinetics and bioequivalence of domestic Dirithromycin Tablets and the imported ones.Methods A randomized,two-way crossover and open design were adopted.18 healthy male volunteers were randomly divided into two groups.Single oral dose(750mg) of domestic and imported Dirithromycin Tablets were given respectively.Drug levels in plasma were determined by microbiological assay.The parameters were valuated by analysis of variance and two one-side t-test.Results The parameters of domestic and imported Dirithromycin Tablets were as the follows respectively:t 1/2ke(19.77±4.51) and (18.57±3.39) h,T peak(3.89±0.76)and(3.83±0.51)h,C max(1.612±0.176) and (1.685±0.108) μg·ml -1,AUC 0～96h(11.40±1.88)and (11.05±1.84)μg·ml -1·h,AUC 0～∞(12.14±2.11) and (11.66±1.88)μg·ml -1·h.The relative bioavailues of domestic to imported tablets was (103.79±10.52)%.Conlusion The results demonstrated that the two preparations were bioequivalent.