阿奇霉素片的相对生物利用度和生物等效性

目的:考察阿奇霉素片人体相对生物利用度及生物等效性。方法:22名健康男性志愿者,采用交叉给药方案,分别单剂量口服20mg受试阿奇霉素片和参比阿奇霉素片,用液相色谱-串联质谱法测定血浆中阿奇霉素浓度,进行人体相对生物利用度和生物等效性评价。结果:单次口服20mg受试阿奇霉素片和参比阿奇霉素片后,达峰时间Tmax分别为(2.0±1.4)h和(1.8±0.6)h;峰值血药浓度Cmax分别为(584.27±258.93)ng/ml和(523.27±186.53)ng/ml;t1/2分别为(47.64±10.38)h和(51.96±12.49)h;药时曲线下面积采用梯形法计算,AUC0→t分别为(3532.26±1311.69)和(3500.10±1229.70)ng.h/ml,AUC0→∞分别为(3986.30±1443.53)ng.h/ml和(4015.14±1426.56)ng.h/ml。结论:国产阿奇霉素片的相对生物利用度为(104.3±27.8%),主要参数的双单侧t检验,结果显示两种制剂为生物等效制剂。

Study on relative bioavailability and bioequiavailability assessment of Azithromycin tablets

Objective To study the relative bioavailability and bioequiavailability of Azithromycin tablets. Method A single oral dose of 20mg test Azithromycin tablets and reference Azithromycin tablets was given to 22 volunteers in a randomized cross-over study. Azithromycin concentrations in plasma were determined with LC/MS/MS method. Results Tmax of test Azithromycin tablets and reference Azithromycin tablets were (2.0±1.4)h and (1.8±0.6)h respectively, Cmax were (584.27±258.93)ng/ml and (523.27±186.53)ng/ml, T_ 1/2 were (47.64±10.38)h and (51.96±12.49)h, AUC_ 0→t were (3532.26±1311.69)ng·h/ml and (3500.10±1229.70)ng·h/ml, and AUC_ 0→∞ were (3986.30±1443.52)ng·h/ml and (4015.14±1426.56)ng·h/ml. Conclusion There is no statistically significant difference between the two preparations in AUC values and the results demonstrate that the two preparations are bioquivalent.