阿奇霉素分散片人体药动学及生物等效性研究

目的研究阿奇霉素分散片健康人体的药动学与生物等效性。方法20名男性健康志愿者随机交叉口服阿奇霉素分散片受试制剂和参比制剂各500mg,采用高效液相色谱-质谱法（LC-MS）测定血药浓度。以DAS2.0软件计算其药动学参数,考察其生物等效性。结果受试制剂和参比制剂阿奇霉素AUC0-168分别为（8.98±1.74）μg·h·mL^-1和（8.75±1.60）μg·h·mL^-1,Cmax分别为（0.81±0.14）μg·mL^-1和（0.80±0.14）μg·mL^-1,t^1/2分别为（48.16±11.10）h和（51.1±7.60）h,Tmax分别为（1.80±0.86）h和（1.82±0.92）h,受试制剂相对于参比制剂的生物利用度为（103.4±20.2）%。结论阿奇霉素分散片受试制剂和参比制剂具有生物等效性。

Study on Pharmacokinetics and Bioequivalence of Azithromycin Dispersible Tablets in Healthy Volunteers

OBJETIVE To study the pharmacokinetics and bioequivalence of azithromycin dispersible tablets in healthy volunteers. METHODS A single oral dose of 500 mg test or reference formulations was given to 20 male healthy volunteers in a randomized cross-over design. The concentration of azithromycin in plasma was determined by HPLC-MS. Pharmacokinetic parameters and relative bioavailability were calculated by DAS 2.0 software. RESULTS The main pharmacokinetic parameters of test and reference azithromycin were as the followings: AUC_0-168 (8.98±1.74) mg·h·mL^-1 and (8.75±1.60) mg·h·mL^-1; C_max (0.81±0.14) mg·mL^-1 and (0.80±0.14) mg·h·mL^-1; t_1/2 (48.16±11.10) h and (51.1±7.60) h; Tmax (1.80±0.86) h and (1.82±0.92) h. The relative bioavailability of test to reference preparation was (103.4±20.2)%. CONCLUSION The test and reference formulations were bioequivalent.