阿奇霉素干混悬剂在健康人体的药代动力学及生物等效性评价

Study on Pharmacokinetics and Bioequivalence of Azithromycin for Suspension in Healthy Volunteers

目的研究阿奇霉素干混悬剂在健康人体的药代动力学特征及其生物等效性。方法20名健康志愿受试者,采用标准二阶段交叉设计自身对照试验方法,单剂量口服阿奇霉素试验品和参比品500mg时,以液相色谱-质谱-质谱联用法测定服药后72h内不同时刻的血药浓度,计算主要药动学参数,并采用方差分析和双单侧t检验(1-2α)90%置信区间进行生物等效性评价。结果受试者分别口服阿奇霉素受试品和参比品后,其主要药动学参数Tmax分别为2.30±0.55、2.25±0.53h,Cmax分别为478.4±133.9、562.6±132.9ng.ml-1,T1/2分别为30.1±8.3、32.4±9.4h;用梯形法计算,AUC0-t分别为4 263±1 341、4511±918ng.h.ml-1,AUC0-∞分别为5 233±2 0735、426±1 011ng.h.ml-1。AUC0-t计算,阿奇霉素的相对生物利用度平均为(95.2±21.5)%。结论两种阿奇霉素制剂在健康志愿者体内具有生物等效性。

Aim To study the phannacokinetics and bioequivalence of Azithromycin for Suspension in healthy volunteers. Methods The concentration of Azithromycin for Suspension of 20 male subjects were determined after oral administration 500mg tested and referenced by liquid chromatographic - mass - mass spectrometric and caculated main pharmacokinetics parameters,analyses bioequivalence of two formulations by two one t test and （1-2α）90%. Results The main pharmacokinetics of tested and referenced were follows： T max were （2.30 ±0.55）h and （2.25 ± 0.53）h; Cmax were （478.4± 133.9）ng·ml^-1 and （562.6± 132.9）ng·ml^-1, T1/2 were （30.1 ± 8.3）h and （32.4 ± 9.4）h;AUC0-t were （4 263 ± 1 341 ） ng·ml^-1 and （4 511 ± 918） ng·ml^-1, respectively. The relative bioavailability of the test formulation was （95.2 ± 21.5） %. Conclusion The two kinds of Azithromycin were bioequivalent in healthy volunteers.