阿奇霉素干混悬剂 颗粒剂和胶囊的人体药代动力学研究

目的使用高效液相色谱-质谱(HPLC-MS)联用法测定人血浆中阿奇霉素的浓度,并研究阿奇霉素干混悬剂、颗粒剂和胶囊在健康人体内的药代动力学情况。方法 20名健康男性志愿者单剂量口服500mg阿奇霉素后,采集不同时间点血样测定血药浓度。结果阿奇霉素的线性范围为2.71～1084μg/L,日内和日间相对标准偏差(RSD)均<5.0%。阿奇霉素干混悬剂主要药代动力学参数为:Cmax:(453±130)μg/L;tmax:(2.3±0.9)h;t1/2:(48±6)h;平均驻留时间(MRT):(53±8)h;曲线下面积(AUC)0-t:(4694±903)μg·h-·1L-1;AUC0-∞:(5118±919)μg·h-1·L-1。结论 3种剂型阿奇霉素的药代动力学参数的差异无统计学意义。

Pharmacokinetics of azithromycin suspension, granules and capsules in healthy Chinese

Objective To evaluate the concentration of Azithromycin in human plasma by HPLC-MS method and to study the pharmacokinetics of azithromycin suspension, granules and capsules in healthy volunteers. Methods We determined the concentration of azithromycin at various time points in 20 healthy males who took single dose of azithromycin at 500 mg. Results The linear range of azithromycin was between 2.71 txg/L and 1084 pLg/L. Both within-day and day-to-day precisions （RSD） were less than 5%. The main pharmacokinetic parameters of azithromycin suspension were as follows： ：Cmax：（453±130）μg/L;tmax：（2.3±0.9）h;t1/2：（48±6）h, MRT：（53±8）h,AUC0＋（4694±903）μg·h-1·L^-1,AUC0-∞：（5118±919）μg·h^-1·L^-1.. Conclusion There were no statistical significance of the main pharmacokinetic parameters of azithromycin granules, suspension and capsules.