阿奇霉素颗粒剂在健康人体中的药代动力学和生物等效性

目的：研究阿奇霉素颗粒剂在健康中国人体内药动学和生物等效性。方法：采用双周期交叉试验设计,20名健康男性受试者随机交叉单剂量口服阿奇霉素颗粒剂试验制剂和参比制剂0.5g,以高效液相色谱-质谱联用法测定人血浆中阿奇霉素经时血药浓度,用DASVer2.0软件计算药动学参数,评价两制剂的生物等效性。结果：阿奇霉素颗粒剂试验制剂和参比制剂的主要药动学参数Cmax分别为（537.4±168.2）ng/ml和（540.6±169.0）ng/ml;tmax分别为（2.0±0.7）h和（1.9±0.7）h;t1/2分别为（31.3±11.6）h和（32.6±16.3）h;AUC0→72分别为（4736.7±2408.9）ng.h/ml和（4779.2±2405.2）ng.h/ml,AUC0→∞分别为（5578.6±2796.3）ng.h/ml和（5635.6±2594.1）ng.h/ml;试验制剂的AUC0→72、AUC0→∞、Cmax的90%置信区间分别为参比制剂相应参数的93.2%～104.4%、91.8%～103.0%和96.5%～102.2%。以AUC72计算试验制剂中阿奇霉素对参比制剂的相对生物利用度F,得（100.5±13.1）%。结论：经方差分析及双单侧t检验结果显示,试验制剂和参比制剂具有生物等效性。

Pharmacokinetics and bioequivalenee of Azithromycin Granules in healthy volunteers

Objective：To study the pharmacokinetics and bioequivalence of Azithromycin Granules in healthy volunteers. Methods：The plasma concentrations of azithromycin in 20 healthy male volunteers were determined by LC/MS/MS methods after being orally administered with single dose of 0.5 g Azithromycin Granules by randomized crossover way ; the pharmacokinetic parameters and the relative bioequivalence of the two preparations of azithromycin were calculated by DAS Ver 2.0 software. Results：The main pharmacokinetic parameters of azithromycin were as follows：Cmax were （537.4±168.2） ng/ml and （540.6±169.0） ng/ml;tmax were （2.0±0.7） h and （1.9±0.7） h;t1/2 were （31.3±11.6） h and （32.6±16.3） h;AUC0→72 were （4 736.7±2 408.9） ng.h/ml and（4 779.2±2 405.2） ng.h/ml; AUC0→∞ were （5 578.6±2 796.3） ng.h/ml and （5 635.6± 2 594.1） ng.h/ml for test preparation and reference preparation respectively. The 90% confindential interval of AUC0→72,AUC0→∞ and Cmax of test preparation were 93.2%-104.4%,91.8%-103.0% and 96.5%-102.2%,respectively. The relative bioavailability of azithromycin was （100.5±13.1）%. Conclusion：The results of the statistic analysis showes that Azithromycin Granules test preparation and reference preparation were bioequivalent.