Pharmacokinetics and bioequivalence 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.