阿奇霉素分散片的人体药物动力学和生物等效性研究

Pharmacokinetics and Bioequivalence of Azithromycin Dispersible Tablets in Human

20名健康男性志愿者交叉口服两种国产阿奇霉素分散片的受试制剂和参比制剂500mg,以HPLC-MS法测定血浆中阿奇霉素的浓度,研究人体药物动力学参数和生物等效性。采用C_8柱,流动相为甲醇-0．02mol／L乙酸铵溶液(70:30), 受试制剂和参比制剂的C_(max)分别为(472．14±216．37)和(432．96±131．80)ng／ml t_(1／2)分别为(68．63±12．93)和(70．63± 15．61)h;T_(max)分别为(2．18±0．89)和(2．25±0．84)h; AUC_(o→144h)分别为(4268．52±1252．89)和(4370．32±807．82)ng·h·ml^(-1)。经方差分析和双单侧t检验,说明两片剂具有生物等效性,受试制剂的相对生物利用度为(97．1±22．7)％。

The pharmacokinetics and bioequivalence of azithromycin dispersible tablets were investigated in 20 healthy male volunteers, according to a randomized crossover design. The concentrations of azithromycin in plasma were determined by HPLC-MS method. A C8 column was used with the mobile phase of methanol-0.02mol/L ammonium acetate （70.30）. The pharmacokinetic parameters were Cmax （472.14 ± 216.37） and （432.96±131.80） ng/ml, t1/2 （68.63 ± 12.93） and （70.63 ±15.61） h, Tmax （2.18 ± 0.89） and （2.25 ± 0.84） h, AUCo→144h （4268.52 ± 1252.89） and （4370.32 ± 807.82） ng·ml^-1·h for test and reference tablets, respectively. The results of variance analysis and two-side t test showed that two products were bioequivalent. The relative bioavailability was （97.1 ± 22.7） %.