【摘要】 目的评价国产阿奇霉素肠溶胶囊与进口阿奇霉素片剂的质量一致性。方法双周期、随机交叉试验设计,24名健康男性受试者单次口服阿奇霉素肠溶胶囊(试验药)或者片剂(参比药)500 mg,定时采集血样,用LC-MS/MS测定血浆中阿奇霉素的血药浓度,用WinNolin 5.2软件计算药代动力学参数并进行生物等效性评价。结果试验药与参比药的主要药代动力学参数如下,Cmax分别为(385±154),(444±155)ng·mL-1;tmax分别为(3.46±1.52),(2.63±1.28)h;t1/2分别为(65.30±21.40),(61.20±13.50)h;AUC0-t分别为(4130±845),(4210±857)ng·h·mL-1。对数变换后cmax、AUC0-t和AUC0-∞比值的90%可信区间分别为71.98%~100.24%,90.10%~106.24%和91.73%~107.18%。结论 2种阿奇霉素药在中国健康男性受试者体内具有生物等效性。更多还原

【Abstract】 Objective To evaluate the quality consistency of enteric-coated capsule with imported tablet of azithromycin by bioequivalence method.Methods A single oral dose 500 mg of test or reference azithromycin formulations were given to 24 healthy male subjects according to an open randomized crossover design.The blood samples were collected according to the schedule after the administration and the concentrations of azithromycin in plasma were determined by LC- MS /MS method.The pharmacokinetic parameters were calculated and the bioequivalence was evaluated by WinNolin 5.2.Results The main pharmacokinetic parameters of the test and reference preparations were as follows:Cmaxwere(385 ± 154),(444 ± 155) ng · mL- 1;tmaxwere(3.46 ±1.52),(2.63 ± 1.28) h;t1 /2were(65.30 ± 21.40),(61.20 ± 13.50)h;AUC0- twere(4130 ± 845),(4210 ± 857) ng·h·mL- 1.The 90%confidential interval of log- transformed ratios of Cmax,AUC0- tand AUC0- ∞of tested formulation were 71.98%- 100.24%,90.10%-106.24% and 91.73%- 107.18% respectively.Conclusion The two preparations of azithromycin were bioequivalent in Chinese healthy male volunteers.更多还原