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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。
Objective To evaluate the quality consistency of domestic azithromycin enteric-coated capsules and imported azithromycin tablets. METHODS: A total of 24 healthy male subjects were given oral azithromycin 500 mg enteric-coated capsules (test drug) or 500 mg tablets (reference drug) once a day. The blood samples were taken periodically and the plasma concentrations were measured by LC-MS / MS Azithromycin in plasma concentration, using WinNolin 5.2 software to calculate pharmacokinetic parameters and bioequivalence. Results The main pharmacokinetic parameters of the test drug and the reference drug were as follows: Cmax were (385 ± 154) and (444 ± 155) ng · mL-1, respectively; tmax were (3.46 ± 1.52) and (2.63 ± 1.28) h and t1 / 2 were (65.30 ± 21.40) and (61.20 ± 13.50) h respectively; AUC0-t were (4130 ± 845) and (4210 ± 857) ng · h · mL-1, respectively. The 90% confidence intervals of the cmax, AUC0-t and AUC0-∞ ratios after logarithmic transformation were 71.98% -100.24%, 90.10% -106.24% and 91.73% -107.18%, respectively. Conclusion The two azithromycin drugs are bioequivalent in Chinese healthy male subjects.