盐酸莫西沙星片在中国健康受试者的生物等效性研究

目的：研究空腹及餐后单剂量口服盐酸莫西沙星片的药代动力学特征，并以Bayer Pharma AG生产的盐酸莫西沙星片作为参比制剂，比较二者的药动学参数，评价两制剂的人体生物等效性。方法：采用单中心、随机、开放、两周期、自身交叉的设计，空腹和餐后给药生物等效性研究各纳入23例健康受试者，每周期单次口服受试制剂或参比制剂0.4 g，采取HPLC-MS/MS法测定给药后不同时间点莫西沙星的血药浓度，计算主要药代动力学参数，评价受试制剂相对于参比制剂的相对生物利用度及生物等效性。结果：空腹组受试者服用受试制剂T和参比制剂R后，莫西沙星的主要药代动力学参数为：Cmax（3 476.0±855.2），（3 632.6±1 011.3）ng/mL；Tmax 1.50（0.25，4.00），2.50（0.25，4.00）h；AUC0-t（54 972.81±11 400.81），（56 757.41±12 670.53）h·ng·mL-1；AUC0-∞（56 791.17±11 681.08），（58 574.37±13 072.17）h·ng·mL-1；T1/2（14.13±2.40），（13.85±2.44）h。餐后组受试者服用受试制剂T和参比制剂R后，盐酸莫西沙星的主要药代动力学参数为：Cmax（3 744.3±819.2），（3 569.1±653.8）ng/mL；Tmax 1.50（0.50，4.00），1.50（0.50，4.00）h；AUC0-t （51 613.98±10 725.93），（52 322.70±10 189.50）h·ng·mL-1；AUC0-∞（53 585.13±10 954.51），（54 207.13±10 313.28）h·ng·mL-1；T1/2（14.47±3.71），（14.53±3.04）h。空腹组和餐后组的Cmax、AUC0-t、AUC0-∞几何均数比值90%CI均落在80.00%～125.00%之间。结论：空腹和餐后状态下受试制剂T与参比制剂R（拜复乐）具有生物等效性且安全性良好。

Bioequivalence of moxifloxacin hydrochloride tablets in healthy Chinese subjects

AIM: To study the pharmacokinetic characteristics of single-dose oral moxifloxacin hydrochloride tablets under fasting and fed conditions, and use moxifloxacin hydrochloride tablets produced by Bayer Pharma AG as a reference to compare the pharmacokinetic parameters of the two preparations, and evaluate the human bioequivalence of the two preparations. METHODS: A single-center, randomized, open, two-period, and self-crossover design was adopted to conduct a fasting and fed bioequivalence study of 23 healthy subjects each. The 0.4 g dose preparations were taken orally per cycle on fasting or fed administration. The plasma concentrations of moxifloxacin at different times after administration were determined by HPLC-MS/MS. The main pharmacokinetic parameters were calculated, and the bioavailability of the test preparation relative to the reference preparation was evaluated. RESULTS: After subjects in the fasting group took the test preparation T and the reference preparation R, the main pharmacokinetic parameters of moxifloxacin hydrochloride were: Cmax (3 476.0±855.2), (3 632.6±1 011.3) ng/mL; Tmax 1.50 (0.25, 4.00), 2.50 (0.25, 4.00) h; AUC0-t (54 972.81±11 400.81), (56 757.41±12 670.53) h·ng·mL-1; AUC0-∞ (56 791.17±11 681.08), (58 574.37±13 072.17) h·ng·mL-1; T1/2 (14.13±2.40), (13.85±2.44) h. After the subjects in the fed group took the test parameter T and the reference parameter R, the main pharmacokinetic parameters of moxifloxacin hydrochloride were: Cmax (3 744.3±819.2), (3 569.1±653.8) ng/mL; Tmax 1.50 (0.50, 4.00), 1.50 (0.50, 4.00) h; AUC0-t (51 613.98±10 725.93), (52 322.70±10 189.50) h·ng·mL-1; AUC0-∞ (53 585.13±10 954.51), (54 207.13±10 313.28) h·ng·mL-1; T1/2 (14.47±3.71), (14.53±3.04) h. The 90%CI of Cmax, AUC0-t, AUC0-∞ geometric mean ratios of the fasting group and the fed group all fell between 80.00%-125.00%. CONCLUSION: The test preparation T and the reference preparation R under fasting and fed conditions are bioequivalent and safe.