【摘要】 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:C_max（3 476.0±855.2）,（3 632.6±1 011.3）ng/mL;T_max 1.50（0.25,4.00）,2.50（0.25,4.00）h; AUC_0-t（54 972.81±11 400.81）,（56 757.41±12 670.53）h·ng·mL^-1;AUC_0-∞（56 791.17±11 681.08）,（58 574.37±13 072.17）h·ng·mL^-1;T_1/2（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:C_max（3 744.3±819.2）,（3 569.1±653.8）ng/mL;T_max 1.50（0.50,4.00）,1.50（0.50,4.00）h; AUC_0-t（51 613.98±10 725.93）,（52 322.70±10 189.50）h·ng·mL^-1;AUC_0-∞（53 585.13±10 954.51）,（54 207.13±10 313.28）h·ng·mL^-1;T_1/2（14.47±3.71）,（14.53±3.04）h。空腹组和餐后组的C_max、AUC_0-t、AUC_0-∞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。更多还原

【Abstract】 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: C_max（3 476.0±855.2）,（3 632.6±1 011.3） ng/mL; T_max 1.50（0.25, 4.00）, 2.50（0.25, 4.00） h; AUC_0-t（54 972.81±11 400.81）,（56 757.41±12 670.53） h·ng·mL^-1; AUC_0-∞（56 791.17±11 681.08）,（58 574.37±13 072.17） h·ng·mL^-1; T_1/2（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: C_max（3 744.3±819.2）,（3 569.1±653.8） ng/mL; T_max 1.50（0.50, 4.00）, 1.50（0.50, 4.00） h; AUC_0-t（51 613.98±10 725.93）,（52 322.70±10 189.50） h·ng·mL^-1; AUC_0-∞（53 585.13±10 954.51）,（54 207.13±10 313.28） h·ng·mL^-1; T_1/2（14.47±3.71）,（14.53±3.04） h. The 90%CI of C_max, AUC_0-t, AUC_0-∞ 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.更多还原