Bioequivalence study of brexprazole tablets in Chinese healthy subjects
10.13699/j.cnki.1001-6821.2023.23.026
- VernacularTitle:布瑞哌唑片在中国健康受试者的生物等效性研究
- Author:
Yi-Jing ZHU
1
;
Juan LIU
;
Xiao-Lin DU
;
Xiao-Lan YONG
Author Information
1. 成都新华医院Ⅰ期临床研究中心,四川成都 610066
- Keywords:
brepiprazole;
pharmacokinetics;
bioequivalence;
safety
- From:
The Chinese Journal of Clinical Pharmacology
2023;39(23):3464-3468
- CountryChina
- Language:Chinese
-
Abstract:
Objective To evaluate the bioequivalence and safety of brexpiprazole tablets(2 mg)in Chinese healthy volunteers under fasting/postprandial conditions.Methods A single-center,single-dose,randomized,open,two-sequence,two-period,and two-crossover design was used.Healthy volunteers were randomly divided into the fasting group and the postprandial group(34 cases in each group).A single oral dose(2 mg)of the test or reference formulation of brexpiprazole tablet was administered in fasting or postprandial state for per period.The concentration of brexpiprazole was determined by ultra-efficient liquid phase mass spectral tandem method.The pharmacokinetic parameters were calculated with Phoenix WinNolin software to analyze the bioequivalence of the two preparations.Results In the fasting test,the Cmax of the test or reference formulation of brexpiprazole tablets were(21.86±6.56)and(22.90±7.90)ng·mL-1,AUC0-t were(1 524.20±590.09)and(1 529.26±635.08)ng·mL-1·h,AUC0-∞ were(1 640.04±663.42)and(1 644.29±725.14)ng·mL-1·h.In the postprandial test,the Cmax of the test or reference formulation of brexpiprazole tablets were(21.98±5.84)and(22.77±5.95)ng·mL-1,AUC0-t were(1 726.08±698.90)and(1 772.18±608.30)ng·mL-1 h,and AUC0-∞ were(1 866.17±805.44)and(1 913.20±696.81)ng·mL-1·h.The 90％confidence intervals of the geometric mean ratios of Cmax,AUC0-t and AUC0-∞ between the test and the reference formulation completely falls between 80.00％-125.00％.There were no serious adverse events in this experiment,and all adverse events were level Ⅰ to Ⅲ adverse events.Conclusion The test and reference formulations of brexpiprazole tablets were bioequivalent,safe,and well tolerated in Chinese healthy people.
