Pharmacokinetics and bioequivalence of rivaroxaban tablet in Chi-nese healthy subjects
10.12092/j.issn.1009-2501.2024.11.012
- VernacularTitle:利伐沙班片在中国健康受试者中的药动学及生物等效性评价
- Author:
Ran XIE
1
;
Lu CHENG
;
Shuang ZHOU
;
Xueyuan ZHANG
;
Xiaoru WANG
;
Xia ZHAO
;
Xu HE
;
Nan ZHAO
;
Bo JIA
;
Yimin CUI
Author Information
1. 北京大学第一医院药学部;北京大学第一医院药物临床试验机构,北京 100034
- Publication Type:Journal Article
- Keywords:
rivaroxaban;
bioequivalence;
narrow-window drugs
- From:
Chinese Journal of Clinical Pharmacology and Therapeutics
2024;29(11):1295-1299
- CountryChina
- Language:Chinese
-
Abstract:
AIM:To evaluate the bioequivalence of the two rivaroxaban tablets in Chinese healthy subjects.METHODS:Twenty-eight subjects under fasting status and twenty-eight subjects under fed status were enrolled in the study.This study was designed as a four period,fully repetitive,cross-over study.All subjects were administered test(T)and reference(R)rivaroxaban tablets(10 mg)un-der fasting and fed condition respectively.Liquid chromatography-tandem mass spectrometry was used to detect the concentrations of rivaroxaban in plasma.WinNonlin 7.0 was used to calculate the main pharmacokinetic parameters(PK)and to eval-uate the bioequivalence.RESULTS:In fasting group,the main pharmacokinetic parameters of T and R preparation were as follows:Cmax were(186.57±56.41)and(187.61±50.89)ng/mL;AUC0-t were(1 156.21±335.85)and(1 177.59±343.72)h·ng·mL-1;AUC0-∞ were(1 235.77±384.03)and(1223.53±392.10)ng·h·mL-1.The 90％confidential interval(CI)of the three main parameters were 90.81％-105.67％,92.83％-103.85％and 95.04％-107.13％.The upper limit of the 90％CI for the test-to-reference ratio of the within-subject of Cmax,AUC0-t and AUC0-∞ were 1.56,1.41 and 1.73.In fed group,the main pharmacokinetic parameters of T and R preparation were as follows:Cmax were(207.81±45.26)and(211.04±36.62)ng/mL;AUC0-t were(1 271.26±260.92)and(1 233.23±201.85)h·ng·mL-1;AUC0-∞ were(1 290.76±264.90)and(1251.68±203.73)ng·h·mL-1.The 90％CI of the three main parameters were 92.82％-102.28％,97.68％-106.68％and 97.71％-106.68％.The upper limit of the 90％CI for the test-to-reference ratio of the within-subject of Cmax,AUC0t and AUC0-∞were 1.76,1.47 and 1.47.CONCLUSION:The two preparations of rivaroxaban tablets were bioequiva-lent.
