PMID- 36871246
OWN - NLM
STAT- Publisher
LR  - 20240216
IS  - 0946-1965 (Print)
IS  - 0946-1965 (Linking)
DP  - 2023 Mar 5
TI  - Comparative pharmacokinetics of two formulations of 2.5-mg rivaroxaban in healthy 
      Korean subjects.
LID - 10.5414/CP204335 [doi]
AB  - OBJECTIVE: Rivaroxaban is a direct factor Xa inhibitor used for the prevention 
      and treatment of thromboembolic disorders. The objective of this study was to 
      compare the pharmacokinetic profiles of two rivaroxaban formulations after a 
      single dose of rivaroxaban (2.5-mg tablet) in healthy Korean subjects. MATERIALS 
      AND METHODS: This study was a randomized, open-label, single-dose, two-period, 
      crossover study that included 34 healthy adult subjects under fasting conditions. 
      The test drug (Yuhan rivaroxaban tablet) or reference drug (Xarelto tablet) was 
      administered in each period. Serial blood samples were collected up to 36 hours 
      post-dose. Plasma concentrations were measured by LC-MS/MS. Pharmacokinetic 
      parameters, including maximum plasma concentration (C(max)) and area under the 
      plasma concentration-time curve from time zero to the last measurable 
      concentration (AUC(t)), were determined by non-compartmental analysis. The 90% 
      confidence intervals (CIs) for the ratio of the geometric means of C(max) and 
      AUC(t) for the test drug/reference drug were calculated to evaluate 
      pharmacokinetic equivalence. RESULTS: A total of 28 subjects were included in the 
      pharmacokinetic analysis. The geometric mean ratios (90% CI) of the test 
      drug/reference drug for rivaroxaban were 1.0140 (0.9794 - 1.0499) for AUC(t) and 
      0.9350 (0.8797 - 0.9939) for C(max). All adverse events (AEs) were mild, and 
      there was no significant difference in the incidence of AEs between the 
      formulations. CONCLUSION: The pharmacokinetic parameters of rivaroxaban were 
      compared between the test and reference drug, and both formulations were 
      bioequivalent. The newly developed rivaroxaban tablet is safe and well tolerated 
      as the reference drug (ClinicalTrials.gov identifiers: NCT05418803).
FAU - Moon, Seol Ju
AU  - Moon SJ
FAU - Kim, Yunjeong
AU  - Kim Y
FAU - Kim, Sun-Young
AU  - Kim SY
FAU - Jeon, Ji-Young
AU  - Jeon JY
FAU - Song, Eunji
AU  - Song E
FAU - Lim, Yeji
AU  - Lim Y
FAU - Kim, Min-Gul
AU  - Kim MG
LA  - eng
SI  - ClinicalTrials.gov/NCT05418803
PT  - Journal Article
DEP - 20230305
PL  - Germany
TA  - Int J Clin Pharmacol Ther
JT  - International journal of clinical pharmacology and therapeutics
JID - 9423309
SB  - IM
EDAT- 2023/03/06 06:00
MHDA- 2023/03/06 06:00
CRDT- 2023/03/05 14:27
PHST- 2023/03/05 00:00 [accepted]
PHST- 2023/03/05 14:27 [entrez]
PHST- 2023/03/06 06:00 [pubmed]
PHST- 2023/03/06 06:00 [medline]
AID - 190133 [pii]
AID - 10.5414/CP204335 [doi]
PST - aheadofprint
SO  - Int J Clin Pharmacol Ther. 2023 Mar 5. doi: 10.5414/CP204335.