PMID- 36458443
OWN - NLM
STAT- MEDLINE
DCOM- 20230320
LR  - 20230320
IS  - 0946-1965 (Print)
IS  - 0946-1965 (Linking)
VI  - 61
IP  - 3
DP  - 2023 Mar
TI  - Pharmacokinetics, safety, and bioequivalence of apixaban tablets in healthy 
      Chinese subjects under fasting and fed conditions.
PG  - 129-138
LID - 10.5414/CP204299 [doi]
AB  - OBJECTIVE: To evaluate the pharmacokinetics (PK), safety, and bioequivalence of 
      two formulations of apixaban in healthy Chinese subjects under fasting and fed 
      conditions. MATERIALS AND METHODS: A single-center, randomized, open, 
      single-dose, two-period crossover PK study was carried out under fasting and fed 
      conditions in 64 healthy subjects enrolled in either the fasting (36 subjects) or 
      the fed (28 subjects) arms of the study. Subjects received a single oral dose of 
      2.5 mg apixaban tablets as test (T) or reference (R) formulation. The primary PK 
      parameters determined were the area under the plasma concentration-time curve 
      from zero to t and infinity (AUC(0-t) and AUC(0-infinity)) and the maximal plasma concentration 
      (C(max)). Safety was assessed mainly from the occurrence of adverse events (AEs). 
      RESULTS: A single drop-out in the fed arm of the trial was excluded from the 
      statistical evaluation. The 90% confidence intervals (CIs) for the geometric mean 
      ratio (GMR) for T/R using AUC(0-t) were 95.4 - 100.9% and 97.8 - 103.8%, and for 
      AUC(0-infinity) were 95.3 - 100.6% and 98.3 - 104.3% under fasting (36 subjects) and fed 
      (27 subjects) conditions, respectively. Similarly, the 90% CIs for C(max) were 
      94.6 - 103.1% and 88.8 - 102.0% under fasting (36 subjects) and the fed (27 
      subjects) conditions, respectively. Therefore, the 90% CIs for the T/R AUC and 
      C(max) ratios were within the standard range for bioequivalence (80.0 - 125.0%). 
      There were no serious adverse events (SAEs). CONCLUSION: The test and reference 
      2.5 mg apixaban tablets were bioequivalent and both showed good tolerability and 
      safety.
FAU - Luo, Hong-Yu
AU  - Luo HY
FAU - Yao, Zhen-Jiang
AU  - Yao ZJ
FAU - Long, Hui-Zhi
AU  - Long HZ
FAU - Zhou, Zi-Wei
AU  - Zhou ZW
FAU - Xu, Shuo-Guo
AU  - Xu SG
FAU - Li, Feng-Jiao
AU  - Li FJ
FAU - Cheng, Yan
AU  - Cheng Y
FAU - Wen, Dan-Dan
AU  - Wen DD
FAU - Deng, Ping
AU  - Deng P
FAU - Guan, Yue-Qing
AU  - Guan YQ
FAU - Gao, Li-Chen
AU  - Gao LC
LA  - eng
PT  - Journal Article
PT  - Randomized Controlled Trial
PL  - Germany
TA  - Int J Clin Pharmacol Ther
JT  - International journal of clinical pharmacology and therapeutics
JID - 9423309
RN  - 3Z9Y7UWC1J (apixaban)
RN  - 0 (Tablets)
RN  - 0 (Pyrazoles)
RN  - 0 (Pyridones)
SB  - IM
MH  - Humans
MH  - Area Under Curve
MH  - Cross-Over Studies
MH  - *East Asian People
MH  - Fasting
MH  - Healthy Volunteers
MH  - Tablets
MH  - *Therapeutic Equivalency
MH  - *Pyrazoles/pharmacokinetics
MH  - *Pyridones/pharmacokinetics
EDAT- 2022/12/03 06:00
MHDA- 2023/03/21 06:00
CRDT- 2022/12/02 03:42
PHST- 2023/02/09 00:00 [accepted]
PHST- 2022/12/03 06:00 [pubmed]
PHST- 2023/03/21 06:00 [medline]
PHST- 2022/12/02 03:42 [entrez]
AID - 189902 [pii]
AID - 10.5414/CP204299 [doi]
PST - ppublish
SO  - Int J Clin Pharmacol Ther. 2023 Mar;61(3):129-138. doi: 10.5414/CP204299.