PMID- 22098139
OWN - NLM
STAT- MEDLINE
DCOM- 20120319
LR  - 20221207
IS  - 1744-7607 (Electronic)
IS  - 1742-5255 (Linking)
VI  - 7
IP  - 12
DP  - 2011 Dec
TI  - A phase I study to characterize the multiple-dose pharmacokinetics, 
      pharmacodynamics and safety of new enteric-coated triflusal formulations in 
      healthy male volunteers.
PG  - 1471-9
LID - 10.1517/17425255.2011.630661 [doi]
AB  - OBJECTIVES: An enteric-coated formulation of triflusal (triflusal EC), an 
      antiplatelet agent, was developed to reduce the high incidence of 
      gastrointestinal adverse events (AEs). The aim of this study is to compare the 
      pharmacokinetics, pharmacodynamics and safety of triflusal EC with triflusal in 
      healthy Korean male subjects to determine bioequivalence and non-inferiority for 
      the purposes of marketing approval. METHODS: A randomized, open-label, 
      two-period, crossover study was conducted in 38 subjects. Either triflusal EC or 
      triflusal was administered orally as a single 900 mg loading dose (day 1) 
      followed by eight 600 mg/day maintenance doses on days 2 - 9, with a 13-day 
      washout period. The plasma concentrations of 2-hydroxy-4-trifluoromethyl benzoic 
      acid (HTB), the predominant active metabolite of triflusal, were assessed after 
      administration of the loading dose, using HPLC/MS/MS. The platelet aggregation 
      response to arachidonic acid was determined using turbidimetric aggregometry. 
      RESULTS: The 90% CIs, for the geometric mean ratios of the log-transformed AUC(tau) 
      and C(max) of HTB were seen to be within the predetermined range of 0.8 - 1.25. 
      Triflusal EC was also shown to be non-inferior in its anti-aggregatory effect. No 
      serious AEs were reported during this study. CONCLUSIONS: The pharmacokinetic and 
      pharmacodynamic profiles of the two triflusal formulations met the requirements 
      for bioequivalence and non-inferiority, respectively. Both formulations were well 
      tolerated.
FAU - Lee, Hae Won
AU  - Lee HW
AD  - Kyungpook National University Graduate School and Hospital, Department of 
      Biomedical Science and Clinical Trial Center, 200 Dongduk-Ro, Jung-gu, Daegu, 
      700-721, Republic of Korea.
FAU - Lim, Mi-sun
AU  - Lim MS
FAU - Seong, Sook Jin
AU  - Seong SJ
FAU - Lee, Joomi
AU  - Lee J
FAU - Park, Jeonghyeon
AU  - Park J
FAU - Seo, Jeong Ju
AU  - Seo JJ
FAU - Yun, Hwi-yeol
AU  - Yun HY
FAU - Baek, In-hwan
AU  - Baek IH
FAU - Kwon, Kwang-il
AU  - Kwon KI
FAU - Yoon, Young-Ran
AU  - Yoon YR
LA  - eng
PT  - Clinical Trial, Phase I
PT  - Comparative Study
PT  - Journal Article
PT  - Randomized Controlled Trial
PT  - Research Support, Non-U.S. Gov't
PL  - England
TA  - Expert Opin Drug Metab Toxicol
JT  - Expert opinion on drug metabolism & toxicology
JID - 101228422
RN  - 0 (Platelet Aggregation Inhibitors)
RN  - 0 (Salicylates)
RN  - 1Z0YFI05OO (triflusal)
RN  - 27YG812J1I (Arachidonic Acid)
RN  - 328-90-5 (4-trifluoromethylsalicylic acid)
SB  - IM
MH  - Administration, Oral
MH  - Adult
MH  - Arachidonic Acid/metabolism
MH  - Asian People
MH  - Chemistry, Pharmaceutical
MH  - Chromatography, High Pressure Liquid
MH  - Cross-Over Studies
MH  - *Dose-Response Relationship, Drug
MH  - Humans
MH  - Male
MH  - Platelet Aggregation/drug effects
MH  - Platelet Aggregation Inhibitors/*administration & dosage/*pharmacokinetics
MH  - Salicylates/*administration & dosage/blood/*pharmacokinetics
MH  - Tandem Mass Spectrometry
MH  - Therapeutic Equivalency
MH  - Young Adult
EDAT- 2011/11/22 06:00
MHDA- 2012/03/20 06:00
CRDT- 2011/11/22 06:00
PHST- 2011/11/22 06:00 [entrez]
PHST- 2011/11/22 06:00 [pubmed]
PHST- 2012/03/20 06:00 [medline]
AID - 10.1517/17425255.2011.630661 [doi]
PST - ppublish
SO  - Expert Opin Drug Metab Toxicol. 2011 Dec;7(12):1471-9. doi: 
      10.1517/17425255.2011.630661.