PMID- 23870611
OWN - NLM
STAT- MEDLINE
DCOM- 20140127
LR  - 20221207
IS  - 1879-114X (Electronic)
IS  - 0149-2918 (Linking)
VI  - 35
IP  - 7
DP  - 2013 Jul
TI  - Effect of food on the pharmacokinetic properties of the oral sarpogrelate 
      hydrochloride controlled-release tablet in healthy male Korean subjects.
PG  - 1038-44
LID - S0149-2918(13)00318-4 [pii]
LID - 10.1016/j.clinthera.2013.06.002 [doi]
AB  - BACKGROUND: A new controlled-release formulation of sarpogrelate, a 
      5-hydroxytryptamine receptor subtype 2 antagonist that blocks serotonin-induced 
      platelet aggregation, has been developed for once-daily administration. 
      OBJECTIVE: This study evaluated the effect of food on the pharmacokinetic 
      properties of controlled-release sarpogrelate (sarpogrelate CR) in healthy 
      volunteers. METHODS: A randomized, open-label, two-period, two-treatment 
      crossover study was performed in healthy male Korean subjects. Following an 
      overnight fast, a single dose of sarpogrelate CR 300 mg was administered either 
      in the fasted condition or immediately after a high-fat breakfast. 
      Pharmacokinetic parameters were calculated using a noncompartmental analysis. 
      Tolerability was determined using clinical laboratory testing and physical 
      examination, including vital sign measurements, electrocardiography, and 
      interviews with the volunteers regarding adverse events (AEs). RESULTS: A total 
      of 24 healthy subjects were enrolled, 23 of whom completed the study (mean 
      [range] age, 26 years [21-45]; weight, 68.1 kg [56.0-79.9]; body mass index, 22.1 
      kg/m(2) [18.8-25.0]). Sarpogrelate C(max) and AUC(last) were decreased In the fed 
      condition compared with those in the fasted condition, with geometric mean ratios 
      (90% CI) of 0.4868 (0.4041-0.5864) and 0.7394 (0.6809-0.8028), respectively. 
      T(max) was delayed from 0.75 to 4.0 hours after a high-fat meal, but the fed 
      condition exhibited a similar elimination profile to that of the fasted 
      condition. The most commonly reported AE was headache (n = 2), and other AEs were 
      reported in 1 subject each. All of the AEs were considered mild in intensity, and 
      the participants recovered without treatment. CONCLUSIONS: Compared with the 
      administration of sarpogrelate CR 300 mg in the fasted condition, administration 
      with food was associated with a decreased rate and extent of absorption, as 
      assessed by C(max) and AUC(last), respectively. The drug was well-tolerated by 
      the healthy subjects in this study.
CI  - Copyright (c) 2013 Elsevier HS Journals, Inc. All rights reserved.
FAU - Jung, Jin Ah
AU  - Jung JA
AD  - Department of Clinical Pharmacology and Therapeutics, Samsung Medical Center, 
      Seoul, Republic of Korea.
FAU - Kim, Jung-Ryul
AU  - Kim JR
FAU - Kim, Tae-Eun
AU  - Kim TE
FAU - Lee, Soo-Youn
AU  - Lee SY
FAU - Huh, Wooseong
AU  - Huh W
FAU - Lee, Jae Won
AU  - Lee JW
FAU - Jun, Hun
AU  - Jun H
FAU - Ko, Jae-Wook
AU  - Ko JW
LA  - eng
PT  - Clinical Trial
PT  - Journal Article
PT  - Randomized Controlled Trial
PT  - Research Support, Non-U.S. Gov't
PL  - United States
TA  - Clin Ther
JT  - Clinical therapeutics
JID - 7706726
RN  - 0 (Delayed-Action Preparations)
RN  - 0 (Succinates)
RN  - 0 (Tablets, Enteric-Coated)
RN  - 19P708E787 (sarpogrelate)
SB  - IM
MH  - Administration, Oral
MH  - Adult
MH  - Asian People
MH  - Cross-Over Studies
MH  - Delayed-Action Preparations
MH  - Drug Administration Schedule
MH  - Drug Tolerance
MH  - *Food
MH  - *Food-Drug Interactions
MH  - Healthy Volunteers
MH  - Humans
MH  - Male
MH  - Middle Aged
MH  - Succinates/administration & dosage/*pharmacokinetics
MH  - Tablets, Enteric-Coated
OTO - NOTNLM
OT  - 5-HT receptor antagonist
OT  - food effect
OT  - healthy subjects
OT  - pharmacokinetics
EDAT- 2013/07/23 06:00
MHDA- 2014/01/28 06:00
CRDT- 2013/07/23 06:00
PHST- 2013/04/22 00:00 [received]
PHST- 2013/05/30 00:00 [revised]
PHST- 2013/06/04 00:00 [accepted]
PHST- 2013/07/23 06:00 [entrez]
PHST- 2013/07/23 06:00 [pubmed]
PHST- 2014/01/28 06:00 [medline]
AID - S0149-2918(13)00318-4 [pii]
AID - 10.1016/j.clinthera.2013.06.002 [doi]
PST - ppublish
SO  - Clin Ther. 2013 Jul;35(7):1038-44. doi: 10.1016/j.clinthera.2013.06.002.