A Phase I study to characterize the multiple-dose pharmacokinetics, pharmacodynamics and safety of new enteric-coated triflusal formulations in healthy male volunteers

Title
A Phase I study to characterize the multiple-dose pharmacokinetics, pharmacodynamics and safety of new enteric-coated triflusal formulations in healthy male volunteers
Author(s)
임미선Hae Won Lee[Hae Won Lee]Sook Jin Seong[Sook Jin Seong]Joomi Lee[Joomi Lee]Jeonghyeon Park[Jeonghyeon Park]Jeong Ju Seo[Jeong Ju Seo]Hwi-yeol Yun[Hwi-yeol Yun]In-hwan Baek[In-hwan Baek]Kwang-il Kwon[Kwang-il Kwon]Young-Ran Yoon[Young-Ran Yoon]
Keywords
MYOCARDIAL-INFARCTION; CEREBRAL INFARCTION; ASPIRIN; SINGLE; PREVENTION; METABOLITE; CAPSULES; TRIAL; DRUG
Issue Date
201112
Publisher
INFORMA HEALTHCARE
Citation
EXPERT OPINION ON DRUG METABOLISM & TOXICOLOGY, v.7, no.12, pp.1471 - 1479
Abstract
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.
URI
http://hdl.handle.net/YU.REPOSITORY/24167http://dx.doi.org/10.1517/17425255.2011.630661
ISSN
1742-5255
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약학대학 > 약학부 > Articles
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