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Pharmacokinetic Comparison of Controlled- and Immediate-Release Formulations of Dexibuprofen after Single and Multiple Oral Doses in Fasting Healthy Male Korean Volunteers

Authors :
Noh, Yook-Hwan
Lim, Hyeong-Seok
Cho, Sang-Heon
Ghim, Jong-Lyul
Choe, Sangmin
Jung, Jin Ah
Kim, Un-Jib
Park, Kyung-Mi
Jang, Mi-jung
Bae, Kyun-Seop
Source :
Clinical Therapeutics. Sep2011, Vol. 33 Issue 9, p1132-1141. 10p.
Publication Year :
2011

Abstract

Abstract: Background: Dexibuprofen is a pure S(+)-enantiomer product of racemic ibuprofen. A new extended-release form of dexibuprofen has recently been developed. Objective: We aimed to compare pharmacokinetic characteristics of controlled-release (CR) and immediate-release (IR) formulations of dexibuprofen after single and multiple oral doses in fasting healthy male Korean volunteers. Methods: Both single- and multiple-dose studies used an open-label, randomized, 2-way, crossover design. In the single-dose study, 24 subjects were administered a 600-mg CR or 300-mg IR formulation. In the multiple-dose study, 24 subjects were administered a 600-mg CR formulation q12h or 300-mg IR formulation q6h. Pharmacokinetic parameters of dexibuprofen were determined by noncompartmental analysis. Results: All formulations used in the single- and multiple-dose studies were well tolerated, and there were no severe adverse events. In the single-dose study, the mean (SD) AUC0–t was 155.60 (40.94) μg/h/mL for the CR formulation and 161.11 (37.50) μg/h/mL for the IR formulation; the mean (SD) Cmax values were 22.71 (6.64) and 23.77 (4.91) μg/mL, respectively; and the median Tmax values were 2.01 hours and 2.00 hours, respectively. The geometric mean ratios (90% CI) of the CR to IR formulations were 0.96 (0.92–1.00) for AUC0–t and 1.00 (0.87–1.14) for Cmax. In the multiple-dose study, the mean (SD) AUC0–τ values for CR and IR were 129.70 (23.72) μg/h/mL and 150.04 (27.09) μg/h/mL, respectively; the mean (SD) Cmax,ss values were 24.51 (5.12) and 21.69 (5.21) μg/mL, respectively; and the median Tmax.ss values were 2.51 hours and 5.25 hours, respectively. The geometric mean ratios (90% CI) of the CR to IR formulations were 0.86 (0.81–0.91) for AUC0–τ and 1.13 (1.03–1.24) for Cmax. Conclusions: The pharmacokinetic parameters of single and multiple administrations of dexibuprofen did not differ for the IR and CR formulations in this small, selected group of healthy male Korean subjects. Both formulations were well tolerated. [Copyright &y& Elsevier]

Details

Language :
English
ISSN :
01492918
Volume :
33
Issue :
9
Database :
Academic Search Index
Journal :
Clinical Therapeutics
Publication Type :
Academic Journal
Accession number :
65944074
Full Text :
https://doi.org/10.1016/j.clinthera.2011.07.019