Back to Journals » Drug Design, Development and Therapy » Volume 11

Pharmacokinetic and pharmacodynamic evaluation according to absorption differences in three formulations of ibuprofen

Authors Shin D, Lee SJ, Ha Y, Choi YS, Kim JW, Park SR, Park MK

Received 6 September 2016

Accepted for publication 1 November 2016

Published 4 January 2017 Volume 2017:11 Pages 135—141

DOI https://doi.org/10.2147/DDDT.S121633

Checked for plagiarism Yes

Review by Single-blind

Peer reviewers approved by Dr Junhua Mai

Peer reviewer comments 3

Editor who approved publication: Dr Georgios Panos

Dongseong Shin,1 Sook Joung Lee,2 Yu-Mi Ha,3 Young-Sim Choi,3 Jae-Won Kim,3 Se-Rin Park,3 Min Kyu Park3

1Clinical Trials Center, Gachon University Gil Medical Center, Incheon, 2Department of Rehabilitation Medicine, 3Department of Clinical Pharmacology and Therapeutics, Dong-A University College of Medicine and Hospital, Busan, South Korea

Objective: Prostaglandin E2 (PGE2) synthesis is modulated by COX2. Changes in PGE2 could be used to quantify the COX2 inhibition after ibuprofen administration. This study investigated the pharmacokinetic and pharmacodynamic relationships for COX2 inhibition according to three formulations of ibuprofen in healthy male subjects.
Materials and methods: A randomized, open-label, single-dose, three-treatment, six-sequence crossover study was performed in 36 healthy South Korean male volunteers. Enrolled subjects received the following three 200 mg ibuprofen formulations: ibuprofen arginine, solubilized ibuprofen capsule, and standard ibuprofen. Pharmacokinetic and pharmacodynamic blood samples were collected for 16 hours following treatment. For pharmacodynamic evaluations, lipopolysaccharide (LPS)-induced PGE2 inhibition at each time point compared to predose was measured. Noncompartmental analysis was used for pharmacokinetic assessment, and time-weighted average inhibition (WAI) of PGE2 was applied to the pharmacodynamic evaluation.
Results: After a single oral dose of the ibuprofen formulations, the median times to maximum concentration were 0.42, 0.5, and 1.25 hours in ibuprofen arginine, solubilized ibuprofen capsule, and ibuprofen, respectively. The maximum observed plasma concentration was lower in ibuprofen, and the area under the plasma concentration–time curve was comparable among the three formulations. A significant difference was observed between fast-acting formulations and standard ibuprofen tablets for both maximum concentration and time taken to reach it. Individual formulations had an effect on PGE2 WAI during the 8 hours following treatment, resulting in significantly lower WAI in standard ibuprofen: ibuprofen arginine 18.4%, solubilized ibuprofen capsule 18.4%, and standard ibuprofen 11.6%.
Conclusion: Rapid absorption and higher peak concentration were observed in ibuprofen arginine and the solubilized ibuprofen capsule. Additionally, fast-acting formulations had more predominant inhibitory activity on the COX2 enzyme.

Keywords: ibuprofen, different formulation, COX2-inhibitory effects 

Creative Commons License This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution - Non Commercial (unported, v3.0) License. By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms.

Download Article [PDF]  View Full Text [HTML][Machine readable]

 

Other article by this author:

Pharmacokinetics and tolerability of DA-8031, a novel selective serotonin reuptake inhibitor for premature ejaculation in healthy male subjects

Shin D, Lee S, Yi S, Yoon SH, Cho JY, Bahng MY, Jang IJ, Yu KS

Drug Design, Development and Therapy 2017, 11:713-723

Published Date: 10 March 2017