Authors
Satoko Ueda, Mitsuaki Chujo, Nobuo Miyadai, Clemence Rauch, Valentine Polivka, Yujin Saito, Ichiro Kawase, Naoki Uchida, Shunji Matsuki
Published in
Clinical pharmacology in drug development. Volume 15. Issue 10. Pages e70112.
Abstract
We conducted a pharmacokinetic study to compare two fixed-dose combinations of ibuprofen/acetaminophen (IP-TA and IP-TB) with different formulation designs and excipient compositions, and explored how formulation differences influence ibuprofen pharmacokinetics by comparing in vitro dissolution and in vivo absorption profiles. In an open-label, randomized, 2-treatment, 2-period, 2-sequence crossover study, 24 healthy Japanese participants received a single oral dose of IP-TA (ibuprofen 195 mg and acetaminophen 195 mg) or IP-TB (ibuprofen 160 mg and acetaminophen 160 mg) under fasting conditions. Pharmacokinetic data were analyzed using a linear mixed-effects model. Fraction absorbed (Fa) was estimated using the Loo-Riegelman method, and ibuprofen dissolution was evaluated at pH 1.2, 4.0, and 6.8. The relationship between weighted mean dissolution rates (D) and Fa was examined. Ibuprofen absorption from IP-TA was faster than from IP-TB, as reflected by higher Cmax and greater early exposure, and these differences remained after dose normalization. Dissolution profiles showed temporal similarity with absorption profiles, particularly for IP-TA. Analysis of Fa also suggested a relatively high degree of synchronization between ibuprofen and acetaminophen absorption in IP-TA. These findings indicate that formulation-dependent differences in dissolution behavior may influence early ibuprofen absorption, although further studies are needed to clarify the underlying mechanisms.
PMID:
42877988
Bibliographic data and abstract were imported from PubMed on 16 Oct 2026.
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