Sarah Maud Fischer, Johannes Parmentier, Stephen Timothy Buckley, Isolde Reimold, Martin Brandl, Gert Fricker
Department of Physics, Chemistry and Pharmacy, University of Southern Denmark, Odense, Denmark.
The Journal of pharmacy and pharmacology 2012 NovThe aim of the current study was to investigate the effect of poloxamer 188 (P-188) on the bioavailability of the BCS class 2 drug ketoprofen in vivo. Aqueous suspension and solution formulations of ketoprofen with and without P-188 were orally administered to fasted male Wistar rats. The intrinsic dissolution rate and solubility of ketoprofen in simulated intestinal fluid, in both the presence and absence of P-188, was measured. The AUC and C(max) were found to be significantly enhanced when ketoprofen was administered as suspension and P-188 was present in the formulation (Susp P-188) as compared to the surfactant-free formulation (∼4-fold higher AUC, 7-fold higher C(max) ). While drug solubility appeared to be almost unaffected by P-188, a significantly faster dissolution was observed. In addition, the influence of P-188 on the drug absorption process was investigated by comparison of solution formulations with and without P-188. The in-vivo performance of these solutions, a pure buffer solution and a P-188-containing buffer solution showed no significant difference, suggesting that the increase in bioavailability for Susp P-188 was primarily a consequence of the dissolution rate-enhancing effect. © 2012 The Authors. JPP © 2012 Royal Pharmaceutical Society.
Sarah Maud Fischer, Johannes Parmentier, Stephen Timothy Buckley, Isolde Reimold, Martin Brandl, Gert Fricker. Oral bioavailability of ketoprofen in suspension and solution formulations in rats: the influence of poloxamer 188. The Journal of pharmacy and pharmacology. 2012 Nov;64(11):1631-7
PMID: 23058050
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