Oral bioavailability of ketoprofen in suspension and solution formulations in rats

• Verfasst von: Fischer, Sarah Maud [VerfasserIn]
• Verfasst von: Parmentier, Johannes [VerfasserIn]
• Verfasst von: Reimold, Isolde [VerfasserIn]
• Verfasst von: Fricker, Gert [VerfasserIn]
• Titel: Oral bioavailability of ketoprofen in suspension and solution formulations in rats
• Titelzusatz: the influence of poloxamer 188
• Verf.angabe: Sarah Maud Fischer, Johannes Parmentier, Stephen Timothy Buckley, Isolde Reimold, Martin Brandl and Gert Fricker
• E-Jahr: 2012
• Jahr: 20 June 2012
• Umfang: 7 S.
• Fussnoten: Gesehen am 12.07.2019
• Titel Quelle: Enthalten in: Journal of pharmacy and pharmacology
• Ort Quelle: Oxford : Oxford University Press, 1949
• Jahr Quelle: 2012
• Band/Heft Quelle: 64(2012), 11, Seite 1631-1637
• ISSN Quelle: 2042-7158
• DOI: doi:10.1111/j.2042-7158.2012.01541.x
• Datenträger: Online-Ressource
• Sprache: eng
• Sach-SW: ketoprofen
• Sach-SW: oral bioavailability
• Sach-SW: pluronic
• Sach-SW: poorly soluble drug
• Sach-SW: solubilisation
• K10plus-PPN: 1583720863

Abstract

Objectives The 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. Methods 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. Key findings The AUC and Cmax 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 Cmax). 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. Conclusions 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.