Oral bioavailability of ketoprofen in suspension and solution formulations in rats: the influence of poloxamer 188
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 r...
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| Hauptverfasser: | , , , |
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| Dokumenttyp: | Article (Journal) |
| Sprache: | Englisch |
| Veröffentlicht: |
20 June 2012
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| In: |
Journal of pharmacy and pharmacology
Year: 2012, Jahrgang: 64, Heft: 11, Pages: 1631-1637 |
| ISSN: | 2042-7158 |
| DOI: | 10.1111/j.2042-7158.2012.01541.x |
| Online-Zugang: | Verlag, Volltext: http://dx.doi.org/10.1111/j.2042-7158.2012.01541.x Verlag, Volltext: https://onlinelibrary.wiley.com/doi/abs/10.1111/j.2042-7158.2012.01541.x 
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| Verfasserangaben: | Sarah Maud Fischer, Johannes Parmentier, Stephen Timothy Buckley, Isolde Reimold, Martin Brandl and Gert Fricker |
| Zusammenfassung: | 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. |
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| Beschreibung: | Gesehen am 12.07.2019 |
| Beschreibung: | Online Resource |
| ISSN: | 2042-7158 |
| DOI: | 10.1111/j.2042-7158.2012.01541.x |