期刊
JOURNAL OF PHARMACY AND PHARMACOLOGY
卷 64, 期 11, 页码 1631-1637出版社
WILEY-BLACKWELL
DOI: 10.1111/j.2042-7158.2012.01541.x
关键词
ketoprofen; oral bioavailability; pluronic; poorly soluble drug; solubilisation
资金
- Phospholipid Research Center, Heidelberg, Germany
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 (similar to 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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