In:
Journal of Pharmacy and Pharmacology, Oxford University Press (OUP), Vol. 64, No. 11 ( 2012-10-12), p. 1631-1637
Abstract:
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.
Type of Medium:
Online Resource
ISSN:
2042-7158
,
0022-3573
DOI:
10.1111/j.2042-7158.2012.01541.x
Language:
English
Publisher:
Oxford University Press (OUP)
Publication Date:
2012
detail.hit.zdb_id:
2041988-0
detail.hit.zdb_id:
2050532-2
SSG:
15,3
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