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KMID : 0043320110340030391
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Archives of Pharmacal Research
2011 Volume.34 No. 3 p.391 ~ p.397
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Enhanced solubility and bioavailability of flurbiprofen by cycloamylose
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Baek Hyung-Hee
Kwon So-Young
Rho Shin-Joung
Lee Won-Seok
Yang Ho-Joon
Hah Jung-Mi
Choi Han-Gon
Kim Yong-Ro
Yong Chul-Soon
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Abstract
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The effect of cycloamylose on the aqueous solubility of flurbiprofen was investigated. To improve the solubility and bioavailability of flurbiprofen (poor water solubility), a solid dispersion was spray dried with a solution of flurbiprofen and cycloamylose at a weight ratio of 1:1. The physicochemical properties of solid dispersions were investigated using SEM, DSC, and X-ray diffraction. The dissolution and bioavailability in rats were evaluated compared with a commercial product. Cycloamylose increased solubility of flurbiprofen approximately 12-fold and dissolution of it by 2-fold. Flurbiprofen was present in an unchanged crystalline state, and cycloamylose was a solubilizing agent for flurbiprofen in this solid dispersion. Furthermore, the dispersion gave higher AUC and Cmax values compared with the commercial product, indicating that it improved the oral bioavailability of flurbiprofen in rats. Thus, the solid dispersion may be useful to deliver flurbiprofen with enhanced bioavailability without changes in crystalline structure.
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KEYWORD
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Bioavailability, Cycloamylose, Cyclodextrins, Flurbiprofen, Solubility
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