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KMID : 0043320120350040683
Archives of Pharmacal Research
2012 Volume.35 No. 4 p.683 ~ p.689
Development of novel ibuprofen-loaded solid dispersion with enhanced bioavailability using cycloamylose
Baek Hyung-Hee

Kim Dae-Hwan
Kwon So-Young
Rho Shin-Joung
Kim Dong-Wuk
Choi Han-Gon
Kim Yong-Ro
Yong Chul-Soon
Abstract
To develop a novel ibuprofen-loaded solid dispersion with enhanced bioavailability using cycloamylose, it was prepared using spray-drying techniques with cycloamylose at a weight ratio of 1:1. The effect of cycloamylose on aqueous solubility of ibuprofen was investigated. The physicochemical properties of solid dispersions were investigated using scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and X-ray diffraction. The dissolution and bioavailability in rats were evaluated compared with ibuprofen powder. This ibuprofen-loaded solid dispersion improved about 14-fold drug solubility. Ibuprofen was present in an unchanged crystalline state, and cycloamylose played the simple role of a solubilizing agent in this solid dispersion. Moreover, the dispersion gave 2-fold higher AUC (area under the drug concentration-time curve) value compared with a ibuprofen powder, indicating that it improved the oral bioavailability of ibuprofen in rats. Thus, the solid dispersion may be useful to deliver ibuprofen with enhanced bioavailability without crystalline change.
KEYWORD
Bioavailability, Cycloamylose, Ibuprofen, Solid dispersion
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