KMID : 0043320120350040683
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Archives of Pharmacal Research 2012 Volume.35 No. 4 p.683 ~ p.689
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Development of novel ibuprofen-loaded solid dispersion with enhanced bioavailability using cycloamylose
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Baek Hyung-Hee
Kim Dae-Hwan Kwon So-Young Rho Shin-Joung Kim Dong-Wuk Choi Han-Gon Kim Yong-Ro Yong Chul-Soon
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Abstract
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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.
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KEYWORD
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Bioavailability, Cycloamylose, Ibuprofen, Solid dispersion
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