Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
5819728 | International Journal of Pharmaceutics | 2014 | 8 Pages |
The aim of this study was to investigate the potential of solid dispersion to improve the dissolution rate and bioavailability of osthole (Ost), a coumarin derivative with various pharmacological activities but with poor aqueous solubility. In present studies, the Ost solid dispersions were prepared with various polymers including Plasdone S-630, HPMC-E5, Eudragit EPO, and Soluplus by hot-melt extrusion method. In vitro characterizations were performed with differential scanning calorimetry (DSC), X-ray powder diffraction (XPRD), Fourier transform infrared (FT-IR) spectroscopy, and in vitro dissolution studies. In addition, in vivo pharmacokinetic studies of Ost solid dispersions were also conducted in rats after a single oral dose. In comparison to the untreated Ost coarse powder and the physical mixture with polymers, the solid dispersions prepared with Plasdone S-630 or HPMC-E5 (drug/polymer: 1:6) showed a significant enhancement of dissolution rate (â¼3-fold higher D30). In addition, such preparations exhibited a significantly decreased Tmax, â¼5-fold higher Cmax and â¼1.4-fold higher AUC when comparing with Ost coarse powder. In conclusion, solid dispersion prepared with appropriate polymer could serve as a promising formulation approach to enhance the dissolution rate and hence oral bioavailability of Ost.
Graphical abstractDownload high-res image (122KB)Download full-size image