Abstract：
: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 (∼3-fold higher D30). In addition, such preparations exhibited a significantly decreased Tmax, ∼5-fold higher Cmax and ∼1.4-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.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Yun F,Kang A,Shan J,Zhao X,Bi X,Li J,Di Ldoi
10.1016/j.ijpharm.2014.02.040subject
Has Abstractpub_date
2014-04-25 00:00:00pages
436-43issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(14)00133-1journal_volume
465pub_type
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