Development of raloxifene-solid dispersion with improved oral bioavailability via spray-drying technique

Title
Development of raloxifene-solid dispersion with improved oral bioavailability via spray-drying technique
Author(s)
김종오트란탄힙포우델비자이마라시니니르말최한곤[최한곤]용철순우종수[우종수]
Keywords
DISSOLUTION RATE; IN-VITRO; PHARMACOKINETICS; CLASSIFICATION; SOLUBILITY; DRUG
Issue Date
201301
Publisher
PHARMACEUTICAL SOC KOREA
Citation
ARCHIVES OF PHARMACAL RESEARCH, v.36, no.1, pp.86 - 93
Abstract
The purpose of this study was to develop a raloxifene-loaded solid dispersion with enhanced dissolution rate and bioavailability via spray-drying technique. Solid dispersions of raloxifene (RXF) were prepared with PVP K30 at weight ratios of 1:4, 1:6 and 1:8 using a spray-drying method, and characterized by differential scanning calorimetry, X-ray powder diffraction, scanning electron microscopy, and solubility and dissolution tests. The bioavailability of the solid dispersion in rats was also evaluated compared to those of RXF powder and commercial product. Results showed that the RXF-loaded solid dispersion was in amorphous form with increased solubility and dissolution rate. The absorption of RXF from solid dispersion resulted in approximately 2.6-fold enhanced bioavailability compared to pure drug. Moreover, RXF-loaded solid dispersion gave similar AUC, C-max and T-max values to the commercial product, suggesting that it was bioequivalent to the commercial product in rats. These findings suggest that an amorphous solid dispersion of RXF could be a viable option for enhancing the oral bioavailability of RXF.
URI
http://hdl.handle.net/YU.REPOSITORY/26821http://dx.doi.org/10.1007/s12272-013-0012-y
ISSN
0253-6269
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약학대학 > 약학부 > Articles
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