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

Tran, Tuan Hiep, Poudel, Bijay Kumar, Marasini, Nirmal, Woo, Jong Soo, Choi, Han-Gon, Yong, Chul Soon and Kim, Jong Oh (2013) Development of raloxifene-solid dispersion with improved oral bioavailability via spray-drying technique. Archives of Pharmacal Research, 36 1: 86-93. doi:10.1007/s12272-013-0012-y


Author Tran, Tuan Hiep
Poudel, Bijay Kumar
Marasini, Nirmal
Woo, Jong Soo
Choi, Han-Gon
Yong, Chul Soon
Kim, Jong Oh
Title Development of raloxifene-solid dispersion with improved oral bioavailability via spray-drying technique
Journal name Archives of Pharmacal Research   Check publisher's open access policy
ISSN 0253-6269
1976-3786
Publication date 2013-01
Sub-type Article (original research)
DOI 10.1007/s12272-013-0012-y
Open Access Status Not Open Access
Volume 36
Issue 1
Start page 86
End page 93
Total pages 8
Place of publication Seoul, Republic of Korea
Publisher Pharmaceutical Society of Korea
Language eng
Formatted 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, Cmax and Tmax 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.
Keyword Raloxifene
Solubility
Bioavailability
Spray drying
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status Non-UQ

Document type: Journal Article
Sub-type: Article (original research)
Collection: School of Chemistry and Molecular Biosciences
 
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Created: Sat, 04 Jun 2016, 12:14:34 EST by Nirmal Marasini on behalf of School of Chemistry & Molecular Biosciences