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

被引:22
|
作者
Tran, Tuan Hiep [1 ]
Poudel, Bijay Kumar [1 ]
Marasini, Nirmal [1 ]
Woo, Jong Soo [1 ]
Choi, Han-Gon [2 ]
Yong, Chul Soon [1 ]
Kim, Jong Oh [1 ]
机构
[1] Yeungnam Univ, Coll Pharm, Kyongsan 712749, South Korea
[2] Hanyang Univ, Coll Pharm, Ansan 426791, South Korea
关键词
Raloxifene; Solubility; Bioavailability; Spray drying; IN-VITRO; DISSOLUTION; DRUG; PHARMACOKINETICS; CLASSIFICATION; SOLUBILITY; SYSTEM;
D O I
10.1007/s12272-013-0012-y
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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.
引用
收藏
页码:86 / 93
页数:8
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