Archives of Pharmacal Research

, Volume 36, Issue 1, pp 86–93 | Cite as

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

  • Tuan Hiep Tran
  • Bijay Kumar Poudel
  • Nirmal Marasini
  • Jong Soo Woo
  • Han-Gon Choi
  • Chul Soon Yong
  • Jong Oh Kim
Research Article

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.

Keywords

Raloxifene Solubility Bioavailability Spray drying 

Notes

Acknowledgments

This research was supported by Yeungnam University research grants in 2012.

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Copyright information

© The Pharmaceutical Society of Korea and Springer Science+Business Media Dordrecht 2013

Authors and Affiliations

  • Tuan Hiep Tran
    • 1
  • Bijay Kumar Poudel
    • 1
  • Nirmal Marasini
    • 1
  • Jong Soo Woo
    • 1
  • Han-Gon Choi
    • 2
  • Chul Soon Yong
    • 1
  • Jong Oh Kim
    • 1
  1. 1.College of PharmacyYeungnam UniversityGyongsanSouth Korea
  2. 2.College of PharmacyHanyang UniversitySangnok-guSouth Korea

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