title: Development of raloxifene-solid dispersion with improved oral bioavailability via spray-drying technique.
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.
authors: College of Pharmacy, Yeungnam University, 214-1, Dae-Dong, Gyongsan 712-749, South Korea.
authors: Tuan Hiep
authors: TH
authors: Tran
authors: Bijay Kumar
authors: BK
authors: Poudel
authors: Nirmal
authors: N
authors: Marasini
authors: Jong Soo
authors: JS
authors: Woo
authors: Han-Gon
authors: HG
authors: Choi
authors: Chul Soon
authors: CS
authors: Yong
authors: Jong Oh
authors: JO
authors: Kim
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding; D008297:Male; D008855:Microscopy, Electron, Scanning; D015394:Molecular Structure; D044367:Phase Transition; D020849:Raloxifene Hydrochloride / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley; D020845:Selective Estrogen Receptor Modulators / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics; D012995:Solubility; D013499:Surface Properties; D014961:X-Ray Diffraction
chemical_list: D004337:Drug Carriers; D020845:Selective Estrogen Receptor Modulators; D020849:Raloxifene Hydrochloride