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Development of raloxifene-solid dispersion with improved oral bioavailability via spray-drying technique.
Arch Pharm Res. 2013 Jan; 36(1):86-93.AP

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+Show Affiliations

College of Pharmacy, Yeungnam University, 214-1, Dae-Dong, Gyongsan 712-749, South Korea.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

23325488

Citation

Tran, Tuan Hiep, et al. "Development of Raloxifene-solid Dispersion With Improved Oral Bioavailability Via Spray-drying Technique." Archives of Pharmacal Research, vol. 36, no. 1, 2013, pp. 86-93.
Tran TH, Poudel BK, Marasini N, et al. Development of raloxifene-solid dispersion with improved oral bioavailability via spray-drying technique. Arch Pharm Res. 2013;36(1):86-93.
Tran, T. H., Poudel, B. K., Marasini, N., Woo, J. S., Choi, H. G., Yong, C. S., & Kim, J. O. (2013). Development of raloxifene-solid dispersion with improved oral bioavailability via spray-drying technique. Archives of Pharmacal Research, 36(1), 86-93. https://doi.org/10.1007/s12272-013-0012-y
Tran TH, et al. Development of Raloxifene-solid Dispersion With Improved Oral Bioavailability Via Spray-drying Technique. Arch Pharm Res. 2013;36(1):86-93. PubMed PMID: 23325488.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Development of raloxifene-solid dispersion with improved oral bioavailability via spray-drying technique. AU - Tran,Tuan Hiep, AU - Poudel,Bijay Kumar, AU - Marasini,Nirmal, AU - Woo,Jong Soo, AU - Choi,Han-Gon, AU - Yong,Chul Soon, AU - Kim,Jong Oh, PY - 2013/1/18/entrez PY - 2013/1/18/pubmed PY - 2013/7/20/medline SP - 86 EP - 93 JF - Archives of pharmacal research JO - Arch Pharm Res VL - 36 IS - 1 N2 - 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. SN - 0253-6269 UR - https://www.unboundmedicine.com/medline/citation/23325488/Development_of_raloxifene_solid_dispersion_with_improved_oral_bioavailability_via_spray_drying_technique_ L2 - https://dx.doi.org/10.1007/s12272-013-0012-y DB - PRIME DP - Unbound Medicine ER -