Preparation of Solid Dispersion of Everolimus in Gelucire 50/13 using Melt Granulation Technique for Enhanced Drug Release
- Authors
- Jang, Sun Woo; Choi, Young Wook; Kang, Myung Joo
- Issue Date
- 20-Jul-2014
- Publisher
- KOREAN CHEMICAL SOC
- Keywords
- Everolimus; Solid dispersion; Gelucire 50/13; Dissolution; Melt granulation
- Citation
- BULLETIN OF THE KOREAN CHEMICAL SOCIETY, v.35, no.7, pp 1939 - 1943
- Pages
- 5
- Journal Title
- BULLETIN OF THE KOREAN CHEMICAL SOCIETY
- Volume
- 35
- Number
- 7
- Start Page
- 1939
- End Page
- 1943
- URI
- https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/12038
- DOI
- 10.5012/bkcs.2014.35.7.1939
- ISSN
- 0253-2964
1229-5949
- Abstract
- Solid dispersion (SD) system of everolimus (EVR) with Gelucire 50/13 (Stearoyl polyoxyl-32 glycerides) was prepared using melt granulation technique with the aim of improving the physicochemical properties and dissolution rate. The solid state characterization using scanning electron microscopy and X-ray powder diffraction, indicated that the drug was homogeneously distributed in the surfactant carrier in a stable amorphous form. The dissolution rate of EVR from the optimized SD composed of the drug, Gelucire 50/13 and microcrystalline cellulose in a weight ratio of 1:5:10, was markedly rapid and higher than that from the drug powder and the market product (Afinitor (R), Novartis Pharmaceuticals) in all dissolution mediums tested from pH 3.0 to pH 6.8. The results of this study suggest that formulation of SD with Gelucire 50/13 using melt granulation procedure may be a simple and promising approach for improving the dissolution rate and oral absorption of the anti-cancer agent without the need for using an organic solvent.
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