삼원계를 통한 페북소스타트 고체분산체 개발 및 평가

Development and Evaluation of Febuxostat Solid Dispersion through Ternary System

Febuxostat is classified as a biopharmaceutical with low solubility in aqueous solution and high intestinal permeability (Biopharmaceutics Classification System [BCS] Class II drug). The solubility of a drug has the characteristic of increasing as pH increases. This study aims to improve the dissolution of febuxostat with Neusilin® US2 and Gelucire®50/13 by a solvent evaporation method. The optimal formulation (solid dispersion, SD1) is developed as a solid dispersion of febuxostat : Gelucire®50/13 : US2®= 1:2:4 (w/w), with a final weight of 280 mg. The dissolution of SD1 in distilled water is 72.0±2.8%, which is 1.67-fold higher than that of the commercial product, Feburic Tab® (43.2±1.8%). The SD1 formulation is believed to have improved dissolution due to changes in physicochemical properties (thermal, interaction, and crystallinity). In conclusion, through the solid dispersion manufacturing method, febuxostat is changed from a crystalline form to an amorphous form in SD1 formulation, and the improved dissolution of febuxostat formulation is developed.