용해도가 개선된 티카그렐러 고체분산체 함유 정제의 개발

Abstract

The objective of this study was to develop a novel ticagrelor (TC) solid dispersion-loaded tablet with enhancedsolubility. Numerous polymers and surfactant were screened, and then Kollidon VA64 and Poloxamer 407 were selectedas a soluble polymer and a surfactant for preparing TC solid dispersions. Various solid dispersions were prepared by spraydryingprocess, and the physicochemical properties, solubility and dissolution profile were investigated. The TC soliddispersion consisted of TC, Kollidon VA64, Poloxamer 407 and colloidal silica at a weight ratio of 1/1/4/1, provided anamorphous drug and spherical particle shape. Moreover, it exhibited excellent solubility and dissolution rate compared tothe TC. The TC solid dispersion-loaded tablet were prepared and their dissolution were evaluated compared to commercialTC tablet. The required time for complete release of the TC solid dispersion and the TC solid dispersion-loaded tabletwere within 60 min and 8 hrs in various dissolution media. However commercial TC tablets showed low dissolution rateless than 10% in pH 1.2, 4.0 and 6.8 buffer up to 8 hrs. Thus, we successfully prepared the TC solid dispersion-loadedtablet for enhancing solubility of TC and this novel TC solid dispersion-loaded tablet could be a potential alternative forcommercial TC tablet.