Supercritical Fluid Technology Preparation Of Itraconazole Solid Dispersion Technology Was Studied

Intraconazole solid dispersion was prepared by supercritical CO2 method to improve the dissolution and bioavailability of intraconazole which is poorly water soluble.Methods of content assay, in-vitro release test and relative substances detection were respectively carried out by UV spectrophotography. The method had good linearity, sufficient recovery and good accuracy. The RSD of intraday and interday precision are lower than 2%.Using dissolution in vitro of intraconazole as index, orthogonal experiment was done based on single factor experiments and the optimal conditions were:Polo 188 was the carrier material, the proportion of intraconazole and Polo 188 was 1:8, supercritical experiment time was 12h, temperature was 55℃, pressure was 25MPa. In-vitro release test showed that the drug’s index prepared by supercritical CO2 method could be 85.21%, which would be much higher than that of melting method (60.41%). The dissolution after the treatment was 14 times higher than that of original drug. Intraconacole was in armorphous phase or dispersed in molecules, indicated by differential scanning calorimeter (DSC).Stability experiment showed that intraconazole solid dispersion would be stable in the conditions of light and heat, but not in the moist environment. Powder mass experiment showed that intraconazole solid dispersion had a great fluidity.