Study of Hot Melt Granulation to Improve Dissolution Rate of Empagliflozin

OBJECTIVE To improve the dissolution rate of empagliflozin by hot-melt granulation technology. METHODS The compositions of empagliflozin were prepared by hot-melt granulation, with microcrystalline cellulose (MCC) as filler, the ratio empagliflozin to MCC in composition 1, 2 and 3 was 1∶2，1∶3 and 1∶4, respectively . Appearances were observed by microscope, the physical states of compositions were investigated by differential scanning calorimetry (DSC) and X-ray powder diffraction analysis (XRPD). The dissolution rate of empagliflozin with different particle sizes and different compositions were also compared. RESULTS The DSC and XRPD spectrum of the compositions showed that empagliflozin existed in amorphous form and crystal form. The dissolution rate of compositions have been improved by hot-melt granulation. The dissolution rate of composition 2 and 3 were similar to that of micronized empagliflozin. CONCLUSION Dissolution rate of empagliflozin has been improved by hot-melt granulation.