Preparation and in Vitro Evaluation of Florfenicol Solid Dispersions with Soluplus^® and PVP VA64 as Matrix

OBJECTIVE To prepare florfenicol solid dispersions(FF-SDs) with Soluplus^® and PVP VA64 as matrix to improve its solubility and in vitro dissolution. METHODS The solubility parameter method was used to predict the compatibility between florfenicol and carrier materials. Consequently, FF-SDs were prepared by solvent evaporation method with Soluplus^® and PVP VA64 as matrix, respectively; and characterized by differential scanning calorimetry(DSC), X-ray powder diffraction(XPRD) and fourier transform infrared spectroscopy(FTIR), and compared with FF-SDs with PVP K30 as matrix. The effects of different carriers on the solubility and in vitro dissolution of florfenicol in solid dispersions were compared. RESULTS The results of DSC, XPRD and FTIR showed that FF was amorphous after being prepared into solid dispersions. In addition, compared with florfenicol, the solubility and cumulative dissolution of FF-SDs were improved. The efficiency of solubilization was as follows:PVP VA64>PVP K30>Soluplus^®. Especially, FF-SD with PVP VA64 as matrix could enhance the solubility remarkably. The solubility was about 3 times of free florfenicol in standard hard water, tap water, and purified water at 25℃, and the cumulative dissolution reached 88.23% at 5 min in hard water, which was 20.56 folds of florfenicol. CONCLUSION The FF-SDs prepared with PVP VA64 as matrix by solvent evaporation method can significantly enhance the solubility and dissolution of florfenicol.