The aim of this study was to prepare and characterize rifaximin nanosuspensions to mask bitter taste and enhance the solubility of this drug. Nanosuspensions were prepared by the precipitation ultrasonication method. The effects of two important process parameters, i.e. the concentration of PVA in the anti-solvent and the time length of ultrasonication on the particle size of nanosuspensions were investigated systematically and the optimal values were 0.15% and 15 min, respectively. The particle size and zeta potential of nanocrystals were 129 nm and −23.9 mV, respectively. The morphology of nanocrystals was found to be flaky and spherical in shape by scanning electron microscopy (SEM) observation. The X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC) analysis indicated that there was no substantial crystalline change in the nanocrystals compared with raw crystals. The taste of rifaximin was significantly masked and its solubility increased by reducing the particle size.
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