Enhanced bioavailability of rebamipide nanocrystal tablets: Formulation and in vitro/in vivo evaluation

The purpose of this study was to formulate rebamipide nanocrystal tablets (REB-NTs) by wet-milling technique to enhance its dissolution rate and oral bioavailability. The formulation and preparation technology were screened by single factor tests with particle size and distribution as indicators. Rebamipide nanocrystals (REB-NSs) was then achieved by freeze-dry from the prepared nanosuspensions which were characterized by differential scanning calorimetry (DSC) and x-ray powder diffraction (XRD), while the vitro dissolution and the plasma drug concentration of the nanocrystal tablets were investigated. The results indicated that the prepared nanosuspensions got an average particle size of 286 nm, PI of 0.173 and the average Zeta potential of −18.2 mv. The average particle size of obtained REB-NSs’ redispersibility was 278 nm, and the crystalline of REB-NSs was the same as the rebamipide bulk drug as shown by DSC and XRD. The drug dissolution rate of self-made nanocrystal tablets in different dissolutions was slightly faster than that from the reference tablets, REB-MTs (Mucosta®), while the Cmax and AUC0–24 of REB-NTs were 1 and 1.57 times higher than that of REB-MTs, which means the nanotechnology could significantly improve the oral bioavailability of rebamipide.