Enhancement of solubility and dissolution rate of domperidone by utilizing different techniques

Abstract

The aim of this study was to enhance solubility and dissolution of water insoluble antiemetic drug, domperidone, with three different techniques viz., solid dispersion, melt granulation, and liquisolid compacts techniques. Solid dispersion and melt granulation systems at 1:1, 1:2 and 1:3 drug to polymer ratios were prepared. Several liquisolid formulations containing various ratios of drug: liquid vehicle (ranging from 5% to 50% w/w) were formulated. The IR spectroscopy, scanning electron microscopy (SEM), X-ray powder diffractometry (XRD) and differential scanning calorimetry (DSC) were used to examine the physical state of the drug. Furthermore, the solubility and the in-vitro dissolution of the drug from the different systems were studied. The in-vitro dissolution study showed that the percent of the drug dissolved from solid dispersions containing 3 parts of each of PF-127, PEG 6000, Myrj 52 or PEG 4000 is 54.3, 48.98, 43.37, and 43.2% after 6 hrs respectively, compared to only 8% dissolved of drug alone. There is a highly significant difference in % of domperidone dissolved from solid dispersion, melt granulation, and liquisolid compacts systems compared to drug alone (P< 0.001), also the difference between solid dispersion system compared to the other systems was highly significant (P< 0.001). It can be concluded that domperidone aqueous solubility and dissolution were markedly improved via solid dispersion technique with PF-127 prepared by solvent evaporation method compared to other methods used. The data from the (SEM), (XRD) and (DSC) revealed absence of crystalline structure for domperidone in its solid dispersion with Pluronic F-127 (1:3) drug to polymer ratio. Also, the IR spectra indicated the absence of well defined interaction.