ABSTRACT

The solubility behaviour of drugs remains one of the most clıallenging aspects in fonnulation development. Many different methods have been tried över a long period for enlıancing the solubility of poorly soluble drugs. Preparing a solid dispersion is one among the methods. Solid dispersions in water-soluble carriers have shown promising results as a means of enlıancing the dissolution rate, thus improving bioavailability for most of hydrophobic drugs. The objective of the present study was to enhance the solubility and dissolution rate of a poorly water-soluble drug, ezetimibe. Solid dispersions were prepared by using Kollidon VA64 as carrier with different drug-to-carrier ratios. Dispersions with Kollidon VA64 were prepared by melt extrusion teclınique. These formulations were characterized for solid State properties by differential scanning calorimetry, X-ray powder diffraction and FTIR spectral studies. Formulations were further evaluated for dissolution and stability studies. The aqueous solubility of ezetimibe, in present fonnulations was improved by the presence of polymer. Solid-state characterization indicated that ezetimibe was present as amorphous material in fonnulation with kollidon VA64, due to efficient entrapment in polyer matrix. Ezetimibe in püre fonn has very slow dissolution rate, when compared with dispersions.