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Guntūr, India

Mehatha A.K.,Matrix Laboratories Ltd | Suryadevara V.,Matrix Laboratories Ltd | Lankapalli S.R.,Matrix Laboratories Ltd | Deshmukh A.M.,Matrix Laboratories Ltd | Sambath L.P.,Matrix Laboratories Ltd
Turkish Journal of Pharmaceutical Sciences | Year: 2014

The solubility behaviour of drugs remains one of the most challenging aspects in formulation development. Many different methods have been tried over a long period for enhancing 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 enhancing 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 technique. 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 formulations was improved by the presence of polymer. Solid-state characterization indicated that ezetimibe was present as amorphous material in formulation with kollidon VA64, due to efficient entrapment in polyer matrix. Ezetimibe in pure form has very slow dissolution rate, when compared with dispersions. Source

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