Characterization, Purity Determination and Decomposition Kinetics of Ezetimibe Under Non-Isothermal Conditions

Abstract

Background: Ezetimibe is a lipid-lowering agent used therapeutically alone or in combination of other drugs. The properties of the solid-state of drugs are critical factors in the pharmaceutical formulation development. Several instrumental techniques can be employed in the analysis of new formulations, but the thermoanalytical techniques, provide a fast and careful evaluation of physicochemical properties of a compound. </P><P> Objective: To carry out the physicochemical characterization, purity evaluation and non-isothermal kinetic studies of ezetimibe raw material. Methods: A combination of the following different analytical technics was employed: Differential Scanning Calorimetry, Thermogravimetric, Scanning Electron Microscopy, X-ray powder diffraction. Results: The results evidenced the crystalline characteristic of ezetimibe. The sample purity was 99.06 % ± 0.02 and the thermal decomposition followed a zero order kinetic, with activation energy of 96.56 kJ mol–1 and Arrhenius frequency factor of 3,442 x 109 min-1. Conclusion: The characterization of ezetimibe together with the non-isothermal kinetic degradation represents important studies for the pharmaceutical area, since it provides crucial information for the pharmacotechnical/quality control/production areas that should establish the specifications necessary to standardize the requirements of the raw material acquire to ensure the batch-to-batch reproducibility.