Patent No. EP3725778 (titled "Formulations Of Enzalutamide") was filed by Astellas Pharma on Sep 11, 2013. The application was issued on Aug 18, 2021.
Pharmaceutical compositions of enzalutamide, an androgen receptor signaling inhibitor, that have improved solubility and absorption compared to crystalline enzalutamide. The compositions contain amorphous enzalutamide dispersed in a polymer called hydroxypropyl methylcellulose acetate succinate (HPMCAS). This polymer enhances enzalutamide concentration in solution. The amorphous enzalutamide dispersion provides higher maximum drug concentration (MDC) and area under the curve (AUC) in dissolution tests. The compositions also have rapid disintegration and dispersibility properties. The process involves preparing the amorphous enzalutamide dispersion, mixing/granulating it, and tableting.

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