FORMULATIONS OF ENZALUTAMIDE
This disclosure provides formulations of enzalutamide and their use for treating hyperproliferative disorders.
1 - 82 . (canceled)
83 . A pharmaceutical composition comprising a solid dispersion containing enzalutamide and a polymer.
84 . The pharmaceutical composition according to claim 83 , wherein enzalutamide is an amorphous state.
85 . The pharmaceutical composition according to claim 83 , wherein the polymer is a polymer or two or more polymers selected from the group consisting of polyvinyl pyrrolidone, polyethyleneoxide, poly(vinyl pyrrolidone-co-vinyl acetate), polymethacrylates, polyoxyethylene alkyl ethers, polyoxyethylene castor oils, polycaprolactam, polylactic acid, polyglycolic acid, poly(lactic-glycolic)acid, lipids, cellulose, pullulan, dextran, maltodextrin, hyaluronic acid, polysialic acid, chondroitin sulfate, heparin, fucoidan, pentosan polysulfate, spirulan, hydroxypropyl methyl cellulose, hydroxypropyl cellulose, 10 carboxymethyl ethylcellulose, hydroxypropyl methylcellulose acetate succinate, cellulose acetate phthalate, cellulose acetate trimellitate, ethyl cellulose, cellulose acetate, cellulose butyrate, cellulose acetate butyrate, and dextran polymer derivative.
86 . The pharmaceutical composition according to claim 85 , wherein the polymer is hydroxypropyl methylcellulose acetate succinate.
87 . The pharmaceutical composition according to claim 83 , wherein the amount of the polymer is 0.5 to 3 parts by weight, with respect to 1 part by weight of the enzalutamide.
88 . The pharmaceutical composition according to claim 83 , wherein the amount of the polymer is 3 parts by weight, with respect to 1 part by weight of the enzalutamide.
89 . The pharmaceutical composition according to claim 83 , which the solubility of enzalutamide is twice or more compared to that of enzalutamide.
90 . The pharmaceutical composition according to claim 83 , prepared by a process comprising:
dissolving and/or suspending the compound of enzalutamide and the polymer in a pharmaceutically acceptable solvent, and
removing the solvent by spray drying to prepare the solid dispersion.
91 . A process of manufacturing a pharmaceutical composition comprising a solid dispersion containing enzalutamide and a polymer, comprising:
(1) preparing the solid dispersion of enzalutamide and the polymer,
(2) mixing and/or granulating the solid dispersion, and
(3) tableting the solid dispersion.
92 . A process of manufacturing a pharmaceutical composition according to claim 91 , comprising:
(1) preparing a solid dispersion of enzalutamide and a polymer,
(2) mixing the solid dispersion with one additive or two or more additives and granulating the mixture, and
(3) tableting the granules.
93 . The pharmaceutical composition of claim 83 , which is a tablet.
94 . The pharmaceutical composition of claim 84 , which is a tablet.
95 . The pharmaceutical composition of claim 85 , which is a tablet.
96 . The pharmaceutical composition of claim 86 , which is a tablet.
97 . The pharmaceutical composition of claim 87 , which is a tablet.
98 . The pharmaceutical composition of claim 88 , which is a tablet.
99 . The pharmaceutical composition of claim 89 , which is a tablet.