US2014179749A1PendingUtilityA1
Formulations of enzalutamide
Est. expirySep 11, 2032(~6.1 yrs left)· nominal 20-yr term from priority
Inventors:Douglas Alan LorenzSanjay KonagurthuRandy J. WaldJason A. EverettSheila MatzYuuki TakaishiToshiro SakaiRyousuke IrieShinsuke ObaHiroyasu ToyotaKoji NishimuraAtsushi Kanbayashi
A61P 43/00A61P 35/00A61K 9/1652A61P 15/00A61P 15/14A61P 15/08A61P 13/08A61K 31/4164C07D 233/86A61K 47/32A61K 9/2054A61K 9/2095A61K 47/38A61K 31/4166A61K 9/16A61K 9/10A61K 9/146A61K 9/2027A61K 9/1635
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Claims
Abstract
This disclosure provides formulations of enzalutamide and their use for treating hyperproliferative disorders.
Claims
exact text as granted — not AI-modified1 - 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.Join the waitlist — get patent alerts
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