JP-2022532935-A5 -

Dates

Publication Date

20230515

Application Date

20200522

Description

Unless otherwise specified, all figures used in the specification and claims, such as amounts of components and reaction conditions, should be understood in all cases to be modified by the term "approximately." Therefore, unless otherwise indicated, the numerical parameters described herein and in the appended claims are approximations that may vary depending on the desired properties to be obtained by this disclosure. In certain embodiments, for example, the following are provided: (Item 1) A pharmaceutical composition comprising a solid dispersion, The solid dispersion is The compound represented by the following: or a pharmaceutically acceptable salt thereof, Contains polymers, The solid dispersion comprises a pharmaceutical composition containing about 10% to about 50% by weight of the compound or a pharmaceutically acceptable salt thereof, and about 40% to about 90% by weight of the polymer. (Item 2) The pharmaceutical composition according to item 1, wherein the solid dispersion comprises about 15% to about 30% by weight of the compound or a pharmaceutically acceptable salt thereof, and about 70% to about 90% by weight of the polymer. (Item 3) The pharmaceutical composition according to item 1 or 2, wherein the polymer is a methacrylate polymer or a cellulose polymer. (Item 4) The pharmaceutical composition according to any one of items 1 to 3, wherein the polymer is selected from the group consisting of poly(methacrylate-comethyl methacrylate), hypromellose acetate succinate, and hydroxypropyl methylcellulose phthalate. (Item 5) The pharmaceutical composition according to any one of items 1 to 4, wherein the solid dispersion is a spray-dried solid dispersion. (Item 6) The pharmaceutical composition according to any one of items 1 to 5, wherein the solid dispersion is substantially an amorphous solid dispersion. (Item 7) The pharmaceutical composition according to any one of items 1 to 5, wherein the solid dispersion is an amorphous solid dispersion. (Item 8) The pharmaceutical composition according to item 6 or 7, wherein the solid dispersion has a single Tg . (Item 9) The pharmaceutical composition according to item 8, wherein the solid dispersion is stable for at least four weeks. (Item 10) The pharmaceutical composition according to any one of items 1 to 9, wherein the pharmaceutical composition further comprises an excipient. (Item 11) The pharmaceutical composition according to item 10, wherein the solid dispersion further comprises an excipient. (Item 12) The pharmaceutical composition according to item 10 or 11, wherein the excipient is selected from the group consisting of fillers, sweeteners, diluents, binders, lubricants, disintegrants, and flow promoters. (Item 13) The pharmaceutical composition according to item 10 or 11, wherein the excipient is selected from the group consisting of microcrystalline cellulose, mannitol, talc, croscarmellose sodium, magnesium stearate, and sodium lauryl sulfate. (Item 14) The pharmaceutical composition according to item 10 or 11, further comprising a coloring agent, a fragrance, or a flavoring agent. (Item 15) The pharmaceutical composition according to any one of items 1 to 14, wherein the pharmaceutical composition is in a dosage form selected from the group consisting of granules, pellets, tablets, particles, and mini-tablets. (Item 16) The pharmaceutical composition according to any one of items 1 to 15, wherein the pharmaceutical composition comprises a pharmaceutically effective amount of the compound or a pharmaceutically acceptable salt thereof. (Item 17) The pharmaceutical composition according to any one of items 1 to 16, wherein the pharmaceutical composition is a dosage form comprising about 75 mg to about 125 mg of the compound or a pharmaceutically acceptable salt thereof. (Item 18) A method for treating hepatitis B (HBV) in a patient requiring treatment for HBV, comprising administering to the patient a therapeutically effective amount of a pharmaceutical composition described in any one of items 1 to 17. (Item 19) A method for preparing a pharmaceutical composition, Combining 11-oxo-N-((2-(trifluoromethyl)thiazole-5-yl)methyl)-10,11-dihydrodibenzo[b,f][1,4]thiazepine-8-carboxamide 5,5-dioxide, or a pharmaceutically acceptable salt thereof, and a polymer in a solvent to form a mixture, The mixture is dried to form a solid dispersion, A method comprising, if necessary, combining the solid dispersion with an excipient. (Item 20) The method according to item 19, wherein drying the mixture includes spray-drying the mixture. (Item 21) The method according to item 19 or 20, wherein the solvent includes water. (Item 22) The method according to any one of items 19 to 21, wherein the solvent includes an organic solvent. (Item 23) The method according to any one of items 19 to 22, wherein the solvent comprises acetone and water. (Item 24) The method according to any one of items 19 to 23, wherein the polymer is selected from the group consisting of