Claims for Patent: 12,059,409

Summary for Patent: 12,059,409

Title:	Pharmaceutical composition for modified release
Abstract:	A pharmaceutical composition for modified release, comprising (1) (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl) amino]ethyl] acetic acid anilide, or a pharmaceutically acceptable salt thereof, (2) at least one additive which ensures penetration of water into the pharmaceutical composition and which has a solubility such that the volume of water required for dissolving 1 g of the additive is 10 mL or less, and (3) a hydrogel-forming polymer having an average molecular weight of approximately 100,000 or more, or a viscosity of 12 mPa·s or more at a 5% aqueous solution at 25 C is disclosed.
Inventor(s):	Yuuki Takaishi, Yutaka Takahashi, Takashi Nishizato, Daisuke Murayama, Emiko Murayama, Soichiro Nakamura, Kazuhiro Sako
Assignee:	Astellas Pharma Inc
Application Number:	US18/613,270
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 12,059,409
Patent Claims:	1. A tablet, comprising 10 mg to 200 mg of (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide, or a pharmaceutically acceptable salt thereof, in a sustained release hydrogel-forming formulation comprising a hydrogel-forming polymer having an average molecular weight of 200,000 to 7,000,000 and an additive having a water solubility of at least 0.1 g/mL at 20+5° C., wherein the hydrogel-forming polymer is polyethylene oxide, wherein the additive is polyethylene glycol, and wherein a drug dissolution rate from the tablet is 39% or less after 1.5 hours, and at least 75% after 7 hours, as measured in accordance with United States Pharmacopoeia in 900 mL of a USP buffer having a pH of 6.8 at a paddle rotation speed of 200 rpm. 2. The tablet according to claim 1, wherein the polyethylene oxide has the average molecular weight of 200,000 to 5,000,000. 3. The tablet according to claim 1, wherein the polyethylene oxide has the average molecular weight of 1,000,000 to 4,000,000. 4. The tablet according to claim 1, wherein the polyethylene oxide has the average molecular weight of 2,000,000 to 4,000,000. 5. The tablet according to claim 1, wherein the polyethylene oxide has the average molecular weight of 2,000,000. 6. The tablet according to claim 1, wherein the polyethylene glycol is selected from the group consisting of PEG 400, PEG 1500, PEG 4000, PEG 6000, and PEG 20000. 7. The tablet according to claim 2, wherein the polyethylene glycol is selected from the group consisting of PEG 400, PEG 1500, PEG 4000, PEG 6000, and PEG 20000. 8. The tablet according to claim 3, wherein the polyethylene glycol is selected from the group consisting of PEG 400, PEG 1500, PEG 4000, PEG 6000, and PEG 20000. 9. The tablet according to claim 4, wherein the polyethylene glycol is selected from the group consisting of PEG 400, PEG 1500, PEG 4000, PEG 6000, and PEG 20000. 10. The tablet according to claim 5, wherein the polyethylene glycol is selected from the group consisting of PEG 400, PEG 1500, PEG 4000, PEG 6000, and PEG 20000. 11. The tablet according to claim 1, wherein the polyethylene glycol is PEG 6000. 12. The tablet according to claim 2, wherein the polyethylene glycol is PEG 6000. 13. The tablet according to claim 3, wherein the polyethylene glycol is PEG 6000. 14. The tablet according to claim 4, wherein the polyethylene glycol is PEG 6000. 15. The tablet according to claim 5, wherein the polyethylene glycol is PEG 6000. 16. The tablet according to claim 1, comprising 10 mg to 200 mg (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide. 17. The tablet according to claim 2, comprising 10 mg to 200 mg (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide. 18. The tablet according to claim 3, comprising 10 mg to 200 mg (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide. 19. The tablet according to claim 4, comprising 10 mg to 200 mg (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide. 20. The tablet according to claim 6, comprising 10 mg to 200 mg (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide. 21. The tablet according to claim 7, comprising 10 mg to 200 mg (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide. 22. The tablet according to claim 8, comprising 10 mg to 200 mg (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide. 23. The tablet according to claim 9, comprising 10 mg to 200 mg (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide. 24. The tablet according to claim 10, comprising 10 mg to 200 mg (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide. 25. The tablet according to claim 11, comprising 10 mg to 200 mg (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide. 26. The tablet according to claim 12, comprising 10 mg to 200 mg (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide. 27. The tablet according to claim 13, comprising 10 mg to 200 mg (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide. 28. The tablet according to claim 14, comprising 10 mg to 200 mg (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide. 29. The tablet according to claim 15, comprising 10 mg to 200 mg (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide.