Claims for Patent: 11,229,627

Summary for Patent: 11,229,627

Title:	Opioid receptor modulator dosage formulations
Abstract:	Abuse deterrent solid dosage formulations containing 5-({[2-Amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid, and processes for the preparation and administration of these formulations.
Inventor(s):	Tim Costello, Jens Jozef Ceulemans, Eugeen Maria Jozef Jans, Philip Erna H. Heyns
Assignee:	Allergan Holdings ULC
Application Number:	US17/507,091
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 11,229,627
Patent Claims:	1. A pharmaceutical tablet comprising: about 75 mg or about 100 mg of 5-({[(2S)-2-Amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[(1S)-1-(4-phenyl-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid; about 70-90% by weight of a combination of a first filler and a second filler; about 3-7% by weight disintegrant; about 0.55-0.95% by weight colloidal silicon dioxide; and about 0.45-1% by weight lubricant; wherein the first filler is mannitol; and wherein the tablet comprises at least 10% by weight mannitol. 2. The tablet of claim 1, wherein the second filler is silicified microcrystalline cellulose. 3. The tablet of claim 1, wherein the disintegrant is crospovidone. 4. The tablet of claim 1, comprising about 5% by weight disintegrant. 5. The tablet of claim 4, comprising about 100 mg of 5-({[(2S)-2-Amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[(1S)-1-(4-phenyl-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid. 6. The tablet of claim 5, comprising about 0.75% by weight colloidal silicon dioxide and about 0.75% by weight lubricant, wherein the lubricant is magnesium stearate. 7. The tablet of claim 5, wherein the disintegrant is crospovidone. 8. The tablet of claim 7, comprising about 0.75% by weight colloidal silicon dioxide and about 0.75% by weight lubricant. 9. The tablet of claim 8, wherein the lubricant is magnesium stearate. 10. The tablet of claim 1, comprising: about 100 mg of 5-({[(2S)-2-Amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[(1S)-1-(4-phenyl-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid; about 560 mg-720 mg of the combination of the first filler and the second filler; about 24 mg-56 mg disintegrant; about 4.4 mg-7.6 mg colloidal silicon dioxide; and about 3.6 mg-8 mg lubricant; wherein the first filler is mannitol; and wherein the tablet comprises at least 80 mg mannitol. 11. The tablet of claim 10, comprising about 40 mg disintegrant. 12. The tablet of claim 11, comprising about 6 mg colloidal silicon dioxide and about 6 mg lubricant, wherein the lubricant is magnesium stearate. 13. The tablet of claim 11, wherein the disintegrant is crospovidone. 14. The tablet of claim 13, comprising about 6 mg colloidal silicon dioxide and about 6 mg lubricant. 15. The tablet of claim 14, wherein the lubricant is magnesium stearate. 16. The tablet of claim 4, comprising about 75 mg of 5-({[(2S)-2-Amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[(1S)-1-(4-phenyl-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid. 17. The tablet of claim 16, comprising about 0.75% by weight colloidal silicon dioxide and about 0.75% by weight lubricant. 18. The tablet of claim 17, wherein the lubricant is magnesium stearate. 19. The tablet of claim 16, wherein the disintegrant is crospovidone. 20. The tablet of claim 19, comprising about 0.75% by weight colloidal silicon dioxide and about 0.75% by weight lubricant. 21. The tablet of claim 20, wherein the lubricant is magnesium stearate. 22. The tablet of claim 1, comprising: about 75 mg of 5-({[(2S)-2-Amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[(1S)-1-(4-phenyl-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid; about 420 mg-540 mg of the combination of the first filler and the second filler; about 24 mg-42 mg disintegrant; about 3.3 mg-5.7 mg colloidal silicon dioxide; and about 2.7 mg-6 mg lubricant, wherein the lubricant is magnesium stearate; wherein the first filler is mannitol; and wherein the tablet comprises at least 10% by weight mannitol. 23. The tablet of claim 22, comprising about 40 mg disintegrant. 24. The tablet of claim 23, comprising about 4.5 mg colloidal silicon dioxide and about 4.5 mg magnesium stearate. 25. The tablet of claim 22, comprising about 30 mg disintegrant, wherein the disintegrant is crospovidone. 26. The tablet of claim 25, comprising about 4.5 mg colloidal silicon dioxide and about 4.5 mg of magnesium stearate. 27. A pharmaceutical tablet comprising: about 75 mg or about 100 mg of 5-({[(2S)-2-Amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[(1S)-1-(4-phenyl-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid; about 60-80% by weight filler; about 7.5-12.5% by weight mannitol; about 3-7% by weight disintegrant; colloidal silicon dioxide; and about 0.45-1% by weight magnesium stearate. 28. The tablet of claim 27, wherein the filler is silicified microcrystalline cellulose and the tablet comprises about 0.55-0.95% by weight colloidal silicon dioxide. 29. The tablet of claim 28, wherein the disintegrant is crospovidone. 30. The tablet of claim 27, wherein the filler is silica fine microcrystalline cellulose and the disintegrant is crospovidone.