Claims for Patent: 11,160,792

Summary for Patent: 11,160,792

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):	Costello; Tim (Rockville, MD), Ceulemans; Jens Jozef (Beerse, BE), Jans; Eugeen Maria Jozef (Beerse, BE), Heyns; Philip Erna H. (Beerse, BE)
Assignee:	Allergan Holdings Unlimited Company (Dublin, IE)
Application Number:	17/211,274
Patent Claims:	1. A pharmaceutical tablet 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 60-80% by weight silicified microcrystalline cellulose; crospovidone; and about 5-15% by weight mannitol. 2. The tablet of claim 1, comprising about 65-75% by weight silicified microcrystalline cellulose, and about 7.5-12.5% by weight mannitol. 3. The tablet of claim 2, comprising about 3-7% by weight crospovidone and further comprising a lubricant. 4. The tablet of claim 3, wherein the lubricant is magnesium stearate present in an amount of about 0.55-0.95% by weight. 5. 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; about 390 mg-450 mg of silicified microcrystalline cellulose; about 18 mg-42 mg crospovidone; about 45 mg-75 mg of mannitol; and about 3.3 mg-5.7 mg of magnesium stearate. 6. The tablet of claim 5, 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 390 mg-450 mg of silicified microcrystalline cellulose; about 30 mg of crospovidone; about 60 mg of mannitol; and about 4.5 mg of magnesium stearate. 7. The tablet of claim 2, further comprising a glidant, wherein the glidant is colloidal silicon dioxide present in an amount of about 0.55-0.95% by weight. 8. The tablet of claim 7, 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 390 mg-450 mg of silicified microcrystalline cellulose; crospovidone; about 45 mg-75 mg of mannitol; and about 3.3 mg-5.7 mg of colloidal silicon dioxide. 9. The tablet of claim 8, 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 390 mg-450 mg of silicified microcrystalline cellulose; crospovidone; about 60 mg of mannitol; and about 4.5 mg of colloidal silicon dioxide. 10. The tablet of claim 2, comprising about 3%-7% by weight crospovidone, and further comprising a glidant and a lubricant. 11. A pharmaceutical tablet 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 60-80% by weight silicified microcrystalline cellulose, crospovidone, and about 5-15% by weight mannitol. 12. The tablet of claim 11, comprising about 65-75% by weight silicified microcrystalline cellulose, and about 7.5-12.5% by weight mannitol. 13. The tablet of claim 12, comprising about 3-7% by weight crospovidone and further comprising a lubricant. 14. The tablet of claim 13, wherein the lubricant is magnesium stearate present in an amount of about 0.55-0.95% by weight. 15. The tablet of claim 14, 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 520 mg-600 mg of silicified microcrystalline cellulose; about 24 mg-56 mg crospovidone; about 60 mg-100 mg of mannitol; and about 4.4 mg-7.6 mg of magnesium stearate. 16. The tablet of claim 13, 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 520 mg-600 mg of silicified microcrystalline cellulose; about 40 mg of crospovidone; about 80 mg of mannitol; and about 6 mg of magnesium stearate. 17. The tablet of claim 12, further comprising a glidant, wherein the glidant is colloidal silicon dioxide present in an amount of about 0.55-0.95% by weight. 18. The tablet of claim 17, 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 520 mg-600 mg of silicified microcrystalline cellulose; crospovidone; about 60 mg-100 mg of mannitol; and about 4.4 mg-7.6 mg of colloidal silicon dioxide. 19. The tablet of claim 18, 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 520 mg-600 mg of silicified microcrystalline cellulose; crospovidone; about 80 mg of mannitol; and about 6 mg of colloidal silicon dioxide. 20. The tablet of claim 12, comprising about 3%-7% by weight crospovidone, and further comprising a glidant and a lubricant. 21. The tablet of claim 20, wherein the glidant is colloidal silicon dioxide and the lubricant is magnesium stearate. 22. The tablet of claim 21, comprising: 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 65-75% by weight silicified microcrystalline cellulose; about 4-6% crospovidone; about 7.5-12.5% by weight mannitol; and colloidal silicon dioxide and magnesium stearate. 23. The tablet of claim 21, 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 520 mg-600 mg of silicified microcrystalline cellulose; about 24 mg-56 mg of crospovidone; about 60 mg-100 mg of mannitol; and colloidal silicon dioxide and magnesium stearate. 24. The tablet of claim 23, 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 520 mg-600 mg of silicified microcrystalline cellulose; about 40 mg of crospovidone; about 80 mg of mannitol; and colloidal silicon dioxide and magnesium stearate. 25. The tablet of claim 10, wherein the glidant is colloidal silicon dioxide and the lubricant is magnesium stearate. 26. The tablet of claim 25, comprising: 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 65-75% by weight silicified microcrystalline cellulose; about 4-6% crospovidone; about 7.5-12.5% by weight mannitol; and colloidal silicon dioxide and magnesium stearate. 27. The tablet of claim 25, 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 390 mg-450 mg of silicified microcrystalline cellulose; about 18 mg-42 mg of crospovidone; about 45 mg-75 mg of mannitol; and colloidal silicon dioxide and magnesium stearate. 28. The tablet of claim 27, 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 390 mg-450 mg of silicified microcrystalline cellulose; about 30 mg of crospovidone; about 60 mg of mannitol; and colloidal silicon dioxide and magnesium stearate.