Claims for Patent: 10,188,632

Summary for Patent: 10,188,632

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 (Wilmington, NC), 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:	15/588,304
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 10,188,632
Patent Claims:	1. A solid pharmaceutical dosage formulation comprising about 20 mg/dose to about 200 mg/dose of 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, about 60-80% by weight of silicified microcrystalline cellulose, about 0.55-0.95% by weight of colloidal silicon dioxide, about 3-7% by weight of crospovidone, about 5-15% mannitol, and about 0.55-0.95% by weight of magnesium stearate, wherein extraction of the formulation with water or saline at 25.degree. C. for up to 12 hours produces a concentration of 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 of less than or approximately 4 mg/ml. 2. The solid pharmaceutical dosage formulation of claim 1, formulated as a tablet or as a capsule. 3. The solid pharmaceutical dosage formulation of claim 1, further comprising a coating selected from a sugar coating, a gelatin coating, a film coating, and an enteric coating. 4. The solid pharmaceutical dosage formulation of claim 3, comprising about 75 mg to about 200 mg of 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. 5. The solid pharmaceutical dosage formulation of claim 3, comprising about 75 mg of 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. 6. The solid pharmaceutical dosage formulation of claim 3, comprising about 100 mg of 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. 7. The solid pharmaceutical dosage formulation of claim 1, wherein the formulation is substantially or completely free of naloxone. 8. The solid pharmaceutical dosage formulation of claim 1, wherein the formulation comprises: about 65-75% by weight of silicified microcrystalline cellulose, about 0.65-0.85% by weight of colloidal silica, about 7.5-12.5% by weight of mannitol, from about 4-6% by weight of crospovidone, and from about 0.65-0.85% by weight of magnesium stearate. 9. The solid pharmaceutical dosage formulation of claim 1, wherein the formulation comprises about 71% by weight of silicified microcrystalline cellulose, about 0.75% by weight of colloidal silica, about 10% by weight of mannitol, about 5% by weight of crospovidone, and about 0.75% by weight of magnesium stearate. 10. The solid pharmaceutical dosage formulation of claim 1, comprising a film coating present at about 2-4% by weight of the pharmaceutical composition. 11. The pharmaceutical composition of claim 10, wherein the film coating is present at about 3% by weight of the pharmaceutical composition. 12. The pharmaceutical composition of claim 10, wherein the film coating is a polyvinyl alcohol (PVA) based film coating. 13. The pharmaceutical composition of claim 1, further comprising at least one inert pharmaceutical excipient selected from a pharmaceutically acceptable dissolution-rate-modifying agent, a pharmaceutically acceptable plasticizer, a pharmaceutically acceptable coloring agent, a pharmaceutically acceptable opacifier, pharmaceutically acceptable anti-oxidant, a pharmaceutically acceptable preservative, a flavorant, a neutralizing agent, a buffering agent and combinations thereof. 14. A pharmaceutical composition comprising: about 75 mg of 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; about 426 mg of silicified microcrystalline cellulose; about 4.5 mg of colloidal silica; about 60 mg of mannitol; about 30 mg of crospovidone; and about 4.5 mg by weight of magnesium stearate; wherein extraction of the composition with water or saline at 25oC for up to 12 hours produces a concentration of 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 of less than or approximately 4 mg/ml. 15. A pharmaceutical composition comprising: about 100 mg of 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; about 568 mg of silicified microcrystalline cellulose; about 6 mg of colloidal silica; about 80 mg of mannitol; about 40 mg of crospovidone; and about 6 mg by weight of magnesium stearate; wherein extraction of the composition with water or saline at 25oC for up to 12 hours produces a concentration of 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 of less than or approximately 4 mg/ml.