Opioid receptor modulator dosage formulations
AssigneeAllergan Holdings Unlimited Company
InventorsTim Costello, Jens Jozef Ceulemans, Eugeen Maria Jozef Jans, Philip Erna H. Heyns
Life of this patent
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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.
Claims16
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 of water or saline at 25° 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.
8-29. (canceled)
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 25° 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.
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 25° 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.
Dependencies are inferred from the claim text.