Opioid receptor modulator dosage formulations
AssigneeFuriex Pharmaceuticals, Inc.
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.
Claims29
A solid pharmaceutical dosage formulation comprising 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 an inert ingredient selected from silicified microcrystalline cellulose, colloidal silicon dioxide, crospovidone, mannitol, and magnesium stearate.
A film-coated, oral tablet formulation consisting of about 75 mg to about 200 mg 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 silicified microcrystalline cellulose, colloidal silicon dioxide, crospovidone, mannitol, and magnesium stearate, and an aqueous film coating.
An abuse deterrent, mono-phasic pharmaceutical composition suitable for single dose administration for treating a condition mediated by an opioid receptor consisting essentially of 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, from about 60-80% by weight of silicified microcrystalline cellulose, from about 0.55-0.95% by weight of colloidal silica, from about 5-15% by weight of mannitol, from about 3-7% by weight of crospovidone, and from about 0.55-0.95% by weight of magnesium stearate.
A method of preparing a solid dosage formulation comprising:
- i) blending 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 with the pharmaceutically acceptable inert excipients:
- silicified microcrystalline cellulose, mannitol, colloidal silica and crospovidone;
- and
- ii) forming the dry blend into a solid dosage formulation.
An abuse deterrent, mono-phasic pharmaceutical composition suitable for single dose administration for treating a condition mediated by an opioid receptor consisting essentially of:
- 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.
An abuse deterrent, mono-phasic pharmaceutical composition suitable for single dose administration for treating a condition mediated by an opioid receptor consisting essentially of:
- 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.
Dependencies are inferred from the claim text.