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Last Updated: March 29, 2024

Claims for Patent: 9,675,587


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Summary for Patent: 9,675,587
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 (IE)
Application Number:13/829,984
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 9,675,587
Patent Claims: 1. 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, from about 0.55-0.95% by weight of magnesium stearate, and a water-soluble, pH-independent film coating, wherein the 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 is present at about 5-20% by weight of the composition, and wherein extraction of the composition 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 abuse deterrent, mono-phasic pharmaceutical composition of claim 1, wherein the composition consists 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 65-75% by weight of silicified microcrystalline cellulose, from about 0.65-0.85% by weight of colloidal silica, from 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.

3. The abuse deterrent, mono-phasic pharmaceutical composition of claim 1, wherein the composition consists 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, 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.

4. The pharmaceutical composition of claim 1, wherein the film coating is present at about 2-4% by weight of the pharmaceutical composition.

5. 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; about 4.5 mg by weight of magnesium stearate; and a water-soluble, pH-independent film coating, wherein extraction of the composition 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.

6. The pharmaceutical composition of claim 5, wherein the film coating is present at about 3% by weight of the pharmaceutical composition.

7. 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; about 6 mg by weight of magnesium stearate; and a water-soluble, pH-independent film coating, wherein extraction of the composition 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.

8. The pharmaceutical composition of claim 7, wherein the film coating is present at about 3% by weight of the pharmaceutical composition.

9. An abuse deterrent, mono-phasic pharmaceutical composition suitable for single dose administration for treating a condition mediated by an opioid receptor comprising: about 100 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 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, about 0.75% by weight of magnesium stearate, and a water-soluble, pH-independent film coating, wherein extraction of the composition 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.

10. The pharmaceutical composition of claim 9, wherein the film coating is present at about 3% by weight of the pharmaceutical composition.

11. The pharmaceutical composition of claim 10, wherein the film coating is a polyvinyl alcohol (PVA) based film coating.

12. An abuse deterrent, mono-phasic pharmaceutical composition suitable for single dose administration for treating a condition mediated by an opioid receptor 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, and a water-soluble, pH-independent film coating, wherein extraction of the composition 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.

13. The pharmaceutical compositions of claim 12, wherein the film coating is present at about 3% by weight of the pharmaceutical composition.

14. The pharmaceutical composition of claim 13, wherein the film coating is a polyvinyl alcohol (PVA) based film coating.

15. The pharmaceutical composition of claim 3 wherein the film coating is present at about 3% by weight of the pharmaceutical composition.

16. The pharmaceutical composition of claim 15 wherein the film coating is a polyvinyl alcohol (PVA) based film coating.

17. The pharmaceutical composition of claim 4 wherein the film coating is a polyvinyl alcohol (PVA) based film coating.

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