Opioid receptor modulator dosage formulations
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.
1. An abuse-deterrent, mono-phasic pharmaceutical tablet comprising:
about 75 mg of 5-({[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 filler;
about 2-8% by weight disintegrant;
about 10% by weight mannitol; and
optionally, a glidant and/or lubricant.
2. The tablet of claim 1 , comprising about 65-75% by weight filler, and about 10% by weight mannitol.
3. The tablet of claim 2 , further comprising a glidant.
4. The tablet of claim 3 , wherein the glidant is colloidal silica.
5. The tablet of claim 4 , wherein the colloidal silica is present in an amount of about 0.55-0.95% by weight.
6. The tablet of claim 2 , further comprising a lubricant, wherein the lubricant is magnesium stearate.
7. The tablet of claim 6 , wherein the magnesium stearate is present in an amount of about 0.45-1.0% by weight.
8. The tablet of claim 3 , further comprising a lubricant, wherein the lubricant is magnesium stearate.
9. The tablet of claim 8 , wherein the magnesium stearate is present in an amount of about 0.45-1.0% by weight.
10. The tablet of claim 1 , wherein the disintegrant is crospovidone.
11. An abuse-deterrent, mono-phasic 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 390 mg 450 mg filler;
about 12 mg 48 mg disintegrant;
about 60 mg of mannitol;
colloidal silica; and
magnesium stearate.
12. The tablet of claim 11 , wherein the filler is silicified microcrystalline cellulose, and the disintegrant is crospovidone.
13. An abuse-deterrent, mono-phasic 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 filler;
about 2-8% by weight disintegrant;
about 10% by weight mannitol; and
optionally, a glidant and/or lubricant.
14. The tablet of claim 13 , comprising about 65-75% by weight filler, and about 10% by weight mannitol.
15. The tablet of claim 14 , further comprising a glidant.
16. The tablet of claim 15 , wherein the glidant is colloidal silica.
17. The tablet of claim 16 , wherein the colloidal silica is present in an amount of about 0.55-0.95% by weight.
18. The tablet of claim 14 , further comprising a lubricant, wherein the lubricant is magnesium stearate.
19. The tablet of claim 18 , wherein the magnesium stearate is present in an amount of about 0.45-1.0% by weight.
20. The tablet of claim 15 , further comprising a lubricant, wherein the lubricant is magnesium stearate.
21. The tablet of claim 20 , wherein the magnesium stearate is present in an amount of about 0.45-1.0% by weight.
22. The tablet of claim 13 , wherein the disintegrant is crospovidone.
23. An abuse-deterrent, mono-phasic 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 520 mg-600 mg of filler;
about 16 mg-64 mg of disintegrant;
about 80 mg of mannitol;
colloidal silica; and
magnesium stearate.
24. The tablet of claim 23 , wherein the filler is silicified microcrystalline cellulose, and the disintegrant is crospovidone.