Opioid receptor modulator dosage formulations

  • US 10,188,632 B2
  • Filed: 05/05/2017
  • Issued: 01/29/2019
  • Est. Priority Date: 03/14/2013
  • Status: Active Grant
First Claim
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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°

  • 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.

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