(Z)-2-cyano-3-hydroxy-but-2-enoic acid-(4'-trifluormethylphenyl)-amide tablet formulations with improved stability
AssigneeSanofi
InventorGerrit Hauck
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Abstract
The invention relates to solid pharmaceutical compositions comprising (Z)-2-cyano-3-hydroxy-but-2-enoic acid-(4′-trifluoromethylphenyl)-amide, as well as a process for the preparation of the same, methods of using such compositions to treat subjects suffering from autoimmune diseases in particular systemic lupus erythematosus or chronic graft-versus-host disease, multiple sclerosis or rheumatoid arthritis.
Claims37
A solid pharmaceutical composition comprising
- a) 1% to 30% weight:weight Teriflunomide, or a pharmaceutically acceptable basic addition salt thereof,
- b) 5% to 20% weight:weight disintegrant,
- c) 0% to 40% weight:weight binder,
- d) 0.1% to 2% weight:weight lubricant, and
- e) the remaining percentage comprising diluents;
- wherein the solid pharmaceutical composition does not contain colloidal silicon dioxide.
A solid pharmaceutical composition comprising a therapeutically effective amount of teriflunomide or a pharmaceutically acceptable basic addition salt thereof, wherein the pH of the solid pharmaceutical composition is no more than about 2.2.
A solid pharmaceutical composition comprising a therapeutically effective amount of teriflunomide or a pharmaceutically acceptable basic addition salt thereof, wherein the solid pharmaceutical composition does not contain colloidal silicon dioxide and the solid pharmaceutical composition contains no more than about 0.3% by weight of 2-cyano-N-(4-trifluoromethyl-phenyl)-acetamide after being stored at about 30° C. and about 65% relative humidity for about 12 months.
A solid pharmaceutical composition comprising a therapeutically effective amount of teriflunomide or a pharmaceutically acceptable basic addition salt thereof, wherein the solid pharmaceutical composition does not contain colloidal silicon dioxide and the solid pharmaceutical composition contains no more than about 1.0% by weight of 2-cyano-N-(4-trifluoromethyl-phenyl)-acetamide after being stored at about 30° C. and about 65% relative humidity for about 36 months.
A solid pharmaceutical composition comprising a therapeutically effective amount of teriflunomide or a pharmaceutically acceptable basic addition salt thereof, wherein the solid pharmaceutical composition does not contain colloidal silicon dioxide and the solid pharmaceutical composition contains no more than about 0.3% by weight of 2-cyano-N-(4-trifluoromethyl-phenyl)-acetamide after being stored at about 30° C. and about 75% relative humidity for about 12 months.
Dependencies are inferred from the claim text.