(trimethoxyphenylamino) pyrimidinyl formulations
View Patent ↗There are provided pharmaceutical compositions comprising greater than 15% w/w of a compound of Formula (I) as defined herein and/or hydrate thereof and an amount of one or more effervescent agents that is sufficient to provide satisfactory in vitro dissolution; and further comprising one or more pharmaceutically acceptable ingredients; and to processes for obtaining them.
1. A method of treating a patient for rheumatoid arthritis, which method comprises administering to said patient a pharmaceutical composition comprising greater than 15% w/w of the compound of Formula (I):
and/or a hydrate thereof;
wherein each X + represents a monovalent cation; and
an amount of one or more effervescent agents sufficient to provide satisfactory in vitro dissolution of said compound at low pH; and
further comprising one or more pharmaceutically acceptable ingredients.
2. The method according to claim 1 wherein each X + in the compound of Formula (I) represents a sodium cation (Na + ).
3. The method according to claim 1 wherein the compound of Formula (I) is in the form of a hexahydrate.
4. A method of treating a patient for cancer, which method comprises administering to said patient a pharmaceutical composition comprising greater than 15% w/w of the compound of Formula (I):
and/or a hydrate thereof;
wherein each X + represents a monovalent cation; and
an amount of one or more effervescent agents sufficient to provide satisfactory in vitro dissolution of said compound at low pH; and
further comprising one or more pharmaceutically acceptable ingredients.
5. The method according to claim 4 wherein each X + in the compound of Formula (I) represents a sodium cation (Na + ).
6. The method according to claim 4 wherein the compound of Formula (I) is in the form of a hexahydrate.
7. A method of treating a patient for systemic lupus erythematosus, which method comprises administering to said patient a pharmaceutical composition comprising greater than 15% w/w of the compound of Formula (I):
and/or a hydrate thereof;
wherein each X + represents a monovalent cation; and
an amount of one or more effervescent agents sufficient to provide satisfactory in vitro dissolution of said compound at low pH; and
further comprising one or more pharmaceutically acceptable ingredients.
8. The method according to claim 7 wherein each X + in the compound of Formula (I) represents a sodium cation (Na + ).
9. The method according to claim 7 wherein the compound of Formula (I) is in the form of a hexahydrate.
10. A method of treating a patient for rheumatoid arthritis, which method comprises administering to said patient unit dosage form comprising greater than or equal to 60 mg of the compound of Formula (I):
and/or a hydrate thereof;
wherein each X + represents a monovalent cation; and
less than or equal to 110 mg of one or more effervescent agents sufficient to provide satisfactory in vitro dissolution of said compound at low pH; and
further comprising one or more pharmaceutically acceptable ingredients.
11. The method according to claim 10 wherein each X + in the compound of Formula (II) represents a sodium cation (Na + ).
12. The method according to claim 10 wherein the compound of Formula (II) is in the form of a hexahydrate.
13. A method of treating a patient for cancer, which method comprises administering to said patient unit dosage form comprising greater than or equal to 60 mg of the compound of Formula (I):
and/or a hydrate thereof;
wherein each X + represents a monovalent cation; and
less than or equal to 110 mg of one or more effervescent agents sufficient to provide satisfactory in vitro dissolution of said compound at low pH; and
further comprising one or more pharmaceutically acceptable ingredients.
14. The method according to claim 13 wherein each X + in the compound of Formula (II) represents a sodium cation (Na + ).
15. The method according to claim 13 wherein the compound of Formula (II) is in the form of a hexahydrate.
16. A method of treating a patient for systemic lupus erythematosus, which method comprises administering to said patient unit dosage form comprising greater than or equal to 60 mg of the compound of Formula (I):
and/or a hydrate thereof;
wherein each X + represents a monovalent cation; and
less than or equal to 110 mg of one or more effervescent agents sufficient to provide satisfactory in vitro dissolution of said compound at low pH; and
further comprising one or more pharmaceutically acceptable ingredients.
17. The method according to claim 16 wherein each X + in the compound of Formula (II) represents a sodium cation (Na + ).
18. The method according to claim 16 wherein the compound of Formula (II) is in the form of a hexahydrate.
19. A method of treating a patient for immune thrombocytic purpura, which method comprises administering to said patient a pharmaceutical composition comprising greater than 15% w/w of the compound of Formula (I):
and/or a hydrate thereof;
wherein each X + represents a monovalent cation; and
an amount of one or more effervescent agents sufficient to provide satisfactory in vitro dissolution of said compound at low pH; and
further comprising one or more pharmaceutically acceptable ingredients.
20. The method according to claim 19 wherein each X + in the compound of Formula (I) represents a sodium cation (Na + ).
21. The method according to claim 19 wherein the compound of Formula (I) is in the form of a hexahydrate.
22. A method of treating a patient for immune thrombocytic purpura, which method comprises administering to said patient unit dosage form comprising greater than or equal to 60 mg of the compound of Formula (I):
and/or a hydrate thereof;
wherein each X + represents a monovalent cation; and
less than or equal to 110 mg of one or more effervescent agents sufficient to provide satisfactory in vitro dissolution of said compound at low pH; and
further comprising one or more pharmaceutically acceptable ingredients.
23. The method according to claim 22 wherein each X + in the compound of Formula (II) represents a sodium cation (Na + ).
24. The method according to claim 22 wherein the compound of Formula (II) is in the form of a hexahydrate.