NOVEL PHARMACEUTICAL COMPOSITION
Disclosed are novel pharmaceutical formulations containing N-{3-p-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide dimethyl sulfoxide solvate, methods of using the compositions in therapy and processes for preparing the same.
1 . A direct powder blend formulation comprising:
a) an amount of a drug, which is N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3- d]pyrimidin-1-yl]phenyl}acetamide dimethyl sulfoxide solvate, and a solubilizer;
wherein,
b) the solubilizer is a combination of between 65 to 70% by weight of the formulation of Sulfobutylether B-Cyclodextrin and between 0.5 to 2% by weight of the formulation of Hypromellose.
2 . (canceled)
3 . (canceled)
4 . A direct powder blend formulation comprising:
a) an amount of a drug, which is N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3- d]pyrimidin-1-yl]phenyl}acetamide dimethyl sulfoxide solvate, a solubilizer, buffer and sweetener:
wherein,
b) the solubilizer is a combination of between 65 to 70% by weight of the formulation of Sulfobutylether B-Cyclodextrin and between 0.5 to 2% by weight of the formulation of Hypromellose; and
c) the particle size distribution of the drug is at least 90% of the particles are from 1 to 20 microns.
5 . (canceled)
6 . An oral solution comprising:
a) an amount of a drug, which is N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3- d]pyrimidin-1-yl]phenyl}acetamide dimethyl sulfoxide solvate, a solubilizer, preservative, buffer, sweetener, and an aqueous vehicle:
wherein,
b) the solubilizer is a combination of between 65 to 70% by weight of the formulation of Sulfobutylether B-Cyclodextrin and between 0.5 to 2% by weight of the formulation of Hypromellose.
7 . An oral solution comprising:
a) an amount of a drug, which is N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3- d]pyrimidin-1-yl]phenyl}acetamide dimethyl sulfoxide solvate, a solubilizer, and an aqueous vehicle:
wherein,
b) the solubilizer is a combination of between 65 to 70% by weight of the formulation of Sulfobutylether B-Cyclodextrin and between 0.5 to 2% by weight of the formulation of Hypromellose.
8 . An oral solution comprising:
a) an amount of a drug, which is N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3- cl]pyrimidin-1-yl]phenyl}acetamide dimethyl sulfoxide solvate, a solubilizer, preservative, buffer, sweetener, flavor, and an aqueous vehicle:
wherein,
b) the solubilizer is a combination of between 65 to 70% by weight of the formulation of Sulfobutylether B-Cyclodextrin and between 0.5 to 2% by weight of the formulation of Hypromellose.
9 . An oral solution comprising:
a) an amount of a drug, which is N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3- d]pyrimidin-1-yl]phenyl}acetamide dimethyl sulfoxide solvate, a solubilizer, preservative, buffer, sweetener, surfactant, flavor, and an aqueous vehicle:
wherein,
b) the solubilizer is a combination of between 65 to 70% by weight of the formulation of Sulfobutylether B-Cyclodextrin and between 0.5 to 2% by weight of the formulation of Hypromellose.
10 . A formulation according to claim 1 for use in the treatment of cancer in a human.
11 . A formulation according to claim 1 for use in inhibiting MEK in a human.
12 . A solution according to claim 6 for use in the treatment of cancer in a human.
13 . A solution according to claim 6 for use in inhibiting MEK in a human.