Pazopanib formulation

1. A composition suitable for reconstitution into an aqueous suspension, comprising 35.0 to 50.0 w/w % micronized 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide hydrochloride, guar gum, wherein said guar gum is present as from 3% to 12% by weight of the weight of the composition, and polyvinylpyrrolidone, wherein said polyvinylpyrrolidone is present as from 2% to 14% by weight of the weight of the composition.

2. A composition according to claim 1 wherein said guar gum is present as from 3% to 8% by weight of the weight of the composition.

3. A composition according to claim 1 wherein said micronized 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide hydrochloride has a particle size distribution such that more than 90% of the particles are between 0.61 and 10.0 microns.

4. A composition according to claim 1 wherein when said composition is reconstituted into an aqueous suspension, it has a pH of from 3.0 to 4.2.

5. A composition according to claim 4 wherein when said composition is reconstituted into an aqueous suspension, it has a pH of from 3.5 to 4.0.

6. Direct blend powder for use in a pharmaceutical composition, comprising

i) 35.0 to 50.0 w/w % micronized 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide hydrochloride,

ii) 3% to 12% w/w guar gum as a thickening agent,

iii) 2% to 14% w/w polyvinylpyrrolidone (PVP) as a suspending agent,

iv) surfactant,

v) buffer,

vi) preservative,

vii) anti-adherent or glidant,

viii) sweetener, and

ix) flavor.

7. The powder of claim 6 , comprising

i) 35.0 to 50.0 w/w % micronized 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide hydrochloride,

ii) 3.0 to 8.0 w/w % guar gum as a thickening agent,

iii) 3.0 to 12.0 w/w % polyvinylpyrrolidone (PVP) as a suspending agent,

iv) 0.02 to 0.55 w/w % Polysorbate 80 as a surfactant,

v) about 4.7 w/w % citric acid and about 4.0 w/w % sodium phosphate as buffer,

vi) 1.2 to 2.0 w/w % methylparaben as an antimicrobial preservative,

vii) 0.32 to 0.64 w/w % colloidal silicon dioxide as an anti-adherent,

viii) 5.0 to 11.0 w/w % sucralose and 18.0 to 30.0 w/w % mannitol as a sweetener, and

ix) 1.0 to 4.0 w/w % lemon flavor.

8. The powder of claim 7 , consisting of

i) 35.0 to 50.0 w/w % micronized 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide hydrochloride,

ii) 3.0 to 8.0 w/w % guar gum as a thickening agent,

iii) 3.0 to 12.0 w/w % polyvinylpyrrolidone (PVP) as a suspending agent,

iv) 0.02 to 0.55 w/w % Polysorbate 80 as a surfactant,

v) about 4.7 w/w % citric acid and about 4.0 w/w % sodium phosphate as buffer,

vi) 1.2 to 2.0 w/w % methylparaben as an antimicrobial preservative,

vii) 0.32 to 0.64 w/w % colloidal silicon dioxide as an anti-adherent,

viii) 5.0 to 11.0 w/w % sucralose and 18.0 to 30.0 w/w % mannitol as a sweetener, and

ix) 1.0 to 4.0 w/w % lemon flavor.

9. An oral suspension pharmaceutical formulation, comprising

i) 35.0 to 50.0 w/w % micronized 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide hydrochloride,

ii) 3% to 12% w/w guar gum as a thickening agent,

iii) 2% to 14% w/w polyvinylpyrrolidone (PVP) as a suspending agent,

iv) surfactant,

v) buffer,

vi) preservative,

vii) anti-adherent,

viii) sweetener,

ix) flavor, and

x) water.

10. An oral suspension comprising

a) a direct blend powder comprising

i) 35.0 to 50.0 w/w % micronized 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide hydrochloride,

ii) 3.0 to 8.0 w/w % guar gum as a thickening agent,

iii) 3.0 to 12.0 w/w % polyvinylpyrrolidone (PVP) as a suspending agent,

iv) 0.02 to 0.55 w/w % Polysorbate 80 as a surfactant,

v) about 4.7 w/w % citric acid and about 4.0 w/w % sodium phosphate as buffer,

vi) 1.2 to 2.0 w/w % methylparaben as an antimicrobial preservative,

vii) 0.32 to 0.64 w/w % colloidal silicon dioxide as an anti-adherent,

viii) 5.0 to 11.0 w/w % sucralose and 18.0 to 30.0 w/w % mannitol as a sweetener, and

ix) 1.0 to 4.0 w/w % lemon flavor, and

b) purified water.

11. The powder of claim 6 , comprising

i) 35.0 to 50.0 w/w % micronized 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide hydrochloride,

ii) 12.0 to 20.0 w/w % platform placebo granules (containing guar gum, polysorbate 80, and mannitol) as a thickening agent,

iii) 3.0 to 12.0 w/w % polyvinylpyrrolidone (PVP) as a suspending agent,

iv) about 4.7 w/w % citric acid and about 4.0 w/w % sodium phosphate as buffer,

v) 5.0 to 11.0 w/w % sucralose and 10.0 to 20.0 w/w % mannitol as a sweetener,

vi) 1.2 to 2.0 w/w % methylparaben as an antimicrobial preservative,

vii) 0.32 to 0.64 w/w % colloidal silicon dioxide as an anti-adherent,

viii) and 1.0 to 4.0 w/w % lemon flavor.

12. The powder of claim 6 , consisting of

i) 35.0 to 50.0 w/w % micronized 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide hydrochloride,

ii) 3.0 to 12.0 w/w % guar gum as a thickening agent,

iii) 0.5 to 4.0 w/w % Hypromellos (HPMC) as a suspending agent,

iv) about 4.7 w/w % citric acid and about 4.0 w/w % sodium phosphate as buffer,

v) 1.2 to 2.0 w/w % methylparaben as an antimicrobial preservative,

vi) 0.32 to 0.64 w/w % colloidal silicon dioxide as an anti-adherent,

vii) 5.0 to 14.0 w/w % sucralose and 18.0 to 30.0 w/w % mannitol as a sweetener, and

viii) 1.0 to 4.0 w/w % lemon flavor.