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Last Updated: March 29, 2024

Claims for Patent: 8,652,492


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Summary for Patent: 8,652,492
Title:Wet granulation using a water sequestering agent
Abstract: Disclosed are tablets comprising hydrolytically stable formulations of (6-(5-fluoro-2-(3,4,5-trimethoxyphenylamino)pyrimidin-4-ylamino)-2,2-dime- thyl-3-oxo-2H-pyrido[3,2-b][1,4]oxazin-4(3H)-yl)methyl phosphate disodium salt (Compound 1) prepared by a wet granulation process.
Inventor(s): Sun; Thomas (Palo Alto, CA), Lo; Ray J. (San Leandro, CA)
Assignee: Rigel Pharmaceutical, Inc. (South San Francisco, CA)
Application Number:13/738,458
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 8,652,492
Patent Claims: 1. A wet granulated formulation comprising water, a therapeutically effective amount of (6-(5-fluoro-2-(3,4,5-trimethoxyphenylamino)pyrimidin-4-ylamino)-2,2-dime- thyl-3-oxo-2H-pyrido[3,2-b][1,4]oxazin-4(3H)-yl)methyl phosphate disodium salt and a sufficient amount of a water sequestering agent to inhibit decomposition of (6-(5-fluoro-2-(3,4,5-trimethoxyphenyl-amino)pyrimidin-4-ylamino)-2,2-dim- ethyl-3-oxo-2H-pyrido[3,2-b][1,4]oxazin-4(3H)-yl)methyl phosphate disodium salt, wherein said wet granulated formulation after drying has a bulk density sufficient to form tablets having a hardness in the range of about 6 kp to about 30 kp.

2. The formulation of claim 1, wherein after drying the formulation has a bulk density of between about 0.35 to about 0.65 g/mL.

3. The formulation of claim 1, wherein the water sequestering agent is selected from the group consisting of starch, magnesium sulfate, calcium chloride, silica gel, and kaolin.

4. The formulation of claim 3, wherein the water sequestering agent is starch.

5. The formulation of claim 4, wherein the starch is partially pregelatinized.

6. The formulation of claim 5, wherein the starch is derived from Maize.

7. The formulation of claim 1 which further comprises at least one of a filler, a lubricant, a suspending/dispersing agent, a binding agent, and a disintegrant.

8. A wet granulating process, comprising: a) blending a composition comprising (6-(5-fluoro-2-(3,4,5-trimethoxyphenylamino)pyrimidin-4-ylamino)-2,2-dime- thyl-3-oxo-2H-pyrido[3,2-b][1,4]oxazin-4(3H)-yl)methyl phosphate disodium salt and a sufficient amount of a water sequestering agent to inhibit the decomposition of 6-(5-fluoro-2-(3,4,5-trimethoxyphenylamino)pyrimidin-4-ylamino)-2,2-dimet- hyl-3-oxo-2H-pyrido[3,2-b][1,4]oxazin-4(3H)-yl)methyl phosphate disodium salt to form a blended mixture; b) granulating the blended mixture of a) while adding water to form wet granules; c) drying the wet granules of b) at below 65.degree. C. until a loss on drying of between about 5% and 11% is achieved to provide dried granules; and d) blending a lubricant into the dried granules of c) to provide blended granules.

9. The method of claim 8, further comprising: compressing the blended granules to form tablets.

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