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Last Updated: March 29, 2024

Claims for Patent: 8,263,122


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Summary for Patent: 8,263,122
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 (Fremont, CA), Lo; Ray (San Leandro, CA)
Assignee: Rigel Pharmaceuticals, Inc. (South San Francisco, CA)
Application Number:12/266,337
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 8,263,122
Patent Claims: 1. A formulation comprising water, (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-dimethyl-3-oxo-2H-pyrido[3,2-b][1,4]oxazin-4(3H)- -yl)methyl phosphate disodium salt during granulation, tablet formation and/or storage, wherein said 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 tablet comprising water, a therapeutically effective amount of (6-(5-fluoro-2-(3,4,5-trimethoxyphenylamino) pyrimidin-4-ylamino)-2,2-dimethyl-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-trimethoxyphenylamino) pyrimidin-4-ylamino)-2,2-dimethyl-3-oxo-2H-pyrido[3,2-b][1,4]oxazin-4(3H)- -yl)methyl phosphate disodium salt, wherein said tablet has a hardness in the range of about 6 kp to about 30 kp.

9. The tablet of claim 8, wherein said tablet exhibits at least 75% dissolution in less than 45 minutes in an aqueous solution maintained at pH 7.4, a temperature of 37.degree. C.+0.5.degree. C., and a paddle speed of 75 rpm.

10. The tablet of claim 8 which further comprises at least one of a filler, a lubricant, a suspending/dispersing agent, a binding agent, and a disintegrant.

11. The tablet of any of claim 8, 9 or 10, wherein the tablet comprises from greater than 25 mg to about 200 mg of (6-(5-fluoro-2-(3,4,5-trimethoxyphenylamino) pyrimidin-4-ylamino)-2,2-dimethyl-3-oxo-2H-pyrido[3,2-b][1,4]oxazin-4(3H)- -yl)methyl phosphate disodium salt.

12. The tablet of claim 11, wherein the tablet comprises about 50 mg to about 100 mg of (6-(5-fluoro-2-(3,4,5-trimethoxyphenylamino) pyrimidin-4-ylamino)-2,2-dimethyl-3-oxo-2H-pyrido[3,2-b][1,4]oxazin-4(3H)- -yl)methyl phosphate disodium salt.

13. The tablet of claim 12, wherein the tablet comprises about 100 mg of (6-(5-fluoro-2-(3,4,5-trimethoxyphenylamino) pyrimidin-4-ylamino)-2,2-dimethyl-3-oxo-2H-pyrido[3,2-b][1,4]oxazin-4(3H)- -yl)methyl phosphate disodium salt.

14. A formulation comprising a therapeutically effective amount of Compound 1, a water sequestering agent, a lubricant, and about 5% to about 11% water, wherein the water sequestering agent is present in an amount sufficient to inhibit decomposition of Compound 1.

15. The formulation of claim 14, wherein the formulation has a bulk density of between about 0.35 to about 0.65 g/mL.

16. A tablet formed by compressing the wet granulated formulation of claim 14.

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