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Last Updated: November 28, 2020

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Claims for Patent: 8,518,446

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Summary for Patent: 8,518,446
Title:Coated tablet formulations and uses thereof
Abstract: The present invention provides coated tablet formulations comprising neratinib maleate, and improved methods for making such coated tablets.
Inventor(s): Ashraf; Muhammad (Elmwood, NJ), Mahmud; Mainuddin (Oak Ridge, NJ), Goolcharran; Chimanlall (East Lyme, CT), Ghosh; Krishnendu (Sparkill, NY), Nagi; Arwinder Singh (Moorpark, CA)
Assignee: Wyeth LLC (Madison, NJ)
Application Number:12/940,808
Patent Claims: 1. A pharmaceutically acceptable composition comprising: a granulation comprising intragranular components: (a) 10-70 weight percent neratinib maleate; (b) 15-65 weight percent of one or more fillers; (c) 0-8 weight percent of one or more disintegrants; (d) 0.2-8 weight percent of one or more glidants; and (e) 5-15 weight percent of one or more surface modifying agents; wherein the granulation is combined with extragranular components: (f) 1-25 weight percent of one or more fillers; (g) 0-8 weight percent of one or more disintegrants; and (h) 0.1-3 weight percent of one or more lubricants.

2. A pharmaceutically acceptable composition comprising intragranular components: 10-70 weight percent of neratinib maleate and 5-15 weight percent of povidone; and extragranular components: microcrystalline cellulose, crospovidone and magnesium stearate.

3. A pharmaceutically acceptable composition comprising intragranular components: (a) 10-70 weight percent of neratinib maleate; (b) 15-65 weight percent of mannitol, microcrystalline cellulose or a combination of both; (c) 0.5-8 weight percent crospovidone, croscarmellose sodium or a combination of both; (d) 0.2-8 weight percent colloidal silicon dioxide; and (e) 5-15 weight percent povidone; and extragranular components: (f) 1-25 weight percent of microcrystalline cellulose; (g) 1-8 weight percent of crospovidone; and (h) 0.5-3 weight percent of magnesium stearate.

4. A tablet comprising the composition of claim 3.

5. A dry-filled capsule comprising the composition of claim 3.

6. The composition according to claim 3, wherein the amount of neratinib maleate is about 41 weight percent.

7. The composition according to claim 3, wherein the amount of mannitol and microcrystalline cellulose, as an intragranular component, is about 50 weight percent.

8. The composition according to claim 3, wherein the amount of crospovidone, as an intragranular component, is about 3 weight percent.

9. The composition according to claim 3, wherein the amount of povidone, as an intragranular component, is about 5 weight percent.

10. The composition according to claim 3, in the form of an oral dosage of 40 mg, 80 mg, or 240 mg.

11. A method for preparing a pharmaceutically acceptable composition, comprising: (1) spraying 5-15 weight percent of one or more surface modifying agents onto intragranular components of a granulation, said intragranular components comprising: (a) 10-70 weight percent neratinib maleate; (b) 15-65 weight percent of one or more fillers; (c) 0-8 weight percent of one or more disintegrants; and (d) 0.2-8 weight percent of one or more glidants; and (2) combining said coated intragranular components with extragranular components of the granulation, said extragranular components comprising: (e) 1-25 weight percent of one or more fillers; (f) 0-8 weight percent of one or more disintegrants; and (g) 0.1-3 weight percent of one or more lubricants.

12. The method according to claim 11, wherein the surface modifying agent is povidone.

13. A method for treating cancer comprising administering an effective amount of a composition according to claim 1; wherein the cancer results from an aberrant tyrosine kinase receptor.

14. The composition according to claim 3, wherein the amount of colloidal silicon dioxide, as an intragranular component, is about 2 weight percent.

15. The composition according to claim 3, wherein the amount of neratinib maleate is about 35 weight percent.

16. The pharmaceutically acceptable composition of claim 3, comprising intragranular components: (a) 10-70 weight percent of neratinib maleate; (b) 15-65 weight percent of mannitol and microcrystalline cellulose; (c) 0.5-8 weight percent of crospovidone; (d) 0.2-8 weight percent of colloidal silicon dioxide; and (e) 5-15 weight percent of povidone; and extragranular components: (f) 1-25 weight percent of microcrystalline cellulose; (g) 1-8 weight percent of crospovidone; and (h) 0.5-3 weight percent of magnesium stearate.

17. The pharmaceutically acceptable composition of claim 3, comprising intragranular components: (a) 35 weight percent of neratinib maleate; (b) about 50 weight percent of mannitol and microcrystalline cellulose; (c) 3 weight percent of crospovidone; (d) 2 weight percent of colloidal silicon dioxide; and (e) 5 weight percent of povidone; and extragranular components: (f) 1.5 weight percent of microcrystalline cellulose; (g) 2 weight percent of crospovidone; and (h) 2 weight percent of magnesium stearate.

18. The pharmaceutically acceptable composition of claim 3, comprising 40 mg of neratinib maleate.

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