Coated tablet formulations and uses thereof
The present invention provides coated tablet formulations comprising neratinib maleate, and improved methods for making such coated tablets.
1. A pharmaceutical composition comprising:
(A) intragranular components:
(a) about 35 weight percent of neratinib maleate measured in the amount of neratinib free base;
(b) mannitol;
(c) about 10.6 weight percent of microcrystalline cellulose;
(d) about 3 weight percent of crospovidone;
(e) about 2 weight percent of colloidal silicon dioxide; and
(f) about 5 weight percent of povidone; and
(B) extragranular components:
(g) about 1.5 weight percent of microcrystalline cellulose;
(h) about 2 weight percent of crospovidone; and
(i) about 2 weight percent of magnesium stearate; and
(C) a film-coating.
2. The pharmaceutical composition of claim 1 , comprising about 40 mg of neratinib maleate as measured in the amount of neratinib free base.
3. The pharmaceutical composition of claim 1 , comprising about 12 mg of microcrystalline cellulose as an intragranular component.
4. The pharmaceutical composition of claim 1 , comprising about 240 mg of neratinib maleate as measured in the amount of neratinib free base.
5. The pharmaceutical composition of claim 1 , comprising about 72 mg of microcrystalline cellulose as an intragranular component.
6. The pharmaceutical composition of claim 1 , wherein the composition is formulated as a tablet.
7. The pharmaceutical composition of claim 1 , wherein the composition is formulated as a capsule.
8. The pharmaceutical composition of claim 1 , wherein the composition is formulated as a dry-filled capsule.
9. The pharmaceutical composition of claim 1 , comprising about 3 weight percent of the film-coating.
10. The pharmaceutical composition of claim 1 , wherein the film-coating is a polyvinyl alcohol.
11. The pharmaceutical composition of claim 1 , wherein the film-coating is red, yellow, or pink.
12. The pharmaceutical composition of claim 10 , wherein the film-coating is red, yellow, or pink.
13. A pharmaceutical composition comprising:
(A) intragranular components:
(a) about 42.3 weight percent of neratinib maleate;
(b) mannitol;
(c) about 10.6 weight percent of microcrystalline cellulose;
(d) about 3 weight percent of crospovidone;
(e) about 2 weight percent of colloidal silicon dioxide; and
(f) about 5 weight percent of povidone;
(B) extragranular components:
(g) about 1.5 weight percent of microcrystalline cellulose;
(h) about 2 weight percent of crospovidone; and
(i) about 2 weight percent of magnesium stearate; and
(C) a film-coating.
14. The pharmaceutical composition of claim 13 , comprising about 48.3 mg of neratinib maleate.
15. The pharmaceutical composition of claim 13 , comprising about 289.9 mg of neratinib maleate.
16. The pharmaceutical composition of claim 13 , wherein the composition is formulated as a tablet.
17. The pharmaceutical composition of claim 13 , wherein the composition is formulated as a capsule.
18. The pharmaceutical composition of claim 13 , wherein the composition is formulated as a dry-filled capsule.
19. The pharmaceutical composition of claim 13 , comprising about 3 weight percent of the film-coating.
20. The pharmaceutical composition of claim 13 , wherein the film-coating is a polyvinyl alcohol.
21. The pharmaceutical composition of claim 13 , wherein the film-coating is red, yellow, or pink.
22. The pharmaceutical composition of claim 20 , wherein the film-coating is red, yellow, or pink.
23. A method for treating cancer in a subject, comprising administering to the subject the composition of claim 1 .