Fumarate ester pharmaceutical compositions
Described herein are pharmaceutical compositions comprising fumarate esters, methods for making the same, and methods for treating subjects in need thereof. In particular, oral pharmaceutical compositions comprising fumarate esters are described.
1. An oral immediate release pharmaceutical composition comprising a single phase non-aqueous vehicle comprising about 60 mg to about 200 mg of one or more fumarate esters or salts thereof having the formula:
wherein R 1 and R 2 , may be the same or different, and independently represent hydrogen or a linear, branched, or cyclic, saturated or unsaturated C 1-20 alkyl radical, which may be optionally substituted with halogen, hydroxy, C 1-4 alkoxy, nitro, or cyano.
2. The composition of claim 1 , wherein R 1 is C 1-4 alkyl.
3. The composition of claim 1 , wherein R 1 is methyl.
4. The composition of claim 1 , wherein R 2 is C 1-4 alkyl.
5. The composition of claim 1 , wherein R 2 is methyl.
6. The composition of claim 1 , wherein R 2 is hydrogen.
7. The composition of claim 1 , wherein R 1 is C 1-4 alkyl and R 2 is C 1-4 alkyl.
8. The composition of claim 1 , wherein R 1 is methyl and R 2 is methyl.
9. The composition of claim 1 , wherein R 1 is a C 1-4 alkyl and R 2 is hydrogen.
10. The composition of claim 1 , wherein R 1 is methyl and R 2 is hydrogen.
11. The composition of claim 1 , wherein the fumarate ester is:
12. The composition of claim 1 , wherein the fumarate ester is:
or a salt thereof.
13. The composition of claim 1 , wherein the composition comprises mono- and di-glycerides, polyvinylpyrrolidone, and polyoxyl 40 hydrogenated castor oil.
14. The composition of claim 1 , wherein the composition comprises lactic acid.
15. The composition of claim 1 , wherein the composition comprises about 25% to about 50% of the one or more fumarate esters or salts thereof about 40% to about 54% of mono- and di-glycerides; about 1% to about 10% polyvinylpyrrolidone; about 2% to about 10% polyoxyl 40 hydrogenated castor oil; and about 5% lactic acid.
16. The composition of claim 1 , wherein the composition is encapsulated in a capsule.
17. The composition of claim 1 , wherein the composition is encapsulated in an enteric soft capsule.
18. The composition of claim 17 , wherein the enteric soft capsule provides delayed release of the fumarate ester.
19. The composition of claim 1 , wherein the fumarate ester is in the form of milled or micronized particles.
20. The composition of claim 1 , wherein the composition is stable for at least 1 year at 25° C.