Claims for Patent: 10,105,335

Summary for Patent: 10,105,335

Title:	Fumarate ester dosage forms
Abstract:	Described herein are pharmaceutical compositions comprising fumarate esters, methods for making the same, and methods for treating subjects in need thereof. In particular, oral controlled release pharmaceutical compositions comprising fumarate esters suspended in liquid matrices are described. One embodiment described herein is a pharmaceutical composition comprising fumarate esters suspended in a lipid or lipophilic liquid with enhanced bioavailability.
Inventor(s):	Vaughn; Jason M. (Browns Summit, NC), Hughey; Justin R. (Asheboro, NC), Roberts; Tanesha (Greensboro, NC), Dyakonov; Tatyana (Greensboro, NC), Agnihotri; Sunil (Scarborough, NC), Fatmi; Aqeel A. (High Point, NC)
Assignee:	Banner Life Sciences LLC (High Point, NC)
Application Number:	15/730,825
Patent Claims:	1. An oral pharmaceutical composition comprising an immediate releasing single phase non-aqueous liquid vehicle and a fumarate ester or a salt thereof having the formula: ##STR00005## wherein R.sub.1 and R.sub.2, may be the same or different, and independently represent hydrogen or a linear, branched, or cyclic, saturated or unsaturated C.sub.1-20 alkyl radical, which may be optionally substituted with halogen, hydroxy, C.sub.1-4 alkoxy, nitro, or cyano. 2. The composition of claim 1, wherein R.sub.1 is C.sub.1-4 alkyl. 3. The composition of claim 1, wherein R.sub.1 is methyl. 4. The composition of claim 1, wherein R.sub.2 is C.sub.1-4 alkyl. 5. The composition of claim 1, wherein R.sub.2 is methyl. 6. The composition of claim 1, wherein R.sub.2 is hydrogen. 7. The composition of claim 1, wherein R.sub.1 is C.sub.1-4 alkyl and R.sub.2 is C.sub.1-4 alkyl. 8. The composition of claim 1, wherein R.sub.1 is methyl and R.sub.2 is methyl. 9. The composition of claim 1, wherein R.sub.1 is a C.sub.1-4 alkyl and R.sub.2 is hydrogen. 10. The composition of claim 1, wherein R.sub.1 is methyl and R.sub.2 is hydrogen. 11. The composition of claim 1, wherein the fumarate ester is: ##STR00006## 12. The composition of claim 1, wherein the fumarate ester is: ##STR00007## wherein R is any C.sub.1-20 alkyl, or a salt thereof. 13. The composition of claim 1, wherein the fumarate ester is: ##STR00008## or a salt thereof. 14. The composition of claim 1, wherein the composition comprises about 80 mg to about 230 mg of the fumarate ester or salt thereof. 15. The composition of claim 1, wherein the composition comprises about 80 mg to about 115 mg or about 160 mg to about 230 mg of the fumarate ester or salt thereof. 16. The composition of claim 1, wherein the liquid vehicle comprises mono- and di-glycerides, polyvinylpyrrolidone, and polyoxyl 40 hydrogenated castor oil. 17. The composition of claim 1, wherein the composition comprises: about 30% to about 40% by weight of the fumarate ester or salt thereof; and about 55% to about 65% by weight of the liquid vehicle. 18. The composition of claim 1, wherein the composition comprises about 5% by weight of lactic acid. 19. The composition of claim 1, wherein the composition is encapsulated in a capsule. 20. The composition of claim 19, wherein the capsule provides delayed release of the fumarate ester or salt thereof. 21. The composition of claim 1, wherein upon administration to a subject, the composition activates a nuclear factor erythroid-derived 2-like (Nrf2) dependent pathway.