# US 10,945,985 B2 · Fumarate ester dosage forms

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- Number: US 10,945,985 B2
- Document ID: US10945985B2
- Status: Granted
- Kind: B2
- Application number: 16/129,887
- Filed: 2018-09-13
- Published: 2019-01-17
- Granted: 2021-03-16
- Earliest claimed: 2015-08-31
- Assignees: Banner Life Sciences LLC
- Applicants: Banner Life Sciences LLC
- Inventors: Jason M. Vaughn; Justin R. Hughey; Tanesha Roberts; Tatyana Dyakonov; Sunil Agnihotri; Aqeel A. Fatmi
- Web page: https://patentgrep.com/patent/US10945985B2

## CPC

- A61K 31/225: Polycarboxylic acids
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/10: Dispersions; Emulsions
- A61K 9/4808: {characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release (capsules filled with granules or microparticles A61K9/16; filled with microcapsules or coated microparticles A61K9/50; with mixture of different granules, microcapsules, (coated) microparticles A61K9/5084)}
- A61K 9/4833: {Encapsulating processes; Filling of capsules (mechanical aspects A61J3/07)}
- A61K 9/4858: {Organic compounds}
- A61K 9/4866: {Organic macromolecular compounds}
- A61K 9/4875: {Compounds of unknown constitution, e.g. material from plants or animals (oils, fats, waxes, shellac A61K9/4858)}
- A61K 9/4891: {Coated capsules; Multilayered drug free capsule shells (with drug coating for immediate release A61K9/4808; osmotic devices A61K9/0004)}
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## 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.

## Claims

### Claim 1

An oral pharmaceutical composition comprising an immediate releasing single phase non-aqueous liquid vehicle comprising a suspension of a fumarate ester or a salt thereof having the formula:

### Claim 2 (depends on 1)

The composition of claim 1, wherein the composition comprises about 80 mg to about 230 mg of the fumarate ester or salt thereof.

### Claim 3 (depends on 1)

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.

### Claim 4 (depends on 1)

The composition of claim 1, wherein the liquid vehicle comprises mono- and di-glycerides, polyvinylpyrrolidone, and polyoxyl 40 hydrogenated castor oil.

### Claim 5 (depends on 1)

The composition of claim 1, wherein the composition comprises:
about 30% to about 40% by weight of the composition of the fumarate ester or salt thereof; and
about 55% to about 65% by weight of the composition of the liquid vehicle.

### Claim 6 (depends on 1)

The composition of claim 1, wherein the liquid vehicle comprises about 5% by weight of the composition of lactic acid.

### Claim 7 (depends on 1)

The composition of claim 1, wherein the composition is encapsulated in a capsule.

### Claim 8 (depends on 7)

The composition of claim 7, wherein the capsule provides delayed release of the fumarate ester or salt thereof.

### Claim 9 (depends on 1)

The composition of claim 1, wherein upon administration to a subject, the composition activates a nuclear factor erythroid-derived 2-like (Nrf2) dependent pathway.

### Claim 10

An oral pharmaceutical composition comprising an immediate releasing single phase non-aqueous liquid vehicle comprising:
mono- and di-glycerides, polyvinylpyrrolidone, and polyoxyl 40 hydrogenated castor oil, and lactic acid; and
a suspension of about 95 mg of a fumarate ester or a salt thereof having the formula:

### Claim 11 (depends on 10)

The composition of claim 10, wherein the composition comprises:
about 30% to about 40% by weight of the composition of the fumarate ester or salt thereof;
about 55% to about 65% by weight of the composition of the liquid vehicle comprising mono- and di-glycerides, polyvinylpyrrolidone, and polyoxyl 40 hydrogenated castor oil; and
and about 5% by weight of the composition of lactic acid.

### Claim 12 (depends on 10)

The composition of claim 10, wherein the composition is encapsulated in an enterically coated soft capsule.

### Claim 13 (depends on 11)

The composition of claim 11, wherein the enterically coated soft capsule provides delayed release of the fumarate ester or salt thereof.