Controlled release dosage form for once daily administration of dimethyl fumarate
View Patent ↗A controlled release dosage form containing monomethyl fumarate, a compound that can be metabolized into monomethyl fumarate in vivo, or a pharmaceutically acceptable salt thereof or combinations thereof, wherein the monomethyl fumarate, a compound that can be metabolized into monomethyl fumarate in vivo, or a pharmaceutically acceptable salt thereof or combinations thereof is delivered to the subject. Also provided is a method of treating a disease or disorder (e.g., multiple sclerosis) by orally administering a controlled release dosage form containing monomethyl fumarate, a compound that can be metabolized into monomethyl fumarate in vivo, or a pharmaceutically acceptable salt thereof or combinations thereof, wherein the monomethyl fumarate, a compound that can be metabolized into monomethyl fumarate in vivo, or a pharmaceutically acceptable salt thereof or combinations thereof.
1. A gastric retention dosage form comprising dimethyl fumarate and one or more pharmaceutically acceptable excipients,
wherein upon oral administration to a subject: (a) said gastric retention dosage form is retained for at least 3 hours in the stomach of the subject; and (b) the dimethyl fumarate is released from the dosage form in the gastrointestinal tract of the subject over a sustained period of time, and
wherein said gastric retention dosage form is a swelling dosage form in the form of a swelling tablet, wherein the swelling tablet is a bilayer tablet comprising: (i) a swelling layer that does not comprise dimethyl fumarate; and (ii) an active layer comprising dimethyl fumarate.
2. The gastric retention dosage form of claim 1 , wherein the swelling layer comprises one or more swelling polymers selected from the group consisting of polyethylene oxide and hydroxyalkyl alkylcellulose polymers.
3. The gastric retention dosage form of claim 1 , wherein the swelling dosage form comprises: (a) dimethyl fumarate in an amount of about 20% w/w to about 80% w/w of the swellable dosage form, wherein the dimethyl fumarate is coated with a seal coat, enteric coat, or a combination thereof, and (b) one or more swelling polymers in an amount of about 10% w/w to about 50% w/w of the swellable dosage form.
4. The gastric retention dosage form of claim 3 , wherein the swelling dosage form comprises dimethyl fumarate in an amount of about 50% w/w to about 60% w/w of the swellable dosage form.
5. The gastric retention dosage form of claim 1 or 3 , wherein the sustained period of time is from about 2 to about 24 hours.
6. The gastric retention dosage form of claim 5 , wherein the sustained period of time is from about 2 to about 16 hours.