US2014037740A1PendingUtilityA1

Controlled release pharmaceutical compositions comprising a fumaric acid ester

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Assignee: FORWARD PHARMA ASPriority: Oct 8, 2004Filed: Aug 1, 2013Published: Feb 6, 2014
Est. expiryOct 8, 2024(expired)· nominal 20-yr term from priority
Inventors:Henrik NilssonFlorian SchönhartingBernd MullerJoseph R. Robinson
A61P 37/00A61P 3/10A61P 35/00A61P 37/06A61P 43/00A61P 5/14A61P 7/06A61P 37/02A61P 25/04A61P 29/00A61P 17/06A61P 25/00A61P 19/02A61P 1/04A61P 17/00A61P 1/16A61K 9/48A61K 9/4808A61K 9/4891A61K 9/50A61K 9/2027A61K 9/2013A61K 9/167A61K 31/215A61K 31/22A61K 9/2853A61K 9/5047A61K 9/5042A61K 9/2081A61K 45/06A61K 9/2031A61K 9/14A61K 9/2846A61K 9/2054A61K 9/2077A61K 31/225A61K 9/2866A61K 9/28A61K 9/20A61K 9/5084A61K 9/0053
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Claims

Abstract

The invention features a delayed release composition wherein the active ingredient consists essentially of about 240 mg of dimethylfumarate and one or more pharmaceutically acceptable excipients.

Claims

exact text as granted — not AI-modified
1 . A delayed release composition wherein the active ingredient consists essentially of about 240 mg of dimethylfumarate and one or more pharmaceutically acceptable excipients. 
     
     
         2 . The composition of  claim 1 , wherein the composition contains a methacrylic acid copolymer. 
     
     
         3 . The composition of  claim 1 , wherein the pharmaceutically acceptable excipients comprise one or more of the following excipients micro crystalline cellulose, cross-linked sodium carboxymethylcellulose, talc, silica, colloidal silicon dioxide, magnesium stearate, or a surfactant having an HLB value above 8. 
     
     
         4 . The composition of  claim 3 , wherein the composition comprises from about 1 to about 60% micro crystalline cellulose. 
     
     
         5 . The composition of  claim 3 , wherein the composition comprises from about 0.2 to about 3% magnesium stearate. 
     
     
         6 . The composition of  claim 3 , wherein the composition comprises from about 0.2 to about 4% silica. 
     
     
         7 . The composition of  claim 3 , wherein the composition comprises cross-linked sodium carboxymethylcellulose. 
     
     
         8 . The composition of  claim 3 , wherein the composition comprises a surfactant having an HLB value above 8. 
     
     
         9 . The composition of  claim 1 , wherein the dimethylfumarate is in the form of micro crystals. 
     
     
         10 . The composition of  claim 9 , wherein the composition comprises micro crystals between 315 and 710 microns. 
     
     
         11 . The composition of  claim 1 , wherein following oral administration of the unit dosage form to a human subject monomethylfumarate appears in the plasma of the subject with a Cmax of about 2 mg/L. 
     
     
         12 . The composition of  claim 11 , wherein the time period for the plasma concentration to decrease to reach 50% of the Cmax is at least 2 hours. 
     
     
         13 . The composition of  claim 12 , wherein the time period for the plasma concentration to decrease to reach 50% of the Cmax is in a range of from about 2 to about 15 hours. 
     
     
         14 . The composition of  claim 13 , wherein the time period for the plasma concentration to decrease to reach 50% of the Cmax is in a range of from about 2 to about 10 hours. 
     
     
         15 . The composition of  claim 14 , wherein the time period for the plasma concentration to decrease to reach 50% of the Cmax is in a range of from about 3 to about 8 hours. 
     
     
         16 . The composition of  claim 1 , wherein the composition is a unit dosage form that is a capsule or a tablet. 
     
     
         17 . The composition of  claim 16 , wherein the capsule is a hard gelatin capsule. 
     
     
         18 . The composition of  claim 1 , wherein the composition is a unit dosage form comprising microtablets. 
     
     
         19 . The composition of  claim 18 , wherein the microtablets have an enteric coating. 
     
     
         20 . The composition of  claim 1 , wherein the composition is a unit dosage form comprising beads. 
     
     
         21 . The composition of  claim 1 , wherein said dimethylfumarate is in the form of micro crystals. 
     
     
         22 . The composition of  claim 21 , wherein the composition is a capsule containing enteric coated micro crystals that have one coating layer. 
     
     
         23 . The composition of  claim 21 , wherein the capsule comprises micro crystals between 315 and 710 microns. 
     
     
         24 . A method of treating a subject by administering a delayed release composition of  claim 1 , wherein 240 mg of said composition is administered twice daily. 
     
     
         25 . The method of  claim 24 , wherein about 240 mg is administered in the morning and the remainder is administered later in the day. 
     
     
         26 . The composition of  claim 2 , wherein the methacrylic acid is in a layer. 
     
     
         27 . The composition of  claim 26 , wherein the composition contains one layer. 
     
     
         28 . The composition of  claim 1 , wherein the composition is a unit dosage form comprising pellets. 
     
     
         29 . The composition of  claim 28 , wherein the methacrylic acid is in a layer on the pellets.

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