Controlled release pharmaceutical compositions comprising a fumaric acid ester

Abstract

The invention features a kit. The kit includes: (i) a first unit dosage form consisting essentially of about 120 mg of dimethylfumarate and one or more pharmaceutically acceptable excipients, wherein the dimethylfumarate is formulated for delayed release; and (ii) a second unit dosage form consisting essentially of about 240 mg of dimethylfumarate and one or more pharmaceutically acceptable excipients, wherein the dimethylfumarate is formulated for delayed release.

1 . A kit comprising:
 (i) a first unit dosage form consisting essentially of about 120 mg of dimethylfumarate and one or more pharmaceutically acceptable excipients, wherein the dimethylfumarate is formulated for delayed release; and   (ii) a second unit dosage form consisting essentially of about 240 mg of dimethylfumarate and one or more pharmaceutically acceptable excipients, wherein the dimethylfumarate is formulated for delayed release.   
     
     
         2 . The kit of  claim 1 , wherein the first unit dosage form is in the form of a capsule or a tablet. 
     
     
         3 . The kit of  claim 2 , wherein the capsule is a hard gelatin capsule. 
     
     
         4 . The kit of  claim 2 , wherein the first unit dosage form comprises microtablets. 
     
     
         5 . The kit of  claim 4 , wherein the microtablets have an enteric coating. 
     
     
         6 . The kit of  claim 2 , wherein the first unit dosage form comprises pellets. 
     
     
         7 . The kit of  claim 1 , wherein the kit comprises fourteen capsules of the first unit dosage form. 
     
     
         8 . The kit of  claim 5 , wherein the kit consists of fourteen capsules of the first unit dosage form. 
     
     
         9 . The kit of  claim 1 , wherein the pharmaceutically acceptable excipients in the first unit dosage comprise one or more of the following: micro crystalline cellulose, cross-linked sodium carboxymethylcellulose, talc, silica colloidal silicon dioxide, magnesium stearate, or a surfactant having an HLB value above 8. 
     
     
         10 . The kit of  claim 9 , wherein the first unit dosage form comprises from about 1 to about 60% micro crystalline cellulose. 
     
     
         11 . The kit of  claim 9 , wherein the first unit dosage form comprises from about 0.2 to about 3% magnesium stearate. 
     
     
         12 . The kit of  claim 9 , wherein the first unit dosage form comprises from about 0.2 to about 4% silica. 
     
     
         13 . The kit of  claim 9 , wherein the first unit dosage form comprises cross-linked sodium carboxymethylcellulose. 
     
     
         14 . The kit of  claim 9 , wherein the first unit dosage form comprises a surfactant having an HLB value above 8. 
     
     
         15 . The kit of  claim 1 , wherein the second unit dosage form is in the form of a capsule or a tablet. 
     
     
         16 . The kit of  claim 15 , wherein the capsule is a hard gelatin capsule. 
     
     
         17 . The kit of  claim 15 , wherein the second unit dosage form comprises microtablets. 
     
     
         18 . The kit of  claim 17 , wherein the microtablets have an enteric coating. 
     
     
         19 . The kit of  claim 15 , wherein the second unit dosage form comprises pellets. 
     
     
         20 . The kit of  claim 1 , wherein the kit comprises fourteen capsules of the second unit dosage form. 
     
     
         21 . The kit of  claim 1 , wherein the pharmaceutically acceptable excipients in the second unit dosage form comprise at least one 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. 
     
     
         22 . The kit of  claim 21 , wherein the second dosage unit comprises from about 1 to about 60% micro crystalline cellulose. 
     
     
         23 . The kit of  claim 21 , wherein the second dosage unit comprises from about 0.2 to about 3% magnesium stearate. 
     
     
         24 . The kit of  claim 21 , wherein the second dosage unit comprises from about 0.2 to about 4% silica. 
     
     
         25 . The kit of  claim 21 , wherein the second unit dosage comprises cross-linked sodium carboxymethylcellulose. 
     
     
         26 . The kit of  claim 21 , wherein the second dosage unit comprises a surfactant having an HLB value above 8. 
     
     
         27 . The kit of  claim 1 , wherein said dimethylfumarate is in the form of micro crystals. 
     
     
         28 . The kit of  claim 27 , wherein said micro crystals have an enteric coating. 
     
     
         29 . The kit of  claim 27 , wherein said first unit dosage form and said second unit dosage form comprise micro crystals between 315 and 710 microns. 
     
     
         30 . The kit of  claim 1 , further comprising a label containing instructions for an oral dosage regimen of (i) and (ii).