CONTROLLED RELEASE PHARMACEUTICAL COMPOSITIONS COMPRISING A FUMARIC ACID ESTER
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).