US2017112793A2PendingUtilityA2

Controlled release pharmaceutical compositions comprising a fumaric acid ester

77
Assignee: FORWARD PHARMA ASPriority: Oct 8, 2004Filed: Mar 13, 2014Published: Apr 27, 2017
Est. expiryOct 8, 2024(expired)· nominal 20-yr term from priority
Inventors:Henrik NilssonBernd Mueller
A61K 9/28A61K 9/2054A61K 31/225A61K 9/2031A61K 9/4891A61K 45/06A61K 9/2013A61K 9/2027A61K 9/2846A61K 31/215A61K 31/22A61K 9/2853A61K 9/2866A61K 9/2077A61K 9/2081A61K 9/4808A61P 1/04A61P 1/16A61P 17/00A61P 17/06A61P 19/02A61P 25/00A61P 25/04A61P 29/00A61P 35/00A61P 37/00A61P 37/02A61P 37/06A61P 43/00A61P 5/14A61P 7/06A61P 3/10A61K 9/5042A61K 9/5047A61K 9/5084A61K 9/14A61K 9/167A61K 9/20A61K 9/48A61K 9/50A61K 9/0053
77
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Claims

Abstract

The present invention relates to controlled release pharmaceutical compositions comprising fumaric acid ester(s) as active substance(s). The compositions are suitable for use in the treatment of e.g. psoriasis or other hyperproliferative, inflammatory or autoimmune disorders and are designated to release the fumaric acid ester in a controlled manner so that local high concentrations of the active substance within the gastrointestinal tract upon oral administration can be avoided and, thereby, enabling a reduction in gastro-intestinal related side-effects.

Claims

exact text as granted — not AI-modified
1 - 90 . (canceled) 
     
     
         91 - 93 . (not entered) 
     
     
         94 . An oral pharmaceutical composition comprising (i) dimethylfumarate as the only fumaric acid ester active substance, (ii) one or more enteric coating polymers, and (iii) one or more pharmaceutically acceptable excipients, said composition being capable of providing controlled release in vivo in humans, wherein said dimethylfumarate is present in an amount of 50-90%, by weight, of said composition. 
     
     
         95 . The composition of  claim 94 , wherein said composition is in a tablet form. 
     
     
         96 . The composition of  claim 94 , wherein said composition is contained in a capsule. 
     
     
         97 . The composition of  claim 96 , wherein said composition is in the form of micro tablets. 
     
     
         98 . The composition of  claim 96 , wherein said composition is in the form of pellets or beads. 
     
     
         99 . The composition of  claim 96 , wherein said composition is in the form of granules. 
     
     
         100 . The composition of  claim 96 , wherein said composition is in the form of micro-crystals. 
     
     
         101 . The composition of  claim 94 , wherein said dimethylfumarate is present in an amount of 50-60%, by weight, of said composition. 
     
     
         102 . The composition of  claim 94 , wherein said dimethylfumarate is present in an amount of 50-80%, by weight, of said composition. 
     
     
         103 . The composition of  claim 94 , wherein said composition comprises a layer containing said one or more enteric coating polymers. 
     
     
         104 . The composition of  claim 101 , wherein said composition comprises a layer containing said one or more enteric coating polymers 
     
     
         105 . The composition of  claim 102 , wherein said composition comprises a layer containing said one or more enteric coating polymers. 
     
     
         106 . The composition of  claim 95 , wherein said tablet comprises a layer containing said one or more enteric coating polymers. 
     
     
         107 . The composition of  claim 97 , wherein said micro tablets comprise a layer containing said one or more enteric coating polymers. 
     
     
         108 . The composition of  claim 98 , wherein said pellets or beads comprise a layer containing said one or more enteric coating polymers. 
     
     
         109 . The composition of  claim 99 , wherein said granules comprise a layer containing said one or more enteric coating polymers. 
     
     
         110 . The composition of  claim 100 , wherein said micro-crystals comprise a layer containing said one or more enteric coating polymers. 
     
     
         111 . The composition of  claim 94 , wherein said one or more enteric coating polymers comprises polyacrylamides, phthalate derivatives, acid phthalates of carbohydrates, amylose acetate phthalate, cellulose acetate phthalate, cellulose ester phthalates, cellulose ether phthalates, hydroxypropylcellulose phthalate, hydroxypropylethylcellulose phthalate, hydroxypropylmethylcellulose phthalate, methylcellulose phthalate, polyvinyl acetate phthalate, poly acrylic methacrylic acid copolymers, shellac, or vinyl acetate and crotonic acid copolymers. 
     
     
         112 . The composition of  claim 111 , wherein said one or more enteric coating polymers is a poly acrylic methacrylic acid copolymer. 
     
     
         113 . (canceled)

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