Controlled release pharmaceutical compositions comprising a fumaric acid ester

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 arc 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.

1 .- 45 . (canceled) 
     
     
         46 . A controlled release pharmaceutical composition for oral administration comprising a biodegradable coat and a matrix, wherein the matrix comprises an active substance and polyethylene glycol-stearate, wherein the active substance is selected from the group consisting of dimethyl fumarate (DMF), monomethyl fumarate (MMF), a pharmaceutically acceptable salt of MMF, and a combination of (i) DMF and (ii) MMF or a pharmaceutically acceptable salt of MMF; and wherein the active ingredient is evenly distributed throughout the matrix form. 
     
     
         47 . The controlled release pharmaceutical composition of  claim 46 , wherein the active substance is DMF. 
     
     
         48 . The controlled release pharmaceutical composition of  claim 46 , wherein the active substance is MMF. 
     
     
         49 . The controlled release pharmaceutical composition of  claim 46 , wherein the active substance is a combination of DMF and MMF in a weight ratio of DMF to MMF between about 1:10 and about 10:1. 
     
     
         50 . The controlled release pharmaceutical composition of  claim 46 , wherein the active substance is a salt of MMF. 
     
     
         51 . The controlled release pharmaceutical composition of  claim 46  consisting essentially of DMF as the active substance. 
     
     
         52 . The controlled release pharmaceutical composition of  claim 46  consisting essentially of MMF as the active substance. 
     
     
         53 . The controlled release pharmaceutical composition of  claim 46  consisting essentially of a pharmaceutically acceptable salt of MMF as the active substance.