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AssigneeForward Pharma A/S
InventorsHenrik NILSSON, Florian SCHOENHARTING, Bernd W. MUELLER, Joseph R. ROBINSON
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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.
A pharmaceutical composition comprising as an active substance one or more fumaric acid esters selected from di-(C1-C5)alkylesters of fumaric acid and mono-(C1-C5)alkylesters of fumaric acid, or a pharmaceutically acceptable salt thereof, which—upon oral administration and in comparison to that obtained after oral administration of Fumaderm® tablets in an equivalent dosage—gives a reduction in GI related side effects.
A controlled release pharmaceutical composition for oral use comprising as an active substance one or more fumaric acid esters selected from di-(C1-C5)alkylesters of fumaric acid and mono-(C1-C5)alkylesters of fumaric acid, or a pharmaceutically acceptable salt thereof, wherein the release of the fumaric acid ester—when subjected to an in vitro dissolution test employing 0.1 N hydrochloric acid as dissolution medium during the first 2 hours of the test and then 0.05 M phosphate buffer pH 6.5 as dissolution medium—is as follows:
A controlled release pharmaceutical composition for oral use comprising as an active substance one or more fumaric acid esters selected from di-(C1-C5)alkylesters of fumaric acid and mono-(C1-C5)alkylesters of fumaric acid, or a pharmaceutically acceptable salt thereof, wherein the release of the fumaric acid ester—when subjected to an in vitro dissolution test employing 0.1 N hydrochloric acid as dissolution medium during the first 2 hours of the test and then 0.05 M phosphate buffer pH 6.5 as dissolution medium—is as follows:
The controlled release pharmaceutical composition according to any one of the preceding claims, wherein the release has zero-order, first-order or square-root (Higuchi's equation) kinetics release profile.
A controlled release pharmaceutical composition comprising as an active substance from 10% to 90% by weight of one or more fumaric acid esters selected from di-(C1-C5)alkylesters of fumaric acid and mono-(C1-C5)alkylesters of fumaric acid, or a pharmaceutically acceptable salt thereof, from 2% to 40% by weight pharmaceutically acceptable polymer(s), and from 1% to 40% by weight hydrophilic excipient(s), and optionally pharmaceutically acceptable excipients or additives.
The controlled release pharmaceutical composition comprising as an active substance from 10% to 90% by weight of one or more fumaric acid esters selected from di-(C1-C5)alkylesters of fumaric acid and mono-(C1-C5)alkylesters of fumaric acid, or a pharmaceutically acceptable salt thereof, and 2% to 40% by weight methacrylic acid copolymer A and B in a weight ratio between 1:9 and 9:1, and optionally pharmaceutically acceptable excipients or additives.
The controlled release pharmaceutical composition according to any one of the preceding claims, wherein the fumaric acid ester is selected from the group consisting of dimethylfumarate, diethylfumarate, dipropylfumarate, dibutylfumarate, dipentylfumarate, methyl-ethyl-fumarate, methyl-propylfumarat, methyl-butylfumarat, methyl-pentylfumarate, monomethylfumarate, monoethylfumarate, monopropylfumarate, monobutylfumarate, and monopentylfumarate, including pharmaceutically acceptable salts thereof.
The controlled release pharmaceutical composition according to any one of the preceding claims, wherein the fumaric acid ester is a mono-(C1-C5)alkylester of fumaric acid that is present in the form of a pharmaceutically acceptable salt.
The controlled release pharmaceutical composition according to any one of the preceding claims comprising dimethylfumarate as the active substance.
The controlled release pharmaceutical composition according to any one of the preceding claims comprising monomethylfumarate as the active substance.
The controlled release composition according to any one of the preceding claims for administration once, twice or three times daily.
The controlled release pharmaceutical composition according to any one of the preceding claims, wherein the amount of one or more fumaric acid esters selected from di-(C1-C5)alkylesters of fumaric acid and mono-(C1-C5)alkylesters of fumaric acid or a pharmaceutically acceptable salt thereof, in a dosage form is from 90 mg to 360 mg active substance.
The controlled release pharmaceutical composition according to any one of the preceding claims in the form of a tablet.
Dependencies are inferred from the claim text.