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Controlled release pharmaceutical compositions comprising a fumaric acid ester

a technology of controlled release and pharmaceutical compositions, which is applied in the direction of botany apparatus and processes, pharmaceuticals, applications, etc., can solve the problems that fumarate therapy like e.g. fumaderm® often gives rise to gastro-intestinal side effects, and achieves the effects of reducing dependence, prolonging time period, and reducing interindividual and/or intraindividual variation in plasma profiles

Inactive Publication Date: 2013-11-28
BIOGEN SWISS MFG GMBH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention is related to a pharmaceutical composition that includes a specific active substance, called monoalkylester of fumaric acid. This compound is metabolized to fumaric acid and has a rapid elimination process. The patent describes a technology called MeltDose®, which involves formulating individual molecules of the active substance into tablets. This technology helps to overcome the limitations of oral absorption of drugs with low water-solubility. The composition is designed to provide a prolonged release of the active substance and to reduce the frequency of dosing and the average daily dose required. The use of the controlled release composition results in improved therapeutic response and increased convenience for patients.

Problems solved by technology

However, therapy with fumarates like e.g. Fumaderm® frequently gives rise to gastro-intestinal side effects such as e.g. fullness, diarrhea, upper abdominal cramps, flatulence and nausea.

Method used

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  • Controlled release pharmaceutical compositions comprising a fumaric acid ester
  • Controlled release pharmaceutical compositions comprising a fumaric acid ester
  • Controlled release pharmaceutical compositions comprising a fumaric acid ester

Examples

Experimental program
Comparison scheme
Effect test

example 1

Preparation of Tablets

[0264]200 g granules are mixed with 150 g microcrystalline cellulose (e.g. Avicel® 102), 97.5 g lactose (e.g. Tablettose®), 10 g sodium carboxymethylcellulose (e.g. Ac-Di-Sol®) and 25 g starch for 30 min. Then 10 g magnesium stearate and 7.5 g amorphous silicium dioxide (e.g. Aerosil® 200) is added and the powder mixture is mixed for 5 min.

[0265]This powder mixture is compressed to tablets in tabletting equipment (tablet diameter 10 mm, surface about 280-300 mm2). The tablets are enteric coated in a pan-coating or in a fluid-bed coating process as described in Example 4.

example 2

Preparation of Tablets

[0266]200 g micro-crystals are mixed with 150 g microcrystalline cellulose (e.g. Avicel® 102), 130 g lactose (e.g. Tablettose®), 10 g of sodium carboxymethylcellulose (e.g. Ac-Di-Son and 25 mg starch for 30 min. Then 10 g magnesium stearate and 7.5 g of amorphous silicium dioxide is added and the powder mixture is mixed for 5 min. This powder mixture is compressed to tablets in tabletting equipment (tablet diameter 10 mm, surface about 280-300 mm2). The tablets are enteric coated in a pan-coating or in a fluid-bed coating process as described in Example 4.

example 3

Preparation of Capsules

[0267]Granules or micro-crystals are filled in HPMC capsules and these capsules are enteric coated as described in the following. In a pan coater Eudragit® L30D-55 is sprayed at drying temperatures of 60° C. to 80° C. onto the capsules in an amount of 20 mg po lymeric material per mm2. Pigments and talc are added in an appropriate amount.

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Abstract

The invention features a method of treating a subject in need of treatment for multiple sclerosis. The method involves orally administering to the subject in need thereof a pharmaceutical composition in unit dosage form consisting essentially of (a) from about 120 mg to about 240 mg of dimethylfumarate formulated for delayed release, and (b) one or more pharmaceutically acceptable excipients, wherein following the orally administering of the unit dosage form monomethylfumarate appears in the plasma of the subject upon hydrolysis of dimethylfumarate and the Cmax of the monomethylfumarate in the plasma of the subject is between about 0.4 and about 2 mg / L, and wherein about 480 mg of dimethylfumarate per day is orally administered to the subject.

Description

FIELD OF THE INVENTION[0001]The present invention relates to controlled release pharmaceutical compositions comprising a fumaric acid ester as an active substance. The compositions are suitable for use in the treatment of e.g. psoriasis or other hyperproliferative, inflammatory or autoimmune disorders and are designed 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.BACKGROUND OF THE INVENTION[0002]Fumaric acid esters, i.e. dimethylfumarate in combination with ethylhydrogenfumarat have been used in the treatment of psoriasis for many years. The combination is marketed under the tradename Fumaderm®. It is in the form of tablets intended for oral use and it is available in two different dosage strengths (Fumaderm® initial and Fumaderm®):Fumaderm ® InitialFumaderm ®Dimethy...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/225
CPCA61K31/225A61K45/06A61K9/2013A61K9/2027A61K9/2054A61K9/2846A61K9/4891A61K31/215A61K31/22A61K9/2853A61K9/2866A61K9/2031A61K9/2077A61K9/2081A61K9/4808A61P1/04A61P1/16A61P17/00A61P17/06A61P19/02A61P25/00A61P25/04A61P29/00A61P35/00A61P37/00A61P37/02A61P37/06A61P43/00A61P5/14A61P7/06A61P3/10A61K2300/00A61K9/5042A61K9/5047A61K9/5084A61K9/14A61K9/167A61K9/20A61K9/28A61K9/48A61K9/50A61K9/0053
Inventor NILSSON, HENRIKSCHÖNHARTING, FLORIANMÜLLER, BERND W.ROBINSON, JOSEPH R.
Owner BIOGEN SWISS MFG GMBH
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