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Controlled release pharmaceutical compositions comprising a fumaric acid ester

A technology of fumarate and controlled release drugs, which is applied in the direction of pill delivery, etc., and can solve problems such as gastrointestinal side effects and colic

Inactive Publication Date: 2007-10-17
前进药物股份公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] However, fumarate therapy, such as Fumaderm  Often causes gastrointestinal side effects such as bloating, diarrhea, upper abdominal cramps, gas, 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

Embodiment 1

[0294] Tablet preparation

[0295] Mix 200 g of granules with 150 g of microcrystalline cellulose (such as Avicel  102), 97.5g lactose (such as Tablettose  ), 10g sodium carboxymethylcellulose (such as Ac-Di-Sol  ) and 25g of starch were mixed for 30min. Then 10 g of magnesium stearate and 7.5 g of amorphous silicon dioxide (such as Aerosil  200), the powder mixture was mixed for 5 min.

[0296] This powder mixture is compressed into tablets in tableting equipment (tablet diameter 10mm, surface area approximately 280-300mm 2 ). Enteric coating was applied during pan coating or fluidized bed coating, as described in Example 4.

Embodiment 2

[0298] Tablet preparation

[0299] Mix 200g microcrystalline with 150g microcrystalline cellulose (such as Avicel  102), 130g lactose (e.g. Tablettose  ), 10g sodium carboxymethylcellulose (such as Ac-Di-Sol  ) and 25mg of starch were mixed for 30min. Then 10 g of magnesium stearate and 7.5 g of amorphous silicon dioxide were added and the powder mixture was mixed for 5 min. This powder mixture is compressed into tablets in tableting equipment (tablet diameter 10mm, surface area approximately 280-300mm 2 ). Enteric coating was applied during pan coating or fluidized bed coating, as described in Example 4.

Embodiment 3

[0301] Preparation of capsules

[0302] The granules or microcrystals were filled into HPMC capsules and enteric coated as described below. In a pan coater, spray the capsules with Eudragit  L30D-55, drying temperature 60°C to 80°C, dosage 20mg polymeric material per mm 2 . Add appropriate amount of coloring and talc.

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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.

Description

field of invention [0001] The present invention relates to controlled release pharmaceutical compositions comprising fumarate esters as active substance. These compositions are suitable for the treatment of e.g. psoriasis or other hyperproliferative, inflammatory or autoimmune disorders and are designed to release fumaric acid in a controlled manner in order to be able to avoid localization of the active substance in the gastrointestinal tract following oral administration. High concentration, thereby reducing gastrointestinal side effects. Background of the invention [0002] Fumarates, the combination of dimethyl fumarate and ethyl hydrogen fumarate, have been used for many years in the treatment of psoriasis. This combination is commercially available under the name Fumaderm  . It comes in the form of an oral tablet and is available in two different dosage strengths (Fumaderm  initial and Fumaderm  ): [0003] Fumaderm  Initial Fumaderm ...

Claims

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Application Information

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IPC IPC(8): A61K9/20
CPCA61K9/2013
Inventor H・尼尔森F・肖恩哈汀B・W・米勒J・R・罗宾逊
Owner 前进药物股份公司
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