Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Controlled release pharmaceutical compositions comprising a fumaric acid ester

a technology of controlled release and pharmaceutical compositions, which is applied in the direction of drug compositions, immunological disorders, metabolism disorders, etc., can solve the problems that fumarate therapy like e.g. fumaderm® often gives rise to gastrointestinal side effects, and achieve the effect of reducing gastrointestinal side effects and reducing gi (gastro-intestinal) side effects

Inactive Publication Date: 2009-12-10
BIOGEN SWISS MFG GMBH
View PDF81 Cites 107 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

"The present invention relates to a pharmaceutical composition that reduces gastrointestinal side-effects when taken orally. This is achieved by administering the active substance in the form of a controlled release composition. The controlled release composition ensures that the fumaric acid ester is released in a controlled manner over a period of time, reducing the impact on the gastrointestinal tract. The release of the fumaric acid ester is tested using a dissolution test and the results show that the fumaric acid ester is released quickly and in a controlled manner. This controlled release composition provides improved efficacy and reduced side-effects when taken orally."

Problems solved by technology

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

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • 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

[0173]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.

[0174]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

[0175]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-Sol®) 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

[0176]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 polymeric material per mm2. Pigments and talc are added in an appropriate amount.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
pHaaaaaaaaaa
timeaaaaaaaaaa
timeaaaaaaaaaa
Login to View More

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

CROSS-REFERENCE TO PRIOR APPLICATIONS[0001]This is a U.S. National Phase Application under 35 U.S.C. §371 of International Patent Application No. PCT / DK2005 / 000648 filed Oct. 7, 2005, and claims the benefit of Danish Patent Applications: PA 2004 01546 filed Oct. 8, 2004; PA 2004 01736 filed Nov. 10, 2004; PA 2005 00211 filed Feb. 11, 2005; PA 2005 00419 filed Mar. 23, 2005; and U.S. Provisional Application No. 60 / 691,513 filed Jun. 16, 2005, all of which are hereby incorporated by reference in their entireties. The International Application was published in English on Apr. 13, 2006 as WO 2006 / 037342 A3 under PCT Article 21(2).FIELD OF THE INVENTION[0002]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 cont...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/20A61K31/22A61K31/225A61P3/10
CPCA61K9/28A61K9/48A61K9/2013A61K9/2027A61K9/2054A61K9/2846A61K9/4891A61K9/50A61K9/20A61K31/215A61K31/225A61K45/06A61K9/5047A61K9/5042A61K9/5084A61K31/22A61K9/2031A61K9/167A61K9/2077A61K9/2081A61K9/4808A61K9/14A61K2300/00A61K9/2853A61K9/2866A61P1/04A61P1/16A61P17/00A61P17/06A61P19/02A61P25/00A61P25/04A61P29/00A61P35/00A61P37/00A61P37/02A61P37/06A61P43/00A61P5/14A61P7/06A61P3/10A61K9/0053
Inventor NILSSON, HENRIKSCHOENHARTING, FLORIANMUELLER, BERND W.ROBINSON, JOSEPH R.ROBINSON, BONNA
Owner BIOGEN SWISS MFG GMBH
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com