WO2003053451A1 - Use of ionic and non-ionic cellulose ethers for producing a gel-like agent for preventing the resorption of fats from the gastro-intestinal tract - Google Patents

Use of ionic and non-ionic cellulose ethers for producing a gel-like agent for preventing the resorption of fats from the gastro-intestinal tract Download PDF

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Publication number
WO2003053451A1
WO2003053451A1 PCT/EP2002/013032 EP0213032W WO03053451A1 WO 2003053451 A1 WO2003053451 A1 WO 2003053451A1 EP 0213032 W EP0213032 W EP 0213032W WO 03053451 A1 WO03053451 A1 WO 03053451A1
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WO
WIPO (PCT)
Prior art keywords
ionic
fats
agent
gel
preventing
Prior art date
Application number
PCT/EP2002/013032
Other languages
German (de)
French (fr)
Inventor
Günther Beisel
Original Assignee
Beisel Guenther
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
Application filed by Beisel Guenther filed Critical Beisel Guenther
Priority to AU2002352075A priority Critical patent/AU2002352075A1/en
Publication of WO2003053451A1 publication Critical patent/WO2003053451A1/en

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • A61K31/716—Glucans
    • A61K31/717—Celluloses

Definitions

  • the invention relates to an agent which, after oral ingestion in humans or in animals in the gastrointestinal tract, reduces the extent of the absorption of dietary fats. Due to the reduced absorption of dietary fats, the agent according to the invention is intended for use in reduction diets to reduce the amount of calories consumed and to lower the cholesterol level.
  • Obesity in humans or animals is caused by the excessive intake of high-calorie food.
  • Herbal slimming agents contain swelling agents such as alginic acid or karaya gum, which are supposed to have a satiating effect due to their volume stimulus.
  • Sypathomimetics are also used as appetite suppressants to support weight loss. Sympathomimetics are said to have a stimulating effect and counteract the tiredness that occurs with reduction diets. Sympathomimetics are absorbed into the bloodstream. They can trigger significant side effects like high blood pressure. In the case of reduction diets, attempts can be made to absorb food fats by means of lipase inhibitors such as. B. Orlistat (U.S. Patent 4,598,089). Orlistat is filled into capsules and used for weight loss in the context of reduction diets. Orlistat is said to be used in the gastrointestinal tract for the absorption of certain dietary fats
  • Orlistat intervenes in metabolic processes in the body. Numerous side effects are described that suggest further pharmacological activities of the substance in the body.
  • ionic or nonionic cellulose ethers are given as solutions, suspensions, powders and granules or in the form of tablets and capsules.
  • Hydroxyethyl cellulose with a high viscosity is preferably given as the cellulose ether. Hydroxyethyl cellulose is used as a solution or aqueous suspension before, with or after meals ingested. A preferred form of preparation is an aqueous suspension which only develops a gel-like consistency in the stomach after ingestion.
  • the cellulose derivatives used for the agent according to the invention are practically not absorbed. They have no side effects.
  • ionic or nonionic gelling agents for the preparation of the agent according to the invention are carmellose, hypromellose, hydroxyethyl cellulose, hydroxypropyl cellulose, ethyl methyl cellulose and
  • Methylcellulose Other gelling agents of other substance classes such as B. Starch derivatives can be used to support gel formation.
  • the ingredients are mixed and processed into granules.

Abstract

The invention relates to an agent for preventing the resorption of fats from the gastro-intestinal tract.

Description

Verwendung von ionischen und nichtionischen Celluloseethern zur Herstellung eines gelartigen Mittels zur Verhinderung der Resorption von Fetten aus dem Magen-Darm-TraktUse of ionic and nonionic cellulose ethers to produce a gel-like agent for preventing the absorption of fats from the gastrointestinal tract
Gegenstand der Erfindung ist ein Mittel, das nach oraler Einnahme beim Menschen oder bei Tieren im Magen-Darm-Trakt das Ausmaß der Resorption von Nahrungsfetten reduziert. Aufgrund der verminderten Resorption von Nahrungsfetten ist ein Einsatz des erfindungsgemäßen Mittels bei Reduktionsdiäten zur Reduzierung der aufgenommenen Kalorienmenge sowie zur Senkung des Cholesterolspiegels vorgesehen.The invention relates to an agent which, after oral ingestion in humans or in animals in the gastrointestinal tract, reduces the extent of the absorption of dietary fats. Due to the reduced absorption of dietary fats, the agent according to the invention is intended for use in reduction diets to reduce the amount of calories consumed and to lower the cholesterol level.
Übergewicht wird beim Menschen oder Tieren (z. B. Hunden) durch die übermäßige Aufnahme kalorienreicher Nahrung verursacht.Obesity in humans or animals (e.g. dogs) is caused by the excessive intake of high-calorie food.
Bisher werden zur Behandlung von Übergewicht neben diätetischen Maßnahmen vorwiegend pflanzliche oder chemisch definierte Abmagerungsmittel oder Appetitzügler verwendet. Pflanzliche Abmagerungsmittel enthalten Quellmittel wie Alginsäure oder Karaya-Gummi, die aufgrund ihres Volumenreizes sättigend wirken sollen.Heretofore, in addition to dietary measures, herbal or chemically defined weight loss agents or appetite suppressants have mainly been used to treat obesity. Herbal slimming agents contain swelling agents such as alginic acid or karaya gum, which are supposed to have a satiating effect due to their volume stimulus.
Im Weiteren werden Sypathomimetika als Appetitzügler zur Unterstützung der Gewichtsreduktion verwendet. Sympathomimetika sollen anregend wirken und der bei Reduktionsdiäten auftretende Müdigkeit entgegenwirken. Sympathomimetika werden in den Blutkreislauf aufgenommen. Sie können erhebliche Nebenwirkungen wie Bluthochdruck auslösen. Bei Reduktionsdiäten kann versucht werden, die Resorption von Nahrungsfetten durch Lipase- Hemmstoffe wie z. B. Orlistat zu vermindern (U.S. Patent 4,598,089). Orlistat wird in Kapseln abgefüllt und zur Gewichtsreduktion im Rahmen von Reduktionsdiäten eingesetzt. Orlistat soll im Magen-Darm-Trakt die für die Resorption bestimmter NahrungsfetteSypathomimetics are also used as appetite suppressants to support weight loss. Sympathomimetics are said to have a stimulating effect and counteract the tiredness that occurs with reduction diets. Sympathomimetics are absorbed into the bloodstream. They can trigger significant side effects like high blood pressure. In the case of reduction diets, attempts can be made to absorb food fats by means of lipase inhibitors such as. B. Orlistat (U.S. Patent 4,598,089). Orlistat is filled into capsules and used for weight loss in the context of reduction diets. Orlistat is said to be used in the gastrointestinal tract for the absorption of certain dietary fats
erforderliche Fettspaltung verhindern. Orlistat greift damit in metabolische Vorgänge im Körper ein. Es werden zahlreiche Nebenwirkungen beschrieben, die weitere pharmakologische Aktivitäten der Substanz im Körper vermuten lassen.Prevent necessary fat splitting. Orlistat intervenes in metabolic processes in the body. Numerous side effects are described that suggest further pharmacological activities of the substance in the body.
Die Nachteile, die in den Nebenwirkungen der bisher bekannten Mittel zur Gewichtsreduktion bzw. zur Reduzierung der Fettresorption liegen, werden durch die vorliegende Erfindung behoben. Durch die Gabe von ionischen oder nichtionischen Celluloseethern oder ihren Mischungen als Gelbildner wird im Magen-Darrn-Trakt die Resorption der Nahrungsfette ganz oder teilweise verhindert. Die Gelbildner verhindern ganz oder teilweise die Mizellbildung der Nahrungsfette mit den Gallensäften, die vollständige Fettspaltung und damit die Resorption Fette bzw. Fettsäuren.The disadvantages which lie in the side effects of the previously known agents for weight reduction or for reducing fat absorption are eliminated by the present invention. Through the administration of ionic or non-ionic cellulose ethers or their mixtures as gel formers, the absorption of the dietary fats in the gastrointestinal tract is completely or partially prevented. The gelling agents completely or partially prevent the micelle formation of the dietary fats with the bile juices, the complete fat splitting and thus the absorption of fats or fatty acids.
Die ionischen oder nichtionischen Celluloseether werden als Lösungen, Suspensionen, Pulver und Granulate oder in Form von Tabletten und Kapseln gegeben.The ionic or nonionic cellulose ethers are given as solutions, suspensions, powders and granules or in the form of tablets and capsules.
Als Celluloseether wird vorzugsweise Hydroxyethylcellulose mit einer hohen Viskosität gegeben. Hydroxyethylcellulose wird als Lösung oder wässrige Suspension vor, zu oder nach den Mahlzeiten eingenommen. Eine bevorzugte Zubereitungsform ist eine wässrige Suspension, die erst nach der Einnahme im Magen eine gelartige Konsistenz ausbildet.Hydroxyethyl cellulose with a high viscosity is preferably given as the cellulose ether. Hydroxyethyl cellulose is used as a solution or aqueous suspension before, with or after meals ingested. A preferred form of preparation is an aqueous suspension which only develops a gel-like consistency in the stomach after ingestion.
Die für das erfindungsgemäße Mittel verwendeten Cellulosedderivate werden praktisch nicht resorbiert. Sie besitzen keine Nebenwirkungen.The cellulose derivatives used for the agent according to the invention are practically not absorbed. They have no side effects.
Beispiele für ionische oder nichtionische Gelbildner zur Herstellung des erfindungsgemäßen Mittels sind Carmellose, Hypromellose, Hydroxyethylcellulose, Hydroxypropylcellulose, Ethylmethylcellulose undExamples of ionic or nonionic gelling agents for the preparation of the agent according to the invention are carmellose, hypromellose, hydroxyethyl cellulose, hydroxypropyl cellulose, ethyl methyl cellulose and
Methylcellulose. Weitere Gelbildner anderer Stoffklassen wie z. B. Stärkederivate können zur Unterstützung der Gelbildung eingesetzt werden.Methylcellulose. Other gelling agents of other substance classes such as B. Starch derivatives can be used to support gel formation.
Herstellungsbeispiel 1 Hydroxyethylcellulose 30.000 3 g Modifizierte Stärke 1 gProduction Example 1 Hydroxyethyl Cellulose 30,000 3 g Modified Starch 1 g
Die Bestandteile werden gemischt und zu einem Granulat verarbeitet.The ingredients are mixed and processed into granules.
Anwendungsbeispiel 1 8 Patienten erhielten an 3 Tagen mit den Mahlzeiten (3x täglich) jeweils 30 g Pflanzenfett. Direkt nach den Mahlzeiten wurden 4 g des im Herstellungsbeispiel 1 beschriebenen Mittels in Wasser eingerührt gegeben. An den folgenden Tagen wurden durchschnittlich täglich etwa 30 g der Nahrungsfette als Fettsäure oder Neutralfette in den Faeces ausgeschieden. Ohne das Mittel gelangen lediglich etwa 8 g Nahrungsfette in den Stuhl. Use Example 1 Eight patients received 30 g of vegetable fat on three days with meals (3 times a day). Immediately after meals, 4 g of the agent described in Preparation 1 were added to water. On the following days, an average of about 30 g of dietary fats were excreted in the faeces as fatty acid or neutral fats. Without the remedy, only about 8 g of dietary fats get into the stool.

Claims

Patentansprücheclaims
Anspruch 1Claim 1
Mittel zur Verhinderung der Resorption von Fetten aus dem Magen- Darm-Trakt, dadurch gekennzeichnet, dass ein Mittel bestehend aus ionischen und/oder nichtionischen Celluloseethern durch Gelbildung im Magen-Darm-Trakt die Fettspaltung und Resorption ganz oder teilweise verhindert.Agent for preventing the absorption of fats from the gastrointestinal tract, characterized in that an agent consisting of ionic and / or nonionic cellulose ethers prevents the splitting and absorption of fat in whole or in part by gel formation in the gastrointestinal tract.
Anspruch 2Claim 2
Mittel nach Anspruch 1 , dadurch gekennzeichnet, dass Carmellose, Hypromellose, Hydroxyethylcellulose, Hydroxypropylcelulose, Ethylmethylcellulose oder Methylcellulose zur Herstellung verwendet werden.Agent according to claim 1, characterized in that carmellose, hypromellose, hydroxyethyl cellulose, hydroxypropyl cellulose, ethyl methyl cellulose or methyl cellulose are used for the preparation.
Anspruch 3Claim 3
Mittel nach Anspruch 1 , dadurch gekennzeichnet, dass zur Unterstützung äer Wirksamkeit Gelbiidner anderer Stoffklassen zugesetzt werden. Agent according to claim 1, characterized in that gel-forming agents of other substance classes are added to support the effectiveness.
PCT/EP2002/013032 2001-12-10 2002-11-21 Use of ionic and non-ionic cellulose ethers for producing a gel-like agent for preventing the resorption of fats from the gastro-intestinal tract WO2003053451A1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2002352075A AU2002352075A1 (en) 2001-12-10 2002-11-21 Use of ionic and non-ionic cellulose ethers for producing a gel-like agent for preventing the resorption of fats from the gastro-intestinal tract

Applications Claiming Priority (2)

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DE10160409A DE10160409A1 (en) 2001-12-10 2001-12-10 Fat resorption composition, useful for treating obesity in humans and animals, comprises ionic and/or nonionic cellulose ether that forms a gel in the gastro-intestinal tract
DE10160409.2 2001-12-10

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EP2088154A1 (en) 2004-03-09 2009-08-12 Ironwood Pharmaceuticals, Inc. Methods and compositions for the treatment of gastrointestinal disorders
JP2010506957A (en) * 2006-10-20 2010-03-04 ダウ グローバル テクノロジーズ インコーポレイティド Use of water-soluble cellulose derivatives to prevent or treat metabolic syndrome
EP2305352A1 (en) 2004-04-02 2011-04-06 Merck Sharp & Dohme Corp. 5-alpha-reductase inhibitors for use in the treatment of men with metabolic and anthropometric disorders
WO2011069038A2 (en) 2009-12-03 2011-06-09 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases
WO2011139763A1 (en) * 2010-04-29 2011-11-10 Dow Global Technologies Llc Methods and compositions for inducing satiety
WO2013138352A1 (en) 2012-03-15 2013-09-19 Synergy Pharmaceuticals Inc. Formulations of guanylate cyclase c agonists and methods of use
WO2014151200A2 (en) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Compositions useful for the treatment of gastrointestinal disorders
WO2014151206A1 (en) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase and their uses
EP2810951A2 (en) 2008-06-04 2014-12-10 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
WO2014197720A2 (en) 2013-06-05 2014-12-11 Synergy Pharmaceuticals, Inc. Ultra-pure agonists of guanylate cyclase c, method of making and using same
EP2998314A1 (en) 2007-06-04 2016-03-23 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
EP3241839A1 (en) 2008-07-16 2017-11-08 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal, inflammation, cancer and other disorders

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EP2348886A1 (en) * 2008-10-17 2011-08-03 Dow Global Technologies LLC Methods of reducing absorption of trans fatty acids using water-insoluble cellulose derivatives
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EP2088154A1 (en) 2004-03-09 2009-08-12 Ironwood Pharmaceuticals, Inc. Methods and compositions for the treatment of gastrointestinal disorders
EP2305352A1 (en) 2004-04-02 2011-04-06 Merck Sharp & Dohme Corp. 5-alpha-reductase inhibitors for use in the treatment of men with metabolic and anthropometric disorders
JP2010506957A (en) * 2006-10-20 2010-03-04 ダウ グローバル テクノロジーズ インコーポレイティド Use of water-soluble cellulose derivatives to prevent or treat metabolic syndrome
EP2998314A1 (en) 2007-06-04 2016-03-23 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
EP2810951A2 (en) 2008-06-04 2014-12-10 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
EP3241839A1 (en) 2008-07-16 2017-11-08 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal, inflammation, cancer and other disorders
WO2011069038A2 (en) 2009-12-03 2011-06-09 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases
EP2923706A1 (en) 2009-12-03 2015-09-30 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia
WO2011139763A1 (en) * 2010-04-29 2011-11-10 Dow Global Technologies Llc Methods and compositions for inducing satiety
JP2013525447A (en) * 2010-04-29 2013-06-20 ダウ グローバル テクノロジーズ エルエルシー Methods and compositions for inducing satiety
CN102905762A (en) * 2010-04-29 2013-01-30 陶氏环球技术有限责任公司 Methods and compositions for inducing satiety
WO2013138352A1 (en) 2012-03-15 2013-09-19 Synergy Pharmaceuticals Inc. Formulations of guanylate cyclase c agonists and methods of use
EP3708179A1 (en) 2012-03-15 2020-09-16 Bausch Health Ireland Limited Formulations of guanylate cyclase c agonists and methods of use
EP4309673A2 (en) 2012-03-15 2024-01-24 Bausch Health Ireland Limited Formulations of guanylate cyclase c agonists and methods of use
WO2014151206A1 (en) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase and their uses
WO2014151200A2 (en) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Compositions useful for the treatment of gastrointestinal disorders
WO2014197720A2 (en) 2013-06-05 2014-12-11 Synergy Pharmaceuticals, Inc. Ultra-pure agonists of guanylate cyclase c, method of making and using same

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