EP1494655A1 - Mittel zur erzeugung eines s ttigungseffekts und zur gewicht sreduktion - Google Patents

Mittel zur erzeugung eines s ttigungseffekts und zur gewicht sreduktion

Info

Publication number
EP1494655A1
EP1494655A1 EP03746298A EP03746298A EP1494655A1 EP 1494655 A1 EP1494655 A1 EP 1494655A1 EP 03746298 A EP03746298 A EP 03746298A EP 03746298 A EP03746298 A EP 03746298A EP 1494655 A1 EP1494655 A1 EP 1494655A1
Authority
EP
European Patent Office
Prior art keywords
aluminum
agent according
producing
agent
salts
Prior art date
Legal status (The legal status 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 status listed.)
Withdrawn
Application number
EP03746298A
Other languages
German (de)
English (en)
French (fr)
Inventor
Günther Beisel
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
SCHUETTE/REICHEL GBR
Original Assignee
SCHUETTE/REICHEL GbR
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.)
Filing date
Publication date
Priority claimed from DE10216551A external-priority patent/DE10216551A1/de
Priority claimed from DE20205854U external-priority patent/DE20205854U1/de
Application filed by SCHUETTE/REICHEL GbR filed Critical SCHUETTE/REICHEL GbR
Publication of EP1494655A1 publication Critical patent/EP1494655A1/de
Withdrawn legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L29/00—Foods or foodstuffs containing additives; Preparation or treatment thereof
    • A23L29/20—Foods or foodstuffs containing additives; Preparation or treatment thereof containing gelling or thickening agents
    • A23L29/206—Foods or foodstuffs containing additives; Preparation or treatment thereof containing gelling or thickening agents of vegetable origin
    • A23L29/231—Pectin; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L29/00—Foods or foodstuffs containing additives; Preparation or treatment thereof
    • A23L29/20—Foods or foodstuffs containing additives; Preparation or treatment thereof containing gelling or thickening agents
    • A23L29/206—Foods or foodstuffs containing additives; Preparation or treatment thereof containing gelling or thickening agents of vegetable origin
    • A23L29/256—Foods or foodstuffs containing additives; Preparation or treatment thereof containing gelling or thickening agents of vegetable origin from seaweeds, e.g. alginates, agar or carrageenan
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/16—Inorganic salts, minerals or trace elements
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/20—Reducing nutritive value; Dietetic products with reduced nutritive value
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/20—Reducing nutritive value; Dietetic products with reduced nutritive value
    • A23L33/21—Addition of substantially indigestible substances, e.g. dietary fibres
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs

Definitions

  • the present invention relates to a means for producing a satiety effect and for reducing weight. Furthermore, the agent according to the invention is also suitable for regulating the cholesterol balance.
  • a means for oral administration which consists of a container which is detachable in the stomach and releases the contents. This is filled with a substance that increases its volume in the stomach after its release, thereby suggesting a feeling of satiety in the body.
  • the disadvantage of this saturant is that there is a risk of intestinal obstructions.
  • the object of the present invention is to provide an improved oral ingestion agent which has a longer gastric residence time than known agents of its kind and thus leads to a more effective satiety effect. It should also be suitable for weight loss. Its suitability for regulating the cholesterol level would also be advantageous, since obesity is usually accompanied by an elevated cholesterol level. In addition, simple manufacture from inexpensive raw materials that do not pose any health risks is desirable.
  • the present object is achieved by a means for producing a saturation effect and for reducing the weight from dried porous gel or foam of at least one anionic polymer, the gel or the foam being present as an aluminum salt.
  • Anionic polymers preferred according to the invention are polysaccharides and here polysaccharides containing polyuronic acid, such as alginic acids and their salts (alginates).
  • polyuronic acid such as alginic acids and their salts (alginates).
  • alginic acids and their salts alginates
  • low-esterified pectins, xanthan, tragacanth, chondroitin sulfate and all other compounds containing uronic acid can also be used according to the invention.
  • synthetic or semi-synthetic cellulose derivatives such as carboxymethyl cellulose or polyacrylates.
  • Dried gels or foams containing mixtures of anionic polymers preferably the aforementioned anionic polysaccharides, particularly preferably mixtures of polyuronic acid-containing and low-esterified polysaccharides and in particular mixtures containing salts of alginic acid and pectin are advantageous according to the invention.
  • Alginic acid is a linear polyuronic acid consisting of alternating proportions of D-mannuronic acid and L-guluronic acid, which are linked to one another by ⁇ -glycosidic bonds, the carboxyl groups not being esterified.
  • One molecule of alginic acid can be composed of approximately 150-1050 uronic acid units, with the average molecular weight varying in a range of 30-200 kDa.
  • the polysaccharide alginic acid is part of the cell walls of brown algae.
  • the proportion of alginic acid in the dry mass of algae can make up to 40%.
  • the alginic acid is obtained by alkaline extraction using methods known per se according to the prior art.
  • the resulting powdered alginic acid is therefore purely vegetable and has a high level of biocompatibility. It can absorb 300 times its own weight of water, forming highly viscous solutions.
  • alginic acid forms so-called gels.
  • the formation of alginate gels in the presence of divalent cations, such as calcium or barium, is described in Shapiro I., et al. (Biomaterials, 1997, 18: 583-90).
  • Pectins consist of chains of ⁇ -1, 4-glycosidically linked galacturonic acid units, the acid groups of which are 20-80% esterified with methanol. A distinction is made between high-esterified (> 50%) and low-esterified ( ⁇ 50%) pectins. The molar mass varies between 10-500 kDa.
  • Pectins are obtained by acidic extraction using methods known per se according to the prior art from the inner portions of citrus fruit peels, fruit residues or sugar beet pulp.
  • the resulting pectins (apple pectin, citrus pectin) are therefore purely vegetable and are highly biocompatible. They can form gels while absorbing water.
  • divalent cations such as calcium or barium is known. The latter, however, is not suitable for use in biomedicine due to its toxicity.
  • calcium gluconate also provides suitable divalent cations. It is also conceivable to use magnesium salts or a mixture of different physiologically harmless divalent cations.
  • pectins according to the invention are advantageously characterized in that pectins have cholesterol-lowering properties. This property is advantageous in the sense of the present invention, since obesity is generally associated with an elevated cholesterol level.
  • inorganic or organic calcium salts e.g. Calcium chloride or calcium gluconate
  • magnesium salts and mixtures of different physiologically acceptable divalent cations is also conceivable.
  • the addition of salts of physiologically acceptable trivalent cations, preferably of soluble aluminum salts is particularly preferred.
  • the agents according to the invention can be prepared by adding soluble aluminum salts to an aqueous solution of anionic polymers, preferably alginates and / or pectins, using a manufacturing method of the type described above.
  • Particularly suitable soluble aluminum salts are aluminum chloride or aluminum sulfate.
  • the soluble aluminum salts can be used alone or in combination.
  • salts of divalent cations such as.
  • calcium or magnesium salts or a combination thereof can be used in the preparation of the agents according to the invention.
  • the present invention thus also relates to a process for the preparation of an improved agent for achieving a saturation effect or for weight reduction, in which water-soluble salts containing trivalent cations, preferably aluminum salts, particularly preferably aluminum chloride or, are used to produce a dried gel or foam of at least one anionic polymer
  • water-soluble salts containing trivalent cations preferably aluminum salts, particularly preferably aluminum chloride or
  • Aluminum sulfate can be used.
  • salts of physiologically harmless divalent cations can also be used, as well as conceivable combinations of salts of divalent and / or trivalent cations.
  • anionic polymers is included individually or in combination according to the invention.
  • the agent for oral administration according to the invention contains at least one anionic polymer in the form of its aluminum salt.
  • the agent according to the invention advantageously contains alginate or pectin or a combination thereof as an anionic polymer.
  • the agent according to the invention is preferably present as aluminum alginate or aluminum pectin or a mixture of aluminum alginate and aluminum pectin.
  • the salt of trivalent cations preferably in the form of an aluminum salt, forms a more stable complex with the anionic polymers, preferably alginates or pectins, than salts of divalent cations used hitherto.
  • aluminum is physiologically harmless compared to barium.
  • the more stable interaction of the anionic polymers according to the invention with salts of trivalent cations gives the agent according to the invention the advantageous property that it is comparable on the one hand in solutions with a pH of 1 to 5, preferably from 1 to 4, particularly preferably in solutions with a pH of the stomach or in the stomach itself, is insoluble or only sparingly soluble and, on the other hand, completely in neutral to weakly acidic solutions with a pH of about 6 to 7, preferably with a pH comparable to that of the intestine or in the intestine itself dissolves.
  • the dissolution of the agent according to the invention containing aluminum alginates begins, for example, at a pK value of about 3.3 to 3.7.
  • the agents also have the advantageous property that they have an increased dimensional stability.
  • This dimensional stability is particularly pronounced in compositions containing mixtures of anionic polymers in the form of their aluminum salts, preferably mixtures of aluminum alginate and aluminum pectinate.
  • Dimensional stability in the sense of the invention means that the composition according to the invention containing aluminum salts of anionic polymers does not shrink in comparison with gels or foams containing only calcium salts of anionic polymers in solutions with a pH of about 1 to 5. That is, known agents from calcium salts of anionic polymers have the disadvantage that they lose at least a third of their volume, usually even more, in acidic solutions.
  • the advantage of the dimensional stability of the agents according to the invention thus has a directly positive effect on their property for producing a satiety effect or for weight reduction, since there is no loss of volume when the agent according to the invention enters the stomach, as is the case with the agents known to date. In this case, compensation for the loss of volume, for example by taking an increased number of saturants, is not necessary according to the invention. This is a pleasant side effect for the consumer.
  • the gel or the foam is preferably in compressed form during ingestion by the patient.
  • the agent according to the invention can also be compressed during ingestion by chewing and / or swallowing movements. The absorption of liquid in the stomach then increases the volume of the agent according to the invention which has the desired effect the generation of a satiety effect, combined with a weight reduction.
  • the agent according to the invention can be present, for example, in the form of tablets, capsules, coated tablets, granules or powder or other configurations.
  • the agent according to the invention can have a coating as an outer layer.
  • an outer layer referred to as a coating can be applied to the agent according to the invention, which may contain further auxiliaries or active ingredients, such as, for example, compounds which make swallowing or taking the agent according to the invention easier and known to the person skilled in the art under "coating"
  • This outer layer can be a lacquer layer or other protective layer which makes it easier to take the agent according to the invention and which only dissolves in the gastrointestinal tract, for example under the influence of gastric fluid.
  • the agent according to the invention can also contain further auxiliary substances and / or active substances.
  • auxiliaries are understood to mean, for example, the following substances, which, however, are not limiting for the present invention: water-insoluble auxiliaries or mixtures thereof, such as lipids, including fatty alcohols, for example cetyl alcohol, stearyl alcohol and cetostearyl alcohol; glycerides, for example glycerol monostearate or mixtures of mono-, Di- and triglycerides of vegetable oils; hydrogenated oils, such as hydrogenated castor oil or hydrogenated cottonseed oil; waxes, for example beeswax or camauba wax; solid hydrocarbons, for example paraffin or earth wax; fatty acids, for example stearic acid; certain cellulose derivatives, for example ethyl cellulose or acetyl cellulose; polymers or copolymers, such as Polyalkylenes, for example polyethylene, polyvinyl compounds, for example polyvinyl chloride or polyvinyl acetate, and also vinyl chloride-vinyl acetate copoly
  • Active ingredients are to be understood as meaning, for example, vitamins, trace elements or pharmaceutical active ingredients.
  • the following substances are listed by way of example, but are not limiting for the present invention:
  • appetite suppressants are: Amfepramon, Fenfluramin, Fenproporex, Levopropylhexedrin, Mazindol, Mefenorex, Metamfepramon, Norephedrin, Norpseudoephedrin.
  • antivirals are: acyclovir, cidofovir, didanosine, famciclovir, foscarnet, ganciclovir, lamivudine, ritonavir, zalcitabine, zidovudine.
  • vitamins are: alfacalcidol, allithiamine, ascorbic acid, biotin, calcifediol, calcitriol, colecalciferol, cyanocobalamin, ergocalciferol, folic acid, hydroxocobalamin, nicotinamide, pantothenic acid, phytomenadione, pyridoxine, retinol, riboflavocifone, thiolamine, transiolamine, thiolamine.
  • the agent according to the invention can additionally contain fillers, disintegrants, binders and lubricants and carriers which have no decisive influence on the release of active ingredients.
  • examples include bentonite (aluminum oxide-silicon oxide hydrate), silica, cellulose (usually microcrystalline cellulose) or cellulose derivatives, for example methyl cellulose, Sodium carboxymethyl cellulose, sugars such as lactose, starches, for example maize starch or derivatives thereof, for example sodium carboxymethyl starch, starch starch, phosphoric acid salts, for example di- or tricalcium phosphate, gelatin, stearic acid or suitable salts thereof, for example magnesium stearate or calcium stearate, talc, colloidal silicon oxide and similar auxiliaries.
  • the present invention also relates to the use of the agent according to the invention for producing a saturation effect and for reducing weight.
  • the use of the agent according to the invention for regulating the cholesterol balance is also included.
  • the agent according to the invention for producing a composition for producing a saturation effect and for reducing weight is conceivable.
  • a use of the agent according to the invention for the preparation of a composition for regulating the cholesterol balance is included.
  • Dried aluminum alginate gels are placed in artificial gastric and intestinal juices and examined for their dissolution.
  • the aluminum alginate dry gels according to the invention are insoluble in solutions with a pH between 1, 2 and 4.5.
  • the solutions according to the invention are completely dissolved in solutions with pH 7

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Food Science & Technology (AREA)
  • Nutrition Science (AREA)
  • Polymers & Plastics (AREA)
  • Mycology (AREA)
  • Dispersion Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Inorganic Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Child & Adolescent Psychology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
EP03746298A 2002-04-15 2003-04-15 Mittel zur erzeugung eines s ttigungseffekts und zur gewicht sreduktion Withdrawn EP1494655A1 (de)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
DE20205854U 2002-04-15
DE10216551A DE10216551A1 (de) 2002-04-15 2002-04-15 Mittel zur Erzeugung eines Sättigungseffektes und zur Gewichtsreduktion
DE20205854U DE20205854U1 (de) 2002-04-15 2002-04-15 Mittel zur Erzeugung eines Sättigungseffektes und zur Gewichtsreduktion
DE10216551 2002-04-15
PCT/EP2003/003910 WO2003086360A1 (de) 2002-04-15 2003-04-15 Mittel zur erzeugung eines sättigungseffekts und zur gewichtsreduktion

Publications (1)

Publication Number Publication Date
EP1494655A1 true EP1494655A1 (de) 2005-01-12

Family

ID=29251758

Family Applications (1)

Application Number Title Priority Date Filing Date
EP03746298A Withdrawn EP1494655A1 (de) 2002-04-15 2003-04-15 Mittel zur erzeugung eines s ttigungseffekts und zur gewicht sreduktion

Country Status (5)

Country Link
US (1) US20050222082A1 (zh)
EP (1) EP1494655A1 (zh)
CN (1) CN1662224B (zh)
AU (1) AU2003226811A1 (zh)
WO (1) WO2003086360A1 (zh)

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US8057420B2 (en) 2003-12-09 2011-11-15 Gi Dynamics, Inc. Gastrointestinal implant with drawstring
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CN101528054B (zh) * 2006-10-17 2013-03-13 荷兰联合利华有限公司 包含气泡的食品组合物及其制备方法
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Also Published As

Publication number Publication date
CN1662224A (zh) 2005-08-31
AU2003226811A1 (en) 2003-10-27
CN1662224B (zh) 2010-09-08
WO2003086360A1 (de) 2003-10-23
US20050222082A1 (en) 2005-10-06

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