EP1494655A1 - Agent for producing a sensation of satiety and for weight loss - Google Patents

Agent for producing a sensation of satiety and for weight loss

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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Withdrawn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)
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 DE20205854U external-priority patent/DE20205854U1/en
Priority claimed from DE10216551A external-priority patent/DE10216551A1/en
Application filed by SCHUETTE/REICHEL GbR filed Critical SCHUETTE/REICHEL GbR
Publication of EP1494655A1 publication Critical patent/EP1494655A1/en
Withdrawn legal-status Critical Current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

Abstract

The invention relates to an improved agent for producing a sensation of satiety and for weight loss, consisting of a dried, porous gel or foam of at least one anionic polymer, whereby the gel or foam is present as an aluminium salt. The inventive agent is also suitable for controlling cholesterol metabolism.

Description

Mittel zur Erzeugung eines Sättigungseffekts und zur Gewichtsreduktion Means for producing a satiety effect and for reducing weight
Die vorliegende Erfindung betrifft ein Mittel zur Erzeugung eines Sättigungseffekts und zur Gewichtsreduktion. Ferner eignet sich das erfindungsgemäße Mittel ebenso zur Regulierung des Cholesterinhaushalts.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.
Es sind zahlreiche Versuche unternommen worden, auf medikamentösem Weg überflüssige Fettanreicherungen im menschlichen Körper abzubauen beziehungsweise deren Entstehung zu verhindern. Es gibt z.B. sogenannte Appetitzügler, die den Körper auf biochemischem Weg eine Abneigung zur Nahrungsaufnahme zu suggerieren versuchen. Diese Mittel haben zum Teil erhebliche schädliche Nebenwirkungen.Numerous attempts have been made to reduce excess fat accumulations in the human body by medication or to prevent their formation. There are e.g. So-called appetite suppressants, which try to suggest to the body an aversion to food in a biochemical way. Some of these agents have considerable harmful side effects.
Neben den zahlreichen bekannten Diätvorschlägen gibt es auch mechanische und elektromechanische Mittel, mit denen ein gezielter Fettabbau beziehungsweise Muskelaufbau erfolgen soll. Die Wirkung solcher Mittel ist jedoch sehr zweifelhaft.In addition to the numerous known diet proposals, there are also mechanical and electromechanical means with which targeted fat loss or muscle building is to take place. However, the effect of such funds is very doubtful.
Aus der DE 4025912 ist ein Mittel zur oralen Einnahme bekannt, das aus einem im Magen lösbaren und den Inhalt freigebenden Behälter besteht. Dieser ist mit einem Stoff gefüllt, der nach seinem Freisetzen im Magen sein Volumen vergrößert und dadurch dem Körper ein Sättigungsgefühl suggeriert. Nachteil dieses Sättigungsmittels ist, daß die Gefahr von Darmverschlüssen besteht.From DE 4025912 a means for oral administration is known 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.
Ferner sind aus DE 199 42 417 Schwamm-artige Zubereitungen mit stabil vernetzten Querverbindungen bekannt, die im Magen ihr Volumen vergrößern und so ein Sättigungsgefühl hervorrufen. Jedoch erfordert die Herstellung dieser Zubereitungen zusätzliche Verfahrensschritte zur Einführung stabiler Quervernetzungen.Furthermore, from DE 199 42 417 sponge-like preparations with stably cross-linked cross-links are known which increase their volume in the stomach and thus produce a feeling of satiety. However, that requires Production of these preparations additional process steps for the introduction of stable cross-links.
Aufgrund des ständig steigenden Gesundheitsbewußtseins ist jedoch eine weitere Verbesserung von Mitteln zur Erzeugung eines Sättigungseffekts von hoher medizinischer und wirtschaftlicher Relevanz.Due to the constantly increasing health awareness, however, a further improvement of means for producing a satiety effect is of high medical and economic relevance.
Aufgabe der vorliegenden Erfindung ist es, ein verbessertes Mittel zur oralen Einnahme zur Verfügung zu stellen, das eine höhere Magenverweilzeit aufweist als bekannte Mittel seiner Art und dadurch zu einem effektiveren Sättigungseffekt führt. Ferner sollte es zur Gewichtsreduzierung geeignet sein. Ebenso vorteilhaft wäre seine Eignung zur Regulierung des Cholesterinspiegels, da Übergewichtigkeit in der Regel mit einem überhöhten Cholesterinspiegel einhergeht. Darüber hinaus ist eine einfache Herstellung aus preiswerten Rohstoffen wünschenswert, die keine gesundheitlichen Risiken in sich bergen.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.
Die vorliegende Aufgabe wird gelöst, durch ein Mittel zur Erzeugung eines Sättigungseffektes und zur Gewichtsreduktion aus getrocknetem porösen Gel oder Schaum wenigstens eines anionischen Polymers, wobei das Gel oder der Schaum als Aluminiumsalz vorliegt.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.
Erfindungsgemäß bevorzugte anionische Polymere sind Polysaccharide und hier Polyuronsäure-haltige Polysaccharide, wie Alginsäuren und deren Salze (Alginate). Aber auch niederveresterte Pectine, Xanthan, Tragant, Chondroitinsulfat sowie alle anderen Uronsäure-haltigen Verbindungen können erfindungsgemäß zum Einsatz kommen. Denkbar ist auch die Verwendung von synthetischen oder halbsynthetischen Cellulosederivaten, wie z.B. Carboxymethylcellulose oder von Polyacrylaten. Erfindungsgemäß vorteilhaft sind getrocknete Gele oder Schäume enthaltend Mischungen anionischer Polymere, bevorzugt der zuvor erwähnten anionischen Polysaccharide, besonders bevorzugt Mischungen Polyuronsäure-haltiger und niederveresterter Polysaccharide und insbesondere Mischungen enthaltend Salze von Alginsäure und Pektin.Anionic polymers preferred according to the invention are polysaccharides and here polysaccharides containing polyuronic acid, such as alginic acids and their salts (alginates). However, low-esterified pectins, xanthan, tragacanth, chondroitin sulfate and all other compounds containing uronic acid can also be used according to the invention. It is also conceivable to use 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.
Alginsäure ist eine lineare Polyuronsäure aus wechselnden Anteilen von D-Mannuronsäure und L-Guluronsäure, die durch ß-glykosidische Bindungen miteinander verknüpft sind, wobei die Carboxylgruppen nicht verestert sind. Ein Molekül Alginsäure kann sich aus etwa 150-1050 Uronsäure-Einheiten zusammensetzen, wobei das durchschnittliche Molekulargewicht in einem Bereich von 30-200 kDa variieren kann.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 β-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.
Das Polysaccharid Alginsäure ist ein Bestandteil der Zellwänden von Braunalgen. Der Anteil der Alginsäure an der Trockenmasse der Algen kann hierbei bis zu 40% ausmachen. Die Gewinnung der Alginsäure erfolgt durch alkalische Extraktion mit an sich bekannten Methoden gemäß dem Stand der Technik. Die resultierende pulverförmige Alginsäure ist somit rein pflanzlich und weist eine hohe Biokompatibilität auf. Sie kann unter Bildung hochviskoser Lösungen die 300-fache Menge ihres Eigengewichtes an Wasser aufnehmen. In Gegenwart von mehrwertigen Kationen bildet Alginsäure sogenannte Gele. Die Bildung von Alginatgelen in Gegenwart zweiwertiger Kationen, wie Calcium oder Barium, sind bei Shapiro I., et al. (Biomaterials, 1997, 18: 583-90) beschrieben. Letzteres ist aufgrund seiner Toxizität für den Einsatz in Biomedizin jedoch nicht geeignet. Neben Calcium-Chlorid liefert auch Calcium-Glukonat geeignete zweiwertige Kationen. Denkbar ist auch der Einsatz von Magnesium-Salzen oder eine Mischung verschiedener physiologisch unbedenklicher zweiwertiger Kationen. Hinsichtlich der anionischen Polymere ist auch der Einsatz niederveresterter Pektine erfindungsgemäß vorteilhaft. Pektine bestehen aus Ketten von α-1 ,4-glykosidisch verbundenen Galakturonsäure- Einheiten, deren Säuregruppen zu 20-80% mit Methanol verestert sind. Man unterscheidet zwischen hochveresterten (> 50%) und niedrigveresterten (< 50%) Pektinen. Die Molmasse variiert zwischen 10- 500 kDa. Die Gewinnung von Pektinen erfolgt durch saure Extraktion mit an sich bekannten Methoden gemäß dem Stand der Technik aus den inneren Anteilen von Citrusfruchtschalen, Obsttrestem oder Zuckerrübenschnitzeln. Die resultierenden Pektine (Apfel-Pektin, Citrus- Pektin) sind somit rein pflanzlich und weisen eine hohe Biokompatibilität auf. Sie können unter Wasseraufnahme Gele bilden. Auch hier ist der Einsatz von Pektingelen in Gegenwart zweiwertiger Kationen, wie Calcium oder Barium bekannt. Letzteres ist auch hier aufgrund seiner Toxizität für den Einsatz in Biomedizin jedoch nicht geeignet. Neben Calcium-Chlorid liefert auch Calcium-Glukonat geeignete zweiwertige Kationen. Denkbar ist auch der Einsatz von Magnesium- Salzen oder eine Mischung verschiedener physiologisch unbedenklicher zweiwertiger Kationen.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. In the presence of polyvalent cations, 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). Due to its toxicity, the latter is not suitable for use in biomedicine. In addition to calcium chloride, calcium gluconate also provides suitable divalent cations. The use of magnesium salts or a mixture of different physiologically harmless divalent cations is also conceivable. With regard to the anionic polymers, the use of low-ester pectins is also advantageous according to the invention. Pectins consist of chains of α-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. Here too, the use of pectin gels in the presence of divalent cations such as calcium or barium is known. The latter, however, is not suitable for use in biomedicine due to its toxicity. In addition to calcium chloride, calcium gluconate also provides suitable divalent cations. It is also conceivable to use magnesium salts or a mixture of different physiologically harmless divalent cations.
Ferner zeichnet sich der erfindungsgemäße Einsatz von - Pektinen in vorteilhafter Weise dadurch aus, daß Pektine cholesterinsenkende Eigenschaften besitzen. Diese Eigenschaft ist im Sinne der vorliegenden Erfindung von Vorteil, da Übergewicht in der Regel mit einem erhöhten Cholesterinspiegel einhergeht.Furthermore, the use of pectins according to the invention is 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.
Verfahren zur Herstellung von Trockengelen oder Trockenschäumen aus Alginat sind bekannt. Hierbei wird beispielsweise eine Lösung von Natriumalginat in Wasser hergestellt und unter Zugabe von Calciumsalzen eingedickt. Durch Einarbeiten von Luft und ggf. nach Zugabe von Tensiden kann ein Gel oder Schaum erhalten werden. Durch Einfrieren und anschließendes Gefriertrocknen wird aus dem Alginatgel oder - schäum ein Trockengel oder Trockenschaum (Schwamm) hergestellt. Die Herstellung von Pektin-haltigen Gelen oder Schäumen erfolgt in analoger Weise, ebenso wie die Herstellung von Gelen oder Schäumen enthaltend Mischungen anionischer Polymere.Processes for producing dry gels or dry foams from alginate are known. For example, a solution of sodium alginate in water is prepared and thickened with the addition of calcium salts. A gel or foam can be obtained by incorporating air and possibly adding surfactants. By freezing and then freeze-drying a dry gel or dry foam (sponge) is produced from the alginate gel or foam. The production of pectin-containing gels or foams is carried out in an analogous manner, as is the production of gels or foams containing mixtures of anionic polymers.
Neben der Zugabe von anorganischen oder organischen Calciumsalzen, wie z.B. Calciumchlorid oder Calciumglukonat, ist auch die Verwendung von Magnesiumsalzen denkbar sowie von Mischungen verschiedener physiologisch unbedenklicher zweiwertiger Kationen.In addition to the addition of inorganic or organic calcium salts, e.g. Calcium chloride or calcium gluconate, the use of magnesium salts and mixtures of different physiologically acceptable divalent cations is also conceivable.
Erfindungsgemäß besonders bevorzugt erfolgt die Zugabe von Salzen physiologisch unbedenklicher dreiwertiger Kationen, bevorzugt von löslichen Aluminiumsalzen. Hierbei kann die Herstellung der erfindungsgemäßen Mittel durch die Zugabe von löslichen Aluminiumsalzen zu einer wässrigen Lösung von anionischen Polymeren, bevorzugt Alginaten und/oder Pektinen, nach einem Herstellungsverfahren der zuvor beschriebenen Art erfolgen. Besonders geeignete lösliche Aluminiumsalze sind Aluminiumchlorid oder Aluminiumsulfat. Die löslichen Aluminiumsalze können alleine oder in Kombination eingesetzt werden. Erfindungsgemäß können neben den löslichen Aluminiumsalzen, die ihrerseits allein oder in Kombination verwendet werden können, zusätzlich auch noch Salze zweiwertiger Kationen, wie z. B. Calcium- oder Magnesiumsalze oder deren Kombination, bei der Herstellung der erfindungsgemäßen Mittel eingesetzt werden.According to the invention, 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. According to the invention, in addition to the soluble aluminum salts, which in turn can be used alone or in combination, salts of divalent cations, such as. As calcium or magnesium salts or a combination thereof, can be used in the preparation of the agents according to the invention.
Gegenstand der vorliegenden Erfindung ist somit auch eine Verfahren zur Herstellung eines verbesserten Mittels zur Erzielung eines Sättigungseffektes oder zur Gewichtsreduktion, bei dem zur Herstellung eins getrockneten Gels oder Schaums wenigstens eines anionischen Polymers wasserlösliche Salze enthaltend dreiwertige Kationen, bevorzugt Aluminiumsalze, besonders bevorzugt Aluminiumchlorid oder Aluminiumsulfat, eingesetzt werden. Ferner können zusätzlich auch Salze physiologisch unbedenklicher zweiwertiger Kationen eingesetzt werden sowie denkbare Kombinationen von Salzen zwei- und/oder dreiwertiger Kationen. Außerdem ist der Einsatz anionischer Polymere einzeln oder in Kombination erfindungsgemäß umfaßt.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 Aluminum sulfate can be used. Furthermore, salts of physiologically harmless divalent cations can also be used, as well as conceivable combinations of salts of divalent and / or trivalent cations. In addition, the use of anionic polymers is included individually or in combination according to the invention.
Das erfindungsgemäße Mittel zur oralen Einnahme enthält wenigstens ein anionisches Polymer in Form seines Aluminiumsalzes. Vorteilhaft enthält das erfindungsgemäße Mittel als anionisches Polymer Alginat oder Pectin oder eine Kombination davon. Bevorzugt liegt das erfindungsgemäße Mittel als Aluminium-Alginat oder Aluminium-Pektin oder eine Mischung von Aluminium-Alginat und Aluminium-Pektin vor.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.
Das Salz dreiwertiger Kationen, bevorzugt in Form eines Aluminumsalzes, bildet mit den anionischen Polymeren, bevorzugt Alginaten oder Pektinen, einen stabileren Komplex als bislang genutzte Salze zweiwertiger Kationen. Darüber hinaus ist Aluminium im Vergleich mit Barium physiologisch unbedenklich. Die stabilere Wechselwirkung der erfindungsgemäßen anionischen Polymere mit Salzen dreiwertiger Kationen verleiht dem erfindungsgemäßen Mittel die vorteilhafte Eigenschaft, daß es einerseits in Lösungen mit einem pH-Wert von 1 bis 5, bevorzugt von 1 bis 4, besonders bevorzugt in Lösungen mit einem pH- Wert vergleichbar des Magens oder im Magen selbst, unlöslich oder nur schwer löslich ist und sich andererseits in neutralen bis schwach sauren Lösungen mit einem pH-Wert von etwa 6 bis 7, bevorzugt mit einem pH- Wert vergleichbar zu dem des Darms oder im Darm selbst, vollständig auflöst. Die Auflösung des erfindungsgemäßen Mittels enthaltend Aluminium-Alginate beginnt beispielsweise bei einem pK-Wert von etwa 3,3 bis 3,7. Neben dem zuvor beschriebenen Verhalten der erfindungsgemäßen Mittel hinsichtlich ihrer Löslichkeit weisen die Mittel außerdem die vorteilhafte Eigenschaft auf, daß sie eine gesteigerte Formstabilität vorweisen. Diese Formstabilität ist vor allem bei Mitteln enthaltend Mischungen anionischer Polymere in Form ihrer Aluminiumsalze, bevorzugt Mischungen aus Aluminium-Alginat und Aluminium-Pektinat, besonders stark ausgeprägt. Unter Formstabilität ist im Sinne der Erfindung zu verstehen, daß das erfindungsgemäße Mittel enthaltend Aluminiumsalze anionischer Polymere im Vergleich mit Gelen oder Schäumen enthaltend alleine Calciumsalze anionischer Polymere in Lösungen mit einem pH-wert von etwa 1 bis 5 nicht schrumpfen. D.h. bekannte Mittel aus Calciumsalzen anionischer Polymere weisen den Nachteil auf, daß sie in sauren Lösungen mindestens ein Drittel ihres Volumens, meist sogar noch mehr, einbüßen. Der Vorteil der Formstabilität der erfindungsgemäßen Mittel wirkt sich somit direkt positiv auf ihre Eigenschaft zur Erzeugung eines Sättigungseffektes oder zur Gewichtsreduktion aus, da beim Eintritt des erfindungsgemäßen Mittels in den Magen kein Volumenverlust auftritt, wie es bei den bislang bekannten Mitteln der Fall ist. Für diesen Fall ist eine Kompensierung des Volumenverlustes etwa durch Einnahme einer erhöhten Stückzahl an Sättigungsmitteln erfindungsgemäß nicht erforderlich. Dies stellt einen angenehmen Nebeneffekt für den Verbraucher dar.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. In addition, 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. In addition to the behavior of the agents according to the invention described above with regard to their solubility, 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.
Darüber hinaus liegt bei dem erfindungsgemäßen Mittel das Gel oder der Schaum während der Einnahme durch den Patienten bevorzugt in komprimierter Form vor. In einer weiteren Ausführungsform kann das erfindungsgemäße Mittel auch während der Einnahme durch Kau- und/oder Schluckbewegungen komprimiert werden. Durch Aufnahme von Flüssigkeit im Magen erfolgt dann eine Volumenvergrößerung des eingenommen erfindungsgemäßen Mittels, die den gewünschten Effekt der Erzeugung eines Sättigungseffektes, verbunden mit einer Gewichtsreduktion auslöst.In addition, in the agent according to the invention, the gel or the foam is preferably in compressed form during ingestion by the patient. In a further embodiment, 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.
Ferner kann das erfindungsgemäße Mittel beispielsweise in Form von Tabletten, Kapseln, Dragees, als Granulat oder Pulver oder anderen Ausgestaltungen vorliegen. Darüber hinaus kann das erfindungsgemäße Mittel als eine äußere Schicht einen Überzug aufweisen. Erfindungsgemäß kann in einer Variante des erfindungsgemäßen Herstellungsverfahrens eine als Überzug bezeichnete äußere Schicht auf das erfindungsgemäße Mittel aufgebracht werden, die weitere Hilfsstoffe oder Wirkstoffe enthalten kann, wie beispielsweise Verbindungen, die das Schlucken oder Einnehmen des erfindungsgemäßen Mittels erleichtern und dem Fachmann unter „Coating"-Verbindungen oder als Dragiermittel bekannt sind. Diese äußere Schicht kann eine Lackschicht oder andere Schutzschicht sein, die die Einnahme des erfindungsgemäßen Mittels erleichtert und die sich erst im Gastrointestinaltrakt, beispielsweise unter Einfluß der Magenflüssigkeit, auflöst.Furthermore, 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. In addition, the agent according to the invention can have a coating as an outer layer. According to the invention, in a variant of the production method according to the invention, 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.
Das erfindungsgemäße Mittel kann auch weitere Hilfsstoffe und/oder Wirkstoffe enthalten.The agent according to the invention can also contain further auxiliary substances and / or active substances.
Unter „Hilfsstoffen" sind beispielsweise folgende Substanzen zu verstehen, die jedoch nicht limitierend für die vorliegende Erfindung sind: wasserunlösliche Hilfsstoffe oder Gemische davon, wie Lipide, u.a. Fettalkohole, z.B. Cetylalkohol, Stearylalkohol und Cetostearylalkohol; Glyceride, z.B. Glycerinmonostearat oder Gemische von Mono-, Di- und Triglyceriden pflanzlicher Öle; hydrierte Öle, wie hydriertes Rizinusöl oder hydriertes Baumwollsamenöl; Wachse, z.B. Bienenwachs oder Camaubawachs; feste Kohlenwasserstoffe, Z.B. Paraffin oder Erdwachs; Fettsäuren, z.B. Stearinsäure; gewisse Cellulosederivate, z.B. Ethylcellulose oder Acetylcellulose; Polymere oder Copolymere, wie Polyalkylene, z.B. Polyäthylen, Polyvinylverbindungen, z.B. Polyvinylchlorid oder Polyvinylacetat, sowie Vinylchlorid-Vinylacetat- Copolymere und Copolymere mit Crotonsäure, oder Polymere und Copolymere von Acrylaten und Methacrylaten, z.B. Copolymerisate von Acrylsäureester und Methacrylsäuremethylester; oder Tenside, wie z.B. Polysorbat 80 oder Docusat.“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 copolymers and copolymers with crotonic acid, or polymers and copolymers of acrylates and methacrylates, for example copolymers of acrylic acid esters and methacrylic acid methyl esters; or surfactants, such as polysorbate 80 or docusate.
Unter „Wirkstoffen" sind beispielsweise Vitamine, Spurenelemente oder Arzneiwirkstoffe zu verstehen. Folgende Substanzen sind beispielhaft aufgezählt, die jedoch nicht limitierend für die vorliegende Erfindung sind:“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:
Beispiele für Appetitzügler sind: Amfepramon, Fenfluramin, Fenproporex, Levopropylhexedrin, Mazindol, Mefenorex, Metamfepramon, Norephedrin, Norpseudoephedrin. Beispiele für Virustatika sind: Aciclovir, Cidofovir, Didanosin, Famciclovir, Foscarnet, Ganciclovir, Lamivudin, Ritonavir, Zalcitabin, Zidovudin. Beispiele für Vitamine sind: Alfacalcidol, Allithiamine, Ascorbinsäure, Biotin, Calcifediol, Calcitriol, Colecalciferol, Cyanocobalamin, Ergocalciferol, Folsäure, Hydroxocobalamin, Nicotinamid, Pantothensäure, Phytomenadion, Pyridoxin, Retinol, Riboflavin, Thiamin, Tocopherol, Transcalcifediol.Examples of appetite suppressants are: Amfepramon, Fenfluramin, Fenproporex, Levopropylhexedrin, Mazindol, Mefenorex, Metamfepramon, Norephedrin, Norpseudoephedrin. Examples of antivirals are: acyclovir, cidofovir, didanosine, famciclovir, foscarnet, ganciclovir, lamivudine, ritonavir, zalcitabine, zidovudine. Examples of 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.
Unter Umständen kann hier zusätzlich eine retardierende Wirkstofffreisetzung erfolgen.Under certain circumstances, a sustained release of active ingredient can also take place here.
Außer den genannten Hilfsstoffen und Wirkstoffen kann das erfindungsgemäße Mittel zusätzlich Füll- Spreng-, Binde- und Gleitmittel sowie Trägerstoffe enthalten, die auf die Wirkstoffabgabe keinen entscheidenden Einfluß haben. Beispiele sind u.a. Bentonit (Aluminiumoxid-Siliciumoxid-hydrat), Kieselsäure, Cellulose (üblicherweise mikrokristalline Cellulose) oder Cellulosederivate, z.B. Methylcellulose, Natriumcarboxymethylcellulose, Zucker, wie Lactose, Stärken, z.B. Maisstärke oder Derivate davon, z.B. Natriumcarboxymethylstärke, Stärkeleister, Phosphorsäuresalze, z.B. Di- oder Tricalcioumphosphat, Gelatine, Stearinsäure oder geeignete Salze davon, z.B. Magnesiumstearat oder Calciumstearat, Talk, kollodiales Siliciumoxid und ähnliche Hilfsstoffe.In addition to the auxiliaries and active ingredients mentioned, 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.
Die vorliegende Erfindung betrifft auch die Verwendung des erfindungsgemäßen Mittels zur Erzeugung eines Sättigungseffektes und zur Gewichtsreduktion. Ebenso ist die Verwendung des erfindungsgemäßen Mittels zur Regulierung des Cholesterinhaushalts umfaßt.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.
Außerdem ist die Verwendung des erfindungsgemäßen Mittels zur Herstellung einer Zusammensetzung zur Erzeugung eines Sättigungseffektes und zur Gewichtsreduktion denkbar. Gleichsam ist eine Verwendung des erfindungsgemäßen Mittels zur Herstellung einer Zusammensetzung zur Regulierung des Cholesterinhaushalts umfaßt. In addition, the use of the agent according to the invention for producing a composition for producing a saturation effect and for reducing weight is conceivable. Likewise, a use of the agent according to the invention for the preparation of a composition for regulating the cholesterol balance is included.
Die vorliegende Erfindung wird durch die nachfolgenden Beispiele näher charakterisiert, die sich jedoch nicht limitierend auf die Erfindung auswirken:The present invention is characterized in more detail by the following examples, which, however, have no limiting effect on the invention:
Herstellungsbeispiel 1Production Example 1
Natriumalginat 300 gSodium alginate 300 g
Aluminiumchlorid 30 gAluminum chloride 30 g
Wasser 12 1Water 12 1
Herstellungsbeispiel 2Production Example 2
Natriumalginat 400. gSodium alginate 400 g
Aluminiumsulfat 50 gAluminum sulfate 50 g
Wasser 12 1Water 12 1
Herstellungsbeispiel 3Production Example 3
Natriumalginat 200 gSodium alginate 200 g
Apfel- oder Citruspektin 200 gApple or citrus pectin 200 g
Aluminiumchlorid 30 gAluminum chloride 30 g
Wasser 12 1Water 12 1
Herstellungsbeispiel 4Production Example 4
Natriumalginat 400 gSodium alginate 400 g
Magnesiumchlorid 4 gMagnesium chloride 4 g
Aluminiumchlorid 20 gAluminum chloride 20 g
Calciumchlorid 10 gCalcium chloride 10 g
Wasser 12 1Water 12 1
Herstellungsbeispiel 5Production Example 5
Natriumalginat 300 gSodium alginate 300 g
Aluminiumchlorid 30 gAluminum chloride 30 g
Polysorbat 80 20 g Wasser 12 1Polysorbate 80 20 g Water 12 1
Die Lösungen der zuvor genannten Rezepturen werden zu Platten mit einer Dicke von etwa 4 cm gefroren und anschließend im Gefriertrockner getrocknet. Nach der Trocknung kann ggf. eine Komprimierung erfolgen. Anschließend werden aus den Platten die entsprechenden Darreichungsformen, wie z.B. Tabletten oder Kapseln, hergestellt.The solutions of the recipes mentioned above are frozen into plates with a thickness of about 4 cm and then dried in the freeze dryer. After drying, compression may take place. Then the appropriate dosage forms, e.g. Tablets or capsules.
Anwendungsbeispielexample
Getrocknete Aluminiumalginatgele werden in künstlichen Magen- und Darmsäften eingebracht und auf ihre Auflösung untersucht. Dabei sind die erfindungsgemäßen Aluminiumalginattrockengele in Lösungen von einem pH-Wert zwischen 1 ,2 und 4,5 unlöslich. In Lösungen mit pH 7 erfolgt eine vollständige Auflösung der erfindungsgemäßenDried 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
Aluminiumalginattrockengele innerhalb von 30 Minuten. Aluminum alginate dry gels within 30 minutes.

Claims

Ansprüche: Expectations:
1. Mittel zur Erzeugung eines Sättigungseffektes und zur Gewichtsreduktion aus getrocknetem porösen Gel oder Schaum wenigstens eines anionischen Polymers, dadurch gekennzeichnet, daß es als Aluminiumsalz vorliegt.1. Means for producing a saturation effect and for weight reduction from dried porous gel or foam of at least one anionic polymer, characterized in that it is present as an aluminum salt.
2. Mittel gemäß Anspruch 1 , dadurch gekennzeichnet, daß es in komprimierter Form vorliegt.2. Composition according to claim 1, characterized in that it is in compressed form.
3. Mittel gemäß einem der Ansprüche 1 oder 2, dadurch gekennzeichnet, daß es als anionisches Polymer Alginat oder Pectin oder eine Kombination davon enthält.3. Composition according to one of claims 1 or 2, characterized in that it contains alginate or pectin or a combination thereof as the anionic polymer.
4. Mittel gemäß einem der Ansprüche 1 bis 3, dadurch gekennzeichnet, daß es als Aluminium-Alginat, Aluminium-Pektinat oder eine Kombination davon vorliegt.4. Composition according to one of claims 1 to 3, characterized in that it is present as aluminum alginate, aluminum pectinate or a combination thereof.
5. Mittel gemäß einem der Ansprüche 1 bis 4, dadurch gekennzeichnet, daß es zusätzlich Wirkstoffe enthält.5. Agent according to one of claims 1 to 4, characterized in that it additionally contains active ingredients.
6. Mittel gemäß einem der Ansprüche 1 bis 5, dadurch gekennzeichnet, daß es als Wirkstoffe Vitamine, Spurenelemente oder Arzneiwirkstoffe enthält.6. Composition according to one of claims 1 to 5, characterized in that it contains vitamins, trace elements or medicinal active substances as active substances.
7. Mittel gemäß einem der Ansprüche 1 bis 6, dadurch gekennzeichnet, daß es in Form von Tabletten, Kapseln, Dragees, als Granulat oder Pulver verabreicht wird.7. Composition according to one of claims 1 to 6, characterized in that it is administered in the form of tablets, capsules, dragees, as granules or powder.
8. Verwendung eines Mittels gemäß einem der Ansprüche 1 bis 7 zur Erzeugung eines Sättigungseffektes und zur Gewichtsreduktion. 8. Use of an agent according to any one of claims 1 to 7 for producing a saturation effect and for weight reduction.
9. Verwendung eines Mittels gemäß einem der Ansprüche 1 bis 7 zur Regulierung des Cholesterinhaushalts.9. Use of an agent according to one of claims 1 to 7 for regulating the cholesterol balance.
10.Verwendung eines Mittels gemäß einem der Ansprüche 1 bis 7 zur Herstellung einer Zusammensetzung zur Erzeugung eines Sättigungseffektes und zur Gewichtsreduktion.10.Use of an agent according to any one of claims 1 to 7 for the preparation of a composition for producing a satiety effect and for weight reduction.
11. Verwendung eines Mittels gemäß einem der Ansprüche 1 bis 7 zur Herstellung einer Zusammensetzung zur Regulierung des11. Use of an agent according to any one of claims 1 to 7 for the preparation of a composition for regulating the
Cholesterinhaushalts. Cholesterol metabolism.
EP03746298A 2002-04-15 2003-04-15 Agent for producing a sensation of satiety and for weight loss Withdrawn EP1494655A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
DE20205854U DE20205854U1 (en) 2002-04-15 2002-04-15 Means for producing a satiety effect and for reducing weight
DE10216551A DE10216551A1 (en) 2002-04-15 2002-04-15 Orally administered composition for obtaining satiation effect, reducing body weight and regulating cholesterol levels, comprising dried porous gel or foam of anionic polymer in aluminum salt form
DE20205854U 2002-04-15
DE10216551 2002-04-15
PCT/EP2003/003910 WO2003086360A1 (en) 2002-04-15 2003-04-15 Agent for producing a sensation of satiety and for weight loss

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WO (1) WO2003086360A1 (en)

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US20050222082A1 (en) 2005-10-06
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CN1662224A (en) 2005-08-31

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