DE20219665U1 - Composition for treatment of obesity in animals, comprising insoluble material swellable in gastrointestinal fluid, and an animal attractant - Google Patents

Abstract

A composition for inducing satiety and treating obesity in animals comprises a swellable material (I) which is insoluble or sparingly soluble in gastrointestinal fluid and/or body fluids, and at least one attractant (II) for the particular species of animal. ACTIVITY : Anorectic. MECHANISM OF ACTION : None given.

Description

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Means for producing a satiety effect and for weight reduction in

Animals

The present invention relates to an agent for producing a satiety effect and for weight reduction in animals.

Numerous attempts have been made to use medication to reduce excess fat accumulation in the human body or to prevent it from forming. There are, for example, so-called appetite suppressants that attempt to biochemically make the body averse to eating. Some of these drugs have significant harmful side effects.

In addition to the numerous well-known diet suggestions, there are also mechanical and electromechanical means that are intended to achieve targeted fat loss or muscle building. However, the effectiveness of such means is very doubtful.

DE 4025912 describes a product for oral consumption that consists of a container that can be dissolved in the stomach and releases its contents. This is filled with a substance that increases its volume after being released in the stomach, thereby giving the body a feeling of satiety. The disadvantage of this satiety agent is that there is a risk of intestinal obstruction.

Furthermore, DE 199 42 417 discloses sponge-like preparations with stable cross-linked compounds that increase their volume in the stomach and thus cause a feeling of satiety. However, the production of these preparations requires additional process steps to introduce stable cross-links.

However, all previous experiments have focused on weight reduction in humans. However, the problem of obesity also exists in pets.

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The object of the present invention is therefore to provide an agent which is suitable for the treatment of obesity in animals.

This object is achieved according to the invention by an agent for producing a satiety effect and for weight reduction in animals, comprising a volume-increasing material which is insoluble or sparingly soluble in gastrointestinal fluids and/or body fluids and at least one attractant which is effective for the respective animal species.

According to the invention, the main attractants considered are flavorings. The term flavoring refers to a sensory impression that the flavorings create. According to DIN 10950, the flavoring is the overall olfactory impression of volatile substances in a sample. It differs from smell in that many of the flavorings are only released when chewing, through the warmth of the oral cavity, etc., and then contribute to the sensation via the throat-nose connection.

According to the invention, natural and nature-identical flavorings can be used. Examples of such flavorings include hydrocarbons, heterocyclics, alcohols, aldehydes, ketones, acetols, esters, phenols, phenol ethers, sulfides, thiols, proteins, amino acids. Examples of heterocyclic compounds are furans, furanones, thiophenes, pyrazines, thiazoles. Preferably, according to the invention, meat, sausage, cheese and/or yeast flavorings are considered. Accordingly, meat, cheese or yeast extracts can be added to the volume-increasing material according to the invention.

The attractants can be incorporated into the volume-increasing material. It is also possible to apply the attractants to a volume-increasing material that already contains incorporated attractants.
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In a further variant of the invention, the attractants can be applied to the surface or part of the surface of the volume-increasing material. Suitable adhesion promoters can be used for this purpose.

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Solid, semi-solid or liquid substances can be used as adhesion promoters. These can be powders, pastes, solutions, melts or films. In the latter case, for example, a film-shaped adhesion promoter layer can have adhesive properties on both sides and in this way ensure that the carrier material adheres to the layer containing the active ingredient.

Compounds that contain natural, synthetic and semi-synthetic polymers are preferred as adhesion promoters. In principle, non-ionic and ionic polymers are suitable. In principle, all hot melt adhesives and contact adhesives known in the art are suitable, provided they are suitable for pharmaceuticals or foodstuffs. In a particular embodiment of the present invention, the adhesion promoter is starch derivatives, cellulose derivatives, gelatin or polysaccharides, preferably polysaccharides containing polyuronic acid, e.g. polyalginates. Examples include hypomellose, carmellose and metholose.

Particularly preferred polysaccharides containing polyuronic acid are alginic acids and their salts (alginates). However, low-ester pectins, xanthan, tragacanth, chondroitin sulfate and all other uronic acid-containing compounds can also be used according to the invention.

By applying this connecting layer to the active ingredient formulation and/or the carrier material, a connection is achieved between the carrier material, which may be compressed and increases the volume in the gastrointestinal tract, and the active ingredient layer. The duration of the existing connection depends on the solubility of the substances used and contained in the connecting layer in gastric juice and/or other gastrointestinal fluids.

Furthermore, the use of thread-like or fabric-like material is also conceivable, by means of which the desired duration of the connection between the carrier material and the active substance-containing layer can be controlled. Accordingly, an agent containing thread-like and/or fabric-like materials as a connecting agent is also the subject of the invention.

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By means of the described adhesion promoter, in addition to the attractants, formulations containing active ingredients can also be applied to the volume-increasing material.
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According to the invention, it is therefore possible, for example, to treat obesity causally and at the same time symptomatically in one medication. For example, a blood pressure-lowering agent can be firmly applied to the carrier material, which reduces food intake and thus weight by creating a feeling of satiety. Since weight reduction can also reduce high blood pressure, the use of the combination preparation described leads to an improvement in effectiveness and therapy compared to the respective individual administration.

After ingestion of the agent according to the invention using the described adhesion promoters, it is broken down in the stomach into material with increased volume and layer(s) containing the active ingredient-containing formulation(s). The active ingredient-containing formulation(s) can therefore reach the intestine, i.e. can be absorbed in the intestine.

The volume-increasing material according to the invention ensures the low-nutritional/low-calorie volume increase of the release system required to develop the satiety effect. The material is therefore larger than the opening of the stomach outlet and is thus prevented from being transported quickly from the stomach to the intestine, i.e. the residence time in the stomach for the carrier material is longer than for the layer containing the active ingredient. As a result of the residence time of the carrier material in the stomach, a feeling of satiety is induced and maintained for the time it remains in the stomach.

According to the invention, it is also possible to combine different active ingredients. For example, in addition to the described adhesion promoter that is soluble in the stomach, an adhesion promoter that does not dissolve in the stomach can be used. Active ingredients that are intended to remain in the stomach and develop their effect there are then applied to this adhesion promoter.

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Furthermore, according to the invention it is possible to bond several volume-increasing pieces of material of the same or different composition together. When the described adhesion promoter, which is soluble in the stomach, is used, these pieces of material detach from one another. This can achieve an increased saturation effect. In such a system, the active ingredients can be arranged between several pieces of material using the adhesion promoter. When the individual pieces of material fall apart in the stomach, the layers of active ingredients detach and reach the intestine to exert their effect there. If necessary, active ingredients can also be used that at least partially dissolve in the stomach and possibly exert their therapeutic effect there.

According to the invention, preferably sponge-like materials can be used as volume-increasing materials. According to the invention, such sponge-like materials are to be understood as solid or semi-solid elastic foams which consist of gas-filled, for example polyhedral cells which are delimited by highly viscous and/or solid cell webs. According to the invention, both naturally occurring sponges and semi-synthetic or synthetically produced sponge-like structures can be used. Examples of synthetic

Sponge-like materials are polyurethanes, polyacrylates,

Poly(met)acrylic acid derivatives, homo- and copolymers of vinyl acetate. Natural and semi-synthetic polymers include cellulose, cellulose ethers or cellulose esters such as cellulose acetate and cellulose acetate phthalate. Examples of natural polymers are polysaccharides such as alginates, tragacanth, xanthan gum, guar gum and their salts and derivatives. The use of chitin and chitin derivatives is possible. Furthermore, substances with a fiber structure such as scleroproteins, e.g. collagen, keratin, conchagens, fibroin, elastin and chitin are preferably used. In addition, stably cross-linked polysaccharides are also the subject of the present invention.

The production of the sponge-like or sponge-shaped structures is carried out using known methods according to the state of the art. Reference is made, for example, to PCT/EP96/03950. Depending on the starting material used, in the simplest case a foam can be produced by blowing in, by

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Beating, shaking, spraying or stirring in the relevant gas atmosphere. In polymers, the foam structure is created by chemical reactions. For example, foaming is achieved by adding blowing agents that decompose at a certain temperature during processing to form gas, or by adding liquid solvents during polymerization. Foaming occurs either when the material leaves the extrusion tool, i.e. after extrusion or injection molding, or in open molds. Curing occurs under the conditions characteristic of the respective chemical compound of the carrier material.

An essential property of the volume-increasing material according to the invention is that it is compressible. Finally, when selecting the carrier material, it is also essential that it remains capable of swelling without destroying the cell webs.

Under physiological conditions, the compressed material can expand, for example, to two to ten times its volume, preferably four to eight times. The active ingredient release areas of the material enlarged under physiological conditions are, for example, 15 to 25 cm ² . In comparison, the values of the release areas according to the state of the art are 0.5 to 1.5 cm ² .

In the agent according to the invention, the material is therefore preferably in compressed form before and/or during ingestion.

Furthermore, the agent according to the invention can be in the form of tablets, capsules, dragees, granules or suppositories or other forms. In addition, the agent according to the invention can have a coating as an outer layer. This can be a lacquer layer or other protective layer that makes it easier to take the agent according to the invention and that only dissolves in the gastrointestinal tract, for example under the influence of gastric fluid.

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In a further preferred variant of the invention, the volume-increasing material according to the invention can also be in the form of powder. According to the invention, this can include finely divided powders, granules, adsorbates and beadlets. Preferably, volume-increasing materials can be produced from dried porous gel or foam. Anionic polymers are preferably used as materials.

Preferred anionic polymers according to the invention are polysaccharides, and here polyuronic acid-containing polysaccharides, such as alginic acids and their salts (alginates).

However, low-ester pectins, xanthan, tragacanth, chondroitin sulfate and all other compounds containing uronic acid can also be used according to the invention. The use of synthetic or semi-synthetic cellulose derivatives, such as carboxymethylcellulose or polyacrylates, is also conceivable. This means that the polysaccharides containing polyuronic acid that are suitable for use as adhesion promoters are also suitable for producing the volume-increasing material.

Advantageous according to the invention can be dried gels or foams containing mixtures of anionic polymers, preferably of the previously mentioned anionic polysaccharides, particularly preferably mixtures of polyuronic acid-containing and low-esterified polysaccharides and in particular mixtures containing salts of alginic acid and pectin.

Alginic acid is a linear polyuronic acid made up of varying proportions of D-mannuronic acid and L-guluronic acid linked together by ß-glycosidic bonds, with the carboxyl groups not esterified. One molecule of alginic acid can consist of about 150-1050 uronic acid units, with the average molecular weight varying in the range of 30-200 kDa.
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The polysaccharide alginic acid is a component of the cell walls of brown algae. The proportion of alginic acid in the dry mass of the algae can be up to 40%. The alginic acid is obtained by alkaline extraction using known methods in accordance with the state of the art. The resulting

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Powdered alginic acid is therefore purely plant-based and highly biocompatible. It can absorb 300 times its own weight in water to form 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 by Shapiro L, et al. (Biomaterials, 1997, 18: 583-90). The latter is not suitable for use in biomedicine due to its toxicity. In addition to calcium chloride, calcium gluconate also provides suitable divalent cations. The use of magnesium salts or a mixture of various physiologically harmless divalent cations is also conceivable.

Low-ester pectins are preferably used as pectins. Such pectins consist of chains of oc-1,4-glycosidically linked galacturonic acid units, the acid groups of which are 20-80% esterified with methanol. A distinction is made between high-ester (> 50%) and low-ester (< 50%) pectins. The molecular weight varies between 10-500 kDa. Pectins are obtained by acid extraction using known methods in accordance with the state of the art from the inner parts of citrus fruit peels, fruit pomace or sugar beet pulp. The resulting pectins (apple pectin, citrus pectin) are therefore purely plant-based and have a high level of biocompatibility. They can form gels when absorbed by water.

Here too, the use of pectin gels in the presence of divalent cations such as calcium or barium is known. However, the latter is not suitable for use in biomedicine due to its toxicity. In addition to calcium chloride, calcium gluconate also provides suitable divalent cations. The use of magnesium salts or a mixture of various physiologically harmless divalent cations is also conceivable.

Furthermore, the use of pectins according to the invention is advantageously characterized by the fact that pectins have cholesterol-lowering properties. This property is advantageous in the sense of the present invention, since excess weight is usually associated with an increased cholesterol level.

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The powdered volume-increasing materials can be produced in various ways. For example, for production in the form of an adsorbate, one or more carriers can be placed in a mixer or in a fluidized bed reactor and then the other components can be added. The carriers are preferably the volume-increasing materials according to the invention. According to the invention, discontinuous or continuous mixers can be used. The carrier material or volume-increasing material is optionally placed together with additives. Classic examples are flight share mixers, conical screw mixers or similar devices. Alternatively, the product can be mixed by moving the entire container. Examples of these are tumble mixers, drum mixers or others. Another possibility is to use pneumatic mixers.

The powdered agents according to the invention can also be produced by spray formulation methods. In this case, for example, in a first step an aqueous solution of a protective colloid, e.g. gelatin and/or gelatin derivatives, and/or gelatin substitutes can be prepared with the addition of the volume-increasing materials described above and a dispersion can first be prepared by adding the attractants and active ingredients while stirring, the aqueous solution of the colloid representing the homogeneous phase of the dispersion. Apparatus in which such spray formulations can be produced are described, for example, in EP 0074050 B1.

Granules can be produced by mixing the volume-increasing substances according to the invention and/or spray-dried powders as well as attractants and, if necessary, active components and binding agents and additives to produce compact granules in a mixer. For example, paddle mixers or flight-share mixers can be used as mixers. The liquid components can be added in various ways, e.g. dripped on or sprayed on, so that a pasty, sticky mass is created. The pasty mass is broken up by selecting the appropriate speed of the mixing tools and/or high-speed blades and

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compact granules. Very large chunks can be broken up using mixing tools and knives and fine powders can be agglomerated.

In another process variant, a solution of sodium alginate in water can be prepared and thickened by adding calcium salts. A gel or foam can be obtained by incorporating air and, if necessary, adding surfactants. A dry gel or dry foam (sponge) can be produced from the alginate gel or foam by freezing and then freeze-drying. 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.

The addition of coating layers, which can contain the attractants for the animals, can be carried out after the powders or granules have been produced in mixers at a lower speed of the mixing tools and stationary knives or in a downstream mixer of a similar design. The shaping of the agents according to the invention can be carried out by pressing the pasty, sticky phases through the die of an extruder during the granulation process.

The dosing or addition of attractants can be carried out together with additives, e.g. using dripping or spraying devices. Examples of this are lances, shower heads, single-component or multi-component nozzles, and in rare cases rotating dripping or atomizing devices. In the simplest case, the addition is also possible locally as a concentrated jet. Alternatively, the attractant can be placed in the mixer first and then the volume-increasing material can be added. The attractant can be added at overpressure, normal pressure or underpressure, counter atmosphere, preferably at normal pressure or underpressure. To increase the load of the volume-increasing material and to minimize the influence of oxygen, it can be advantageous to evacuate the mixer containing the volume-increasing material before adding the attractant and, if necessary, to cover it with protective gas.

The volume-increasing material according to the invention as well as the attractants used can also contain further auxiliary substances, whereby these can be

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volume-increasing material or the attractants can be applied and/or incorporated into the volume-increasing material.

For example, in addition to the addition of inorganic or organic calcium salts, such as calcium chloride or calcium gluconate, the use of magnesium salts is also conceivable, as well as mixtures of various physiologically harmless divalent cations.

According to the invention, salts of physiologically acceptable trivalent cations, e.g. soluble aluminum salts, can also be added. The preparation of the agents according to the invention can be carried out by adding soluble aluminum salts to an aqueous solution of anionic polymers, preferably alginates and/or pectins, according to a production process 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 calcium or magnesium salts or a combination thereof, can also be used in the preparation of the agents according to the invention.

Furthermore, the following excipients can also be added: water-insoluble excipients or mixtures thereof, such as lipids, including fatty alcohols, e.g. cetyl alcohol, stearyl alcohol and cetostearyl alcohol; glycerides, e.g. glycerol monostearate or mixtures of mono-, di- and triglycerides of vegetable oils; hydrogenated oils, such as hydrogenated castor oil or hydrogenated cottonseed oil; waxes, e.g. beeswax or carnauba wax; solid hydrocarbons, e.g. paraffin or petroleum wax; fatty acids, e.g. stearic acid; certain cellulose derivatives, e.g. ethylcellulose or acetylcellulose; Polymers or copolymers, such as polyalkylenes, e.g. polyethylene, polyvinyl compounds, e.g. polyvinyl chloride or polyvinyl acetate, as well as vinyl chloride-vinyl acetate copolymers and copolymers with crotonic acid, or polymers and copolymers of acrylates and methacrylates, e.g. copolymers of acrylic acid ester and methyl methacrylate, can be used.

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In addition to the excipients mentioned, the agents according to the present invention can also contain fillers, disintegrants, binders and lubricants as well as carriers which have no decisive influence on the release of the active ingredient. Examples include bentonite (aluminum oxide-silicon oxide hydrate), silica, cellulose (usually microcrystalline cellulose) or cellulose derivatives, e.g. methylcellulose, sodium carboxymethylcellulose, sugars such as lactose, starches, e.g. corn starch or derivatives thereof, e.g. sodium carboxymethyl starch, starch esters, phosphoric acid salts, e.g. di- or tricalcium phosphate, gelatin, stearic acid or suitable salts thereof, e.g. magnesium stearate or calcium stearate, talc, colloidal silicon oxide and similar excipients.

In addition to the attractants described, active substances can also be applied to the volume-increasing material described, preferably using the adhesion promoters described. The active substances can also be applied directly in combination with the attractants if, for example, they contain adhesion-promoting substances or develop adhesion-promoting properties under pressure or temperature. Finally, the active substances can be incorporated into the volume-increasing material in the same way as the attractants.

For the purposes of the invention, active ingredient means all substances with a pharmaceutical or biological effect. Examples of active ingredient-containing formulations from different therapeutic classes according to the invention are given below, but these are not limiting for the present invention.

Examples of ACE inhibitors are: Benazepril, Captopril, Cilazapril, Enalapril, Fosinopril, Lisinopril, Perinodopril, Quinapril, Ramipril, Trandolopril.
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Examples of analeptics are: almitrine, amiphenazole, caffeine, doxapram, etamivan, fominoben, metamfetamine, nicethamide, pentetrazol.

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Examples of analgesics (opioids) are: alfentanil, buprenorphine, cetobemidone, dextromoramide, dextropropoxyphene, fentanyl, flupirtine, hydromorphone, levomethadone, levorphanol, meptazinol, morphine, nalbuphine, oxycodone, pentazocine, pethidine, piritramide, tilidine, tramadol.
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Examples of analgesics (non-opioids) are: acetylsalicylic acid, benzyl mandelate, bucetin, ethenzamide, ketorolac, metamizole, morazon, paracetamol, phenacetin, phenazone, propyphenazone, salicylamide.

Examples of anthelmintics are: albendazole, diethylcarbamazine, mebendazole, praziquantel, tiabendazole.

Examples of antiallergics/antihistamines are: anatazoline, astemizole, azelastine, bamipine, brompheniramine, buclizine, carbinoxamine, cetririzine, chlorphenamine, clemastine, cyslizine, cyproheptadine, dimenhydramine, doxylamine, fexofenadine, ketotifen, loratadine, mepyramine, mizolastine, nedrocromil, oxatomide, oxomemazine, pheniramine, phenyltoloxamine, spaglumic acid, terfenadine, triprolidine.

Examples of antiarrhythmics are: ajmaline, amiodarone, aprindine, quinidine, disopyramide, mexiletine, procainamide, propafenone, tocainide.

Examples of antibiotics/chemotherapeutics are: Amikacin, Gentamicin, Kanamycin, Paromomycin, Sisomicin, Streptomycin Tobramycin, Chloroquine, Halofantrin, Hydroxychloroquine, Mefloquine, Proguanil, Ethambutol, Isoniazid, Rifabutin, Rifampicin, Cefacetril, Cefaclor, Cefadroxil, Cefalexin, Cefalotin, Cefamandole, Cefazolin, Cefixime, Cefmenoxime, Cefoperazone, Cefotaxime, Cefotetan, Cefotiam, Cefoxitin, Cefpodoxime (proxetil), Cefradine, Cefsulodin, Ceftazidime, Ceftizoxime, Ceftriaxone, Cefuroxime (axetil), Latamoxef, Cinoxacin, Ciprofloxacin, Enoxacin, Nalidixic acid, norfloxacin, Ofloxacin, pipemic acid, rosoxacin, clarithromycin, erythromycin, roxithromycin, amoxicillin, ampicillin, apalcillin, azidocillin, azlocillin, bacampicillin, benzylpenicillin, carbenicillin, carindacillin, dicloxacillin, flucloxacillin, mezlocillin, oxacillin, phenoxymethypenicillin, piperacillin , pivampicillin, propicillin, ticarcillin, colistin, Teicoplanin, vancomycin, cotrimoxazole, sulfametoxydiazine,

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Doxycycline, Oxytetracyline, Tetracycline, Atovaquone, Chloramphenicol, Fosfomycin, Imipenem, Metronidalzole, Nitrofurantoin, Pentamidine, Taurolidine, Trimethoprim.

Examples of antidepressants are: amitriptyline, amitriptyline oxide, clomipramine, desipramine, dibenzepine, dosulepin, doxepin, fluoxetine, fluvoyamine, imipramine, lithium salts, maprotiline, nomifensine, opipramol, oxitriptan, tranylcypromine, trimipramine, tryptophan.

Examples of antidiabetics / antihypoglycemics are: acarbose, carbutamide, chlorpropamide, glibenclamide, glibornuride, gliclazide, glimepiride, glipizide, gliquidone, glisoxepide, glymidine, guar, insulin, metformin, tolazamide, tolbutamide.

Examples of antidiarrheals are: difenoxin, diphenoxylate, loperamide, petin, tannin.
Examples of antidotes are: flumazenil, naloxone, naltrexone.

Examples of antiemetics are: alizaprid, betahistine, thiethylperazine.

Examples of antiepileptic drugs are: barbexaclone, carbamazepine, ethosuximide, lamotrigine, mepacrine, mesuximide, phenobarbital, phenytoin, primidone, sulthiame, trimethadione, valproic acid, vigabatrin.

Examples of antifibrinolytics are: aminocaproic acid, 4-(aminomethyl)benzoic acid, tranexamic acid.
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Examples of antihypertensives are: clonidine, diazoxide, doxazosin, guanethidine, hydralazine, methyldopa, moxonidine, sodium nitroprusside, phentolamine, prazosin, reserpine, tiamenidine, urapidil.

Examples of antihypotents are: dihydroergotamine, dobutamine, dopamine, etilefrine, norepinephrine, norfennephrine.

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Examples of anticoagulants are: acenocoumarol, dalteparin sodium, enoxaparin, heparin, heparinoids, hirudin, lepirudin, nadroparin, parnaparin, phenprocoumon, reviparin, tinzaparin, warfarin.

Examples of antifungals are: Amorolfine, Amphotericin B, Bifonazole, Chlormidazole, Ciclopiroxolamine, Clotrimazole, Croconazole, Econazole, Fenticonalzole, Fluconazole, Griseofulvin, Isoconazole, Itraconazole, Ketoconazole, Miconazole, Naftifin, Naystatin, Omoconazole, Oxiconazole, Terbinafine, Terconazole, Tioconazole, Tolnaftate.

Examples of antirheumatics are: Acemetacin, azapropazone, benorilate, bumadizone, carprofen, choline salicylate, diclofenac, diflunisal, etofenamate, felbinac, fenbufen, fenoprofen, flufenamic acid, flurbiprofen, ibuprofen, indomethacin, isoxicam, ketoprofen, lonazolac, mefenamic acid, meloxicam, mofebutazone, nabumetone, naproxen, nifenazone, niflumic acid, oxyphenbutazone, phenylbutazone, piroxicam, pirprofen, proglumetacin, pyrazinobutazone, salsalate, sulindac, suxibuzone, tenoxicam, tiaprofenic acid, tolmetin, auranofin, aurothioglucose, aurothiomalate, aurothioplypeptide, chloroquine, hydroxychloroquine, Penicillamine, Ademetionine, Benzydamine, Bufexamac, Famprofazone, Glucosamine, Oxaceprol.

Examples of antitussives are: benproperin, butamirate, butetamate, clobutinol, clofedanol, codeine, dextromethorphan, dihydrocodeine, hydrocodone, isoaminil, sodium dibunate, noscapine, oxeladine, pentoxyverine, pholcodine, pipacetate.

Examples of appetite suppressants are: amfepramone, fenfluramine, fenproporex, levopropylhexedrine, mazindol, mefenorex, metamfepramone, norephedrine, norpseudoephedrine.

Examples of beta-receptor blockers are: acebutolol, alprenolol, atenolol, betaxolol, bisoprolol, bopindolol, bupranolol, carvedilol, celiprolol, labetalol, levobunolol, mepindolol, metipranolol, metoprolol, nadolol, oxprenolol, penbutolol, pindolol, propranolol, sotalol.

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Examples of bronchospasmolytics / antiasthmatics are: bambuterol, carbuterol, clenbuterol, epinephrine, fenoterol, hexoprenaline, ipratropium bromide, isoetarin, orciprenaline, oxitropium bromide, pirbuterol, procaterol, reproterol, salbutamol, salmeterol, terbutaline, theopohylline, tolubuterol.
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Examples of calcium antagonists are: amlodipine, felodipine, isradipine, nicardipine, nifedipine, nilvadipine, nitrendipine, nisoldipine, verapamil.

Examples of cholagogues are: anethole trithion, azintamide, chenodeoxycholic acid, dehydrocholic acid, hymecromone, piprozoline, ursodeoxycholic acid.

Examples of cholinergics / cholinolytics are: aceclidine, acetylcholine, carbachol, cyclopentolate, distigmine, edrophonium, emepronium, homatropine, methantheline, neostigmine, pilocarpine, propantheline, propiverine, pyridostigmine, tropicamide.
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Examples of diuretics are: acetazolamide, amiloride, bendroflumethiazide, bumetanide, chlorothiazide, chlorthalidone, clopamide, etacrynic acid, furosemide, hydrochlorothiazide, triamterene, xipamide.

Examples of blood circulation stimulants / nootropics are: buflomedil, buphenine, dextran 40, dihydroergotoxin, lloprost, meclofenoxate, nicergoline, nicotinic acid, pentifylline, piracetam, piribedil, pyritinol, tolazoline, viquidil.

Examples of enzymes/inhibitors/transport proteins are: antithrombin III, aprotinin, carnitine, clavulanic acid, dornase alfa, sulbactan.

Examples of expectorants are: acetylcysteine, ambroxol, bromhexine, carbocisteine, colfosceril, surfactant (from beef liver), surfactant (from pig lung).

Examples of gout medications are: allopurinol, benzbromarone, colchicine, probenecid, sulfinpyrazone.

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AT 0209 GbM

14.10.2002

Examples of glucocorticoids are: betamethasone, budesonide, cloprednol, cortisone, dexamethasone, flunisolide, fluticasone, hydrocortisone, methylprednisolone, paramethasone, prednisolone, prednisone, prednylidene, triamcinolone.

Examples of hemostatics are: Adrealon, blood coagulation factor VII, blood coagulation factor VIII, blood coagulation factor IX, blood coagulation factor XIII, carbazochrome, etamsylate, fibrinogen, collagen, menadiol, menadione, protamine, somatostain, thrombin, thromboplastin.

Examples of pituitary/hypothalamic hormones and inhibitors are: argipressin, chorionic gonadotrophin, desmopressin, felypressin, gonadorelin, lypressin, menotropin, ornipressin, quinagolide, terlipressin, thyrotrophin.

Examples of immunotherapeutics and cytokines are: aldesleukin, azathioprine, BCG, ciclosporin, filgrastim, interferon alfa, interferon beta, interleukin-2, muromonab-CD3, tacrolism, thymopentin, thymostimulin.

Examples of cardiac drugs are: Acetyldigitoxin, acetyldiagoxin, convallatoxin, digitoxin, digoxin, gitoformate, lanatoside, meproscillarin, metildigoxin, pengitoxin, peruvosid, proscillahdin, strophanthin, thevetin, amrinone, enoximone, milrinone,

Examples of coronary agents are: carbocromen, isosorbide dinitrate, nitroglycerin, pentaerythrityl tetranitrate.

Examples of laxatives are: Bisacodyl, Dantron, Docusate, Glycerol, Lactulose, Magnesium sulfate, Sodium picosulfate, Sodium sulfate, Paraffinum subliqiudum,
Phenolphthalein, castor oil, sorbitol.

Examples of liver therapeutics are: choline, citiolon, myo-inositol, silymarin.

Examples of lipid-lowering agents are: acipimox, bezafibrate, clofibrate, etofibrate, fluvastin, lovastatin, pravastatin, simvastatin.

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AT 0209 GbM '\ \.5 . *38* . ^: . S i'. ^! October 14, 2002

Examples of local anesthetics are: articaine, benzocaine, bupivacaine, butanilicaine, chloroethane, cinchocaine, cocaine, etidocaine, fomocaine, lidocaine, mepivacaine, myrtecaine, oxetacaine, oxybuprocaine, polidocanol, prilocaine, procaine, proxymetacaine, quinisocaine, tetracaine.
5

Examples of gastrointestinal agents are: bismuth subcitrate, bromopride, garbenoxolone, cimetidine, domperidone, famotidine, metoclopramide, nizatidine, omeprazole, proglumide, ranitidine, roxatidine, sucralfate, sulfasalazine.

Examples of migraine medications are: ergotamine, lisuride, naratriptan, pizotifen, sumatriptan, zolmitriptan.

Examples of muscle relaxants are: Alcuronium, Atracurium, Baclofen, Carisoprodol, Chlormezanone, Clostridium toxin botulinum toxin A,
15

Examples of parathyroid therapeutics/calcium metabolism regulators are: clodronic acid, dihydrotachysterol, parathyroid glands, pamidronic acid.

Examples of neuroleptics are: benperidol, chlorpromazine, droperidol, fluoxetine, haloperidol, melperone, promethazine, zuclopenthixol.

Examples of Parkinson's drugs are: amantadine, benserazide, benzatropine, biperiden, bornaprine, bromocriptine, cabergoline, carbidopa, diphydroergocriptine, levodopa, metixen, pergolide, pramipexole, ropinirole, tolcapone.
25

Examples of psychostimulants are: amfetaminil, deanol, fencamfamine, fenetylline, kavain, methylphenidate, pemoline, prolintan.

Examples of thyroid therapeutics are: carbimazole, glandulae thyreoideae, iodine, iodide, levothyroxine, liothyronine, methylthiouracil, perchlorate, prolonium iodide, propylthiouracil, radioiodine, thiamazole.

AT 0209 GbM "; ^: ··| · "ji9*,. ^: . j \\· ¹ 10/14/2002

Examples of sedatives/hypnotics are: amobarbital, chloral hydrate, clomethiazole, glutethimide, hexobarbital, methaqualone, methyprylone, pentobarbital, scopolamine, secbutabarbital, secobarbital, vinylbital, zolpidem, zopiclone.

Examples of sex hormones are: chlorotrianisene, clomiphene, clostebol, cyproterone, drostanolone, epimestrol, estradiol, estriol, estrone, ethinylestradiol, flutamide, fosfestrol, conjugated estrogens, medroxyprogesterone, mesterolone, mestranol, metenolone, methyltestosterone, nandrolone, oxymetholone, polyestradiophosphate, quinestrol, stanozolol, testosterone.
10

Examples of spasmolytics are: atropine, butylscopolamine, flavoxate, glycopyrronium, mebeverine, methylscopolamine, oxybutynin, tiropramide, trospium.

Examples of platelet aggregation inhibitors are: abciximab, acetylsalicylic acid, dipyridamole, ticlopidine.

Examples of transquilizers are: alprazolam, bromazepam, brotizolam, buspirone, camazepam, chlordiazepoxide, clobazam, clonazepam, clorazepate, clothiazepam, diazepam, flunitrazepam, flurazepam, hydroxyzine, ketazolam, loprazolam, lorazepam, lormetazepam, medazepam, meprobamate, metaclazepam, midazolam, nitrazepam, oxazepam, oxazolam, prazepam, temazepam, tetrazepam, thazolam.

Examples of urological drugs are: finasteride.
25

Examples of Varia are: dapiprazole, diethyltoluamide, lipoic acid.

Examples of vein medications are: aescin, calcium dobesilate, coumarin, diosmin, rutoside, troxerutin.
30

Examples of antivirals are: aciclovir, cidofovir, didanosine, famciclovir, foscarnet, ganciclovir, lamivudine, ritonavir, zalcitabine, zidovudine.

BEI 0209 GbM : *..: . 20 .* . : : .* 14.10.2002

Examples of vitamins are: alfacalcidol, allithiamine, ascorbic acid, biotin, calcifediol, calcitriol, cholecalciferol, cyanocobalamin, ergocalciferol, folic acid, hydroxocobalamin, nicotinamide, pantothenic acid, phytomenadione, pyridoxine, retinol, riboflavin, thiamine, tocopherol, transcalcifediol.
5

Examples of cytostatics are: aclarubicin, altretamine, aminoglutethimide, amsacrine, asparaginase, bleomycin, buserelin, busulfan, carboplatin, carmustine, chlorambucil, cladribine, cisplatin, cyclophosphamide, cytarabine, dacarbazine, daunorubicin, diethylstilbestrol, docetaxel, doxorubicin, epirubicin, etoposide, fludarabine, fluorouracil, gemcitabine, goserelin, hydroxycarbamide, idarubicin, ifosfamide, lomustine, melphalan, mercaptopurine, mesna, methotrexate, miltefosine, mitomycin,
Mitoxantrone, Panorex, Paclitaxel, Plicamycin, Tamoxifen, Tegafur, Thiotepa, Tioguanine, Topotecan, Triptorelin, Vinblastine, Vincristine, Vindesine, Zorubicin.

According to the invention, the active ingredients mentioned can be in the form of a powder, a paste, a film, as a solution or as a melt and can be applied to the volume-increasing material, preferably using the adhesion promoters described above. The active ingredients described can also be incorporated into the volume-increasing material. In some circumstances, a delayed release of the active ingredient can also be achieved here.

The attractants, active substances and auxiliary substances described can in principle be applied to the surface of the volume-increasing material or incorporated into it in any combination, depending on the end product desired in each case. In the simplest case, the agents according to the invention can therefore be designed in the form of a volume-increasing material into which only attractants are introduced or onto which only attractants are applied. Active substances can also be applied or incorporated for medical purposes. The active substances described in more detail above are preferably used for this. Instead of the active substances or in addition to them, other auxiliary substances can also be present. These are in particular the auxiliary substances described above. They can also be any nutrients, e.g. vitamins or trace elements.

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Claims (9)

1. Agent for producing a satiety effect and for weight reduction in animals, containing a volume-increasing material which is insoluble or poorly soluble in gastrointestinal fluids and/or body fluids and at least one attractant which is effective for the respective animal species. 2. Agent according to claim 1, characterized in that the attractant is at least partially bound to the surface of the volume-increasing material. 3. Agent according to one of claims 1 or 2, characterized in that the attractant is bound to the surface of the volume-increasing material by means of an adhesion promoter which is at least partially soluble in the stomach. 4. Agent according to one of claims 1 to 3, characterized in that the attractant is incorporated into the volume-increasing material. 5. Agent according to one of claims 1 to 4, characterized in that it contains natural or nature-identical flavorings or mixtures thereof as attractants. 6. Agent according to one of claims 1 to 5, characterized in that it is in the form of powders, granules, tablets, capsules, dragees, adsorbates or beatlets. 7. Agent according to one of claims 1 to 6, characterized in that the volume-increasing material contains natural, semi-synthetic or synthetic polymers. 8. Agent according to one of claims 1 to 7, characterized in that the volume-increasing material contains polysaccharides. 9. Agent according to one of claims 1 to 8, characterized in that the volume-increasing material contains compressed sponge-like substances.