WO2004056209A1 - Ginseng-containing agent for producing a sensation of satiety and for weight reduction - Google Patents

Abstract

The invention relates to an agent for producing a sensation of satiety and for weight reduction, which contains at least one active substance contained in ginseng and a volume-increasing material that is insoluble or hardly soluble in gastro-intestinal liquids and/or body fluids. The invention also relates to a method for producing the agent and the use thereof.

Description

GINSEN AGENT FOR PRODUCING A SATURATION EFFECT AND FOR WEIGHT REDUCTION

The present invention relates to a means for producing a satiety effect and for reducing weight, which is particularly suitable for use in diet programs.

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. B. so-called appetite suppressants, which try to suggest to the body an aversion to food in a biochemical way. Some of these remedies have considerable harmful side effects.

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.

From DE 4025912 a means for oral ingestion 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.

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, the production of these preparations requires additional process steps to introduce stable cross-links. 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.

The object of the present invention is to provide an improved agent for oral administration which has a longer stomach 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 while regulating cholesterol levels, 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. Furthermore, the agent should be well tolerated and, in addition to the "passive" function of the satiety effect, should also actively support weight loss and should not, as far as possible, reduce the well-being of the people taking the agent.

In addition, the agent should provide immune stimulation and strengthening during the weight loss phase.

This object is achieved according to the invention by a means for producing a saturation effect and for weight reduction containing at least one active ingredient contained in ginseng and a volume-increasing material which is insoluble or poorly soluble in gastrointestinal fluids and / or body fluids.

Active substance in the sense of the invention means all substances with a pharmaceutical or biological effect. Ginseng is a perennial, anemone-like Araliacee (Panax ginseng), which grows wild in the mountain forests of East Asia and is also cultivated, the root of which contains steroid derivatives. The ingredients isolated so far include sitosterol and more than 10 triterpene glycosides ginsenosides. The ginsenoids are a group of glycosides of tetracyclic triterpenes (sapogenins) from the ginseng root (Panax ginseng): 24-Dammaren-3,12,20-triol, the (3a, 12b, 20S) form is called Betulafolienttriol and the diastereomers (3b, 12b, 20S) -form protopanaxadiol. Protopanaxatriol has an additional 6a-hydroxy group. The sugar components in these glycosides are D-glucopyranose, L-arabinopyranose, L-arabinofuranose, D-xylofuranose and D-xylopyranose as well as L-rhamnopyranose. The ginsenosides are said to have anti-ischemic, immunostimulating, antithrombotic (PAF-antagonist), hypoglycemic and cholesterol-lowering properties. According to new studies, the ginseng extract generally stimulates protein and nucleic acid metabolism. Furthermore, one found, among other things, an essential oil responsible for the ginseng smell, in which a number of sesquiterpenes were characterized. Ginseng is mainly used as Roborans and Geriatricum (Source: Römpp Lexikon Chemie - CD Version 2.0, Stuttgart / New York: Georg Thieme Verlag 1999).

The combination of the at least one active ingredient contained in the ginseng and the volume-increasing material thus improves not only the satiety effect but also the well-being and the weight loss is positively influenced.

In short, ginseng is known for its health-promoting use as a universal agent. Ginseng acts as a stimulating and stimulating cardiovascular agent, as an antidepressant and as Nervennahrung. In addition, ginseng has a strong immunostimulatory effect, promotes body protein build-up, improves memory and concentration, as well as mental and physical resilience. In addition, ginseng has a positive influence on adult diabetes, stimulates the metabolism, regulates blood fat levels and lowers blood pressure.

Ginseng increases the adaptability and tolerance of the body to stress and protects against the negative effects of permanent stress. In addition, ginseng increases physical performance and generally promotes the building processes and provides the body with more energy; one speaks of an anabolic effect. Ginseng also increases concentration and alertness, improves thinking and memory and works against fatigue and exhaustion. Furthermore, ginseng has a stimulating or calming effect on the central nervous system, as required. Ginseng is able to lower an elevated blood sugar level and to raise an excessively low blood sugar level. Ginseng is also known to stimulate the immune system through several mechanisms. Ginseng is also able to activate important enzymes in cell metabolism and the liver. This leads to an increased synthesis of DNA, RNA and important proteins. In particular, the amount of reduced glutathione is increased, which plays an important role in cell metabolism, especially in the liver. In addition, the active ingredients contained in ginseng have an antioxidative effect, ie they especially prevent free radicals, which otherwise damage cells. Ginseng is used to support the therapy of cardiovascular diseases, in which it liquefies the blood, controls blood pressure, lowers cholesterol and lowers the heart's oxygen demand and strengthens the heart muscle. Ginseng is also able to influence the blood count through the active ingredients it contains, in particular Bone marrow cell stimulation known for division and blood formation. Ginseng is also known to improve respiratory functions and reduce inflammation through its use. In addition, ginseng is said to have a sexual stimulating effect.

In particular, the influence of active ingredients contained in ginseng on the immune system has been investigated. It has been demonstrated that the intake of a standardized ginseng extract increases the immune response against a flu vaccination, the acidic poiysaccharides of the root promote the production of interleukin 8, the ginseng poiysaccharides induce the production of interferon, the phagocytosis of the reticuloendothelial system, the production of antibodies and promote an increase in the continent in the blood, as well as increases the cellular immune response (Scaglione et al, Drugs Expl. Clin. Res. 23 82), 1996: 65-72; Sonoda et al, Immunopharmacology 1998; Smolina et al, Antibiotic Khimioter 1998; Chang-Xiao et al, Ethnopharmacology 1992; Jie et al, Argenst Actions 15 (3-4), 1984: 386-91; Kim et al, Immunopharmacology and Immunotoxicology 12 (2), 1990: 257-76).

According to the invention, all substances contained in ginseng are suitable as active substances contained in ginseng. In particular, the above-mentioned steroid derivatives, sitosterol, ginsenoids and essential oils are included. It also includes active ingredients contained in ginseng that have not yet been isolated and / or characterized. These active ingredients can be obtained from the ginseng itself or can be produced artificially. The invention also includes the use of liquid, pasty, solid, granular and powdery preparations, extracts and partial extracts, solutions and melts of ginseng, synthetically produced ingredients of ginseng and / or mixtures thereof. Natural ginseng is preferably used. Especially preferably from Asia, especially Korea, because the ginseng from there is considered the most effective.

The at least one active ingredient contained in the ginseng can be applied in, on or on the agent.

In a variant of the invention, the active ingredients contained in the ginseng can be applied to the surface or to a part of the surface of the volume-increasing material. Suitable adhesion promoters can be used for this.

Volume-increasing material is understood to mean a material which increases its volume under appropriate conditions (see below), i. H. its extent changed, as z. B. is possible by swelling, foaming or decompression.

Solid, semi-solid or liquid substances can be considered as adhesion promoters. These can be powders, pastes, solutions, melts or foils. In the latter case, for example, a film-shaped adhesion promoter layer can have adhesive properties on both sides and in this way ensure the cohesion of the carrier material with the layer containing the active substance.

By applying the active ingredient-containing formulation and / or the carrier material with this connecting layer, a connection is established between the carrier material, which may be compressed and increases the volume in the gastrointestinal tract, and the active ingredient-containing layer. The duration of the existing connection depends on the solubility of the substances used and contained in the connecting layer in the 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, the invention also relates to an agent containing thread-like and / or fabric-like substances as a connecting agent.

As adhesion promoters, preference is given to compounds which contain natural, synthetic and semisynthetic polymers. In principle, nonionic and ionic polymers come into consideration. In principle, all hot-melt adhesives and contact adhesives known from the prior art can be used, provided they are suitable for pharmaceuticals or food. In a special embodiment of the present invention, the adhesion promoter is starch derivatives, cellulose derivatives, gelatin or poiysaccharides, preferably polyuronic acid-containing poiysaccharides, e.g. B. Polyalginates. Hypomellose, Carmellose, Metholose may be mentioned as examples.

Particularly preferred polyuronic acid-containing polyaccharides are 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.

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, the average molecular weight being able to vary in a range from 30-200 kDa. The polysaccharide alginic acid is a component 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 in 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 L, et al. (Biomaterials, 1997, 18: 583-90). However, 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. In general, all physiologically acceptable poly cations, especially divalent cations, can be used.

In addition to the active ingredients contained in the ginseng, the adhesive agent described can also be used to apply further active ingredient-containing formulations to the volume-increasing material.

According to the invention it is therefore z. B. possible in a drug to treat the cause of obesity and at the same time symptomatic the respective symptom. For example, an antihypertensive active ingredient can be firmly applied to the carrier material, which reduces the food intake and thus the weight by creating a feeling of satiety. Since weight reduction is also able to lower high blood pressure, the combination preparation described leads to an improvement in the effectiveness and therapy compared to the individual dose. The active ingredients contained in the ginseng and / or the further active ingredients can be applied to the described volume-increasing material, preferably using the adhesion promoters described. Likewise, the active ingredients contained in ginseng and / or possibly the other active ingredients can be applied directly if they are e.g. B. have adhesion-promoting substances or develop adhesion-promoting properties under pressure at temperatures. Furthermore, it is possible for the active ingredients contained in the ginseng and / or possibly the further active ingredients in the volume-increasing material z. B. already in the manufacture or manufacture of the carrier.

The active ingredients contained in ginseng and / or the further active ingredients can also be applied in one or more layers to the carrier material and z. B. be covered by a top protective layer (paint). This lacquer should then dissolve under the appropriate conditions and allow the release of the active ingredients.

After the agent has been taken in the stomach, the agent according to the invention using the adhesion promoters described is split up into volume-enlarged material and the layer (s) containing the active ingredient-containing formulation (s). The active substance-containing formulation (s) can therefore enter the intestine, i.e. H. because of this, be absorbed in the intestine.

The material which increases the volume according to the invention ensures the increase in volume of the release system required to develop the saturation effect. Because of this, the material is larger than the opening of the stomach outlet and is therefore prevented from being transported quickly from the stomach into the intestine, ie the dwell time in the The stomach for the carrier material is longer than for the active substance-containing layer. As a result of the residence time of the carrier material in the stomach, a feeling of satiety is created and is maintained for the time it remains in the stomach.

According to the invention, however, it is also possible to combine different active ingredients. In addition to the adhesive that is soluble in the stomach and described, an adhesive that does not dissolve in the stomach can be used. Active ingredients are then applied to this coupling agent, which are to remain in the stomach and develop their effect there.

Furthermore, according to the invention it is possible to glue together several volume-increasing pieces of material of the same or different composition. When using the adhesive that is soluble in the stomach, these pieces of material become detached from one another. As a result, an increased saturation effect can be achieved. In such a system, the active substances can be arranged between several pieces of material by means of the adhesion promoter. When the individual pieces of material in the stomach fall apart, the layers of active substance detach and enter the intestine to develop their effect there. If necessary, active substances can also be used which at least partially dissolve in the stomach and, where appropriate, develop their therapeutic effect there.

According to the invention, in a variant of the invention, sponge-like materials can also be contained in the volume-increasing material, which z. B. after previous compression in the stomach or swell, for example, under the influence of the liquid present in the stomach. 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, semi-synthetic or synthetically produced sponge-like structures can be used. Examples of synthetic sponge-like materials are polyurethanes, polyacrylates, poly (meth) acrylic acid derivatives, homo- and copolymers of vinyl acetate. The natural and semisynthetic polymers include cellulose, cellulose ethers or cellulose esters such as cellulose acetate and cellulose acetate phthalate. Examples of natural polymers are polyaccharides such as alginates, tragacanth, xanthan gum, guar gum and their salts and derivatives. The use of chitin and chitin derivatives is possible. In addition, fabrics with a fiber structure such as ski proteins are preferred. B. collagen, keratin, conchagens, fibroin, elastin and chitin are used. In addition, the present invention also relates to stably crosslinked polyaccharides.

The sponge-like or -shaped structures are produced using methods known per se according to the prior art. Reference is made here to WO98 / EP96 / 03950, which is also the subject of the present invention. Depending on the starting material used, a foam can be obtained in the simplest case by blowing in, by beating, shaking, spraying or stirring in the gas atmosphere in question. In the case of polymers, the foam structure arises due to chemical reactions. So z. B. foamed by adding blowing agents that decompose at a certain temperature during processing with gas formation, or by adding liquid solvents during the polymerization. Foaming takes place either when leaving the extrusion die, ie in Connection to extrusion or injection molding or in open molds. Hardening takes place under the conditions which are 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 or can increase its volume. Finally, when selecting the carrier material, it is essential that it remains swellable without the cell webs being destroyed. The compressed material retains its sponge structure even when compressed.

Under physiological conditions, the compressed material can, for example, expand two to ten times, preferably four to eight times its volume. The active substance 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 prior art are 0.5 to 1.5 cm ² .

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

The volume-increasing materials can also consist of dried porous gel or foam. Anionic polymers are preferably used as materials.

Anionic polymers preferred according to the invention are poiysaccharides and here polyuronic acid-containing poiysaccharides, 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. The use of synthetic or semi-synthetic is also conceivable Cellulose derivatives, such as. B. 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 poiysaccharides, and in particular mixtures containing salts of alginic acid and pectin, are advantageous according to the invention.

With regard to the anionic polymers, the use of low ester pectins is also advantageous according to the invention. 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 peel, fruit pulp or sugar beet pulp. The resulting pectins (apple pectin, citrus pectin) are therefore purely vegetable and are highly biocompatible. They can form gels under water.

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

The agent according to the invention can be present, for example, in the form of tablets, capsules, dragees, as granules or suppositories or other configurations. In addition, the agent according to the invention can have a coating as an outer layer. This can be a varnish 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.

The volume-increasing material according to the invention can also be in the form of powder in addition to the sponge form. According to the invention, this includes both finely divided powders, granules, adsorbates and beadlets.

The powdery volume-increasing materials can be produced in various ways. For example, for the 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 further components can be added. The carrier substances are preferably the volume-increasing materials according to the invention. According to the invention, batch or continuous mixers can be used. The carrier material or volume-increasing material may be presented together with additives. Classic examples are flight share mixers, cone screw mixers or similar devices. Alternatively, the product can be mixed by moving the entire container. Examples include tumble mixers, drum mixers, etc. Another option is to use pneumatic mixers. The use of screws for mixing and / or reduction is also conceivable.

The dosage or addition of active ingredients contained in ginseng or other active ingredients may be carried out together with additives, e.g. B. on devices for dripping or spraying. Examples of this are lances, shower heads, single-substance or multi-substance nozzles, in rare cases rotating dripping or atomizing devices. In the simplest case, addition is also possible locally as a concentrated jet. Alternatively, the active ingredient contained in the ginseng and / or the further active ingredient can first be introduced into the mixer in order to then give up the volume-increasing material.

Furthermore, it is possible to soak the volume-increasing material in a liquid active ingredient containing ginseng or ginseng extract etc.

The active ingredient contained in the ginseng and / or the further active ingredient can be added under positive pressure, normal pressure or under negative pressure, counter atmosphere, preferably under normal pressure or negative pressure. In order to increase the loading of the volume-increasing material and to minimize the effects of oxygen, it may be expedient to evacuate the mixer containing the volume-increasing material before adding the active ingredient and / or further active ingredient contained in ginseng and, if necessary, to cover it with protective gas.

According to the invention, powdery agents can also be produced by the spray formulation process. Here, for example, in an initial step, an aqueous solution of a protective colloid, e.g. B. gelatin and / or gelatin derivatives, and / or gelatin substitutes with the addition of the volume-increasing materials described above and by adding the active ingredients contained in the ginseng and / or other active ingredients with stirring, a dispersion is first produced, the aqueous solution of the colloid representing the homogeneous phase of the dispersion , Devices in which such spray formulations can be produced are described, for example, in EP 0074050 B1.

The production of granules can be achieved in that the volume-increasing substances and / or spray-dried powders as well as active substances and optionally

Active components and binders as well as aggregates compact

Granules are generated. As a mixer, for example

Bucket mixers or flight share mixers can be used. The liquid components can be added in various ways, e.g. B. dripped or sprayed on so that a pasty, sticky mass is formed. The paste-like mass is broken up by suitable selection of the speed of the mixing tools and / or high-speed knives and compact granules are formed. Very large chunks can be cut up using mixing tools and knives and, on the other hand, fine powders can be agglomerated.

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. Pectin-containing gels or foams are produced in an analogous manner, as are gels or foams containing mixtures of anionic polymers. In addition to the addition of inorganic or organic calcium salts, such as. As calcium chloride or calcium gluconate, the use of magnesium salts and mixtures of various physiologically acceptable divalent cations is also conceivable.

According to the invention, the addition of salts of physiologically acceptable trivalent cations, e.g. B. from soluble aluminum salts. 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. B. calcium or magnesium salts or a combination thereof can be used in the preparation of the agents according to the invention.

The coating layers, which may contain the active ingredients contained in the ginseng and, if appropriate, the further active ingredients, can be added after the powder or granules have been produced in mixers at a lower speed of the mixing tools and stationary knives or in a type-related downstream mixer. The agents according to the invention can be shaped by pressing the pasty, sticky phases during the granulation process through the die of an extruder. The volume-increasing material according to the invention and the active ingredients contained in the ginseng and optionally the further active ingredients can contain further auxiliary substances.

These include, for example, the following substances, which, however, are not limiting for the present invention: Water-insoluble auxiliaries or mixtures thereof, such as lipids, and the like. a. Fatty alcohols, e.g. B. cetyl alcohol, stearyl alcohol and cetostearyl alcohol; Glycerides, e.g. B. 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. B. paraffin or earth wax; Fatty acids, e.g. B. stearic acid; certain cellulose derivatives, e.g. B. ethyl cellulose or acetyl cellulose; Polymers or copolymers, such as polyalkylenes, e.g. As polyethylene, polyvinyl compounds, e.g. B. polyvinyl chloride or polyvinyl acetate, and vinyl chloride-vinyl acetate copolymers and copolymers with crotonic acid, or polymers and copolymers of acrylates and methacrylates, for. B. copolymers of acrylic acid ester and methacrylic acid methyl ester can be used.

In addition to the auxiliaries mentioned, the agents according to the present invention can additionally contain fillers, disintegrants, binders and lubricants, and carriers which have no decisive influence on the release of active ingredient. Examples include concrete (aluminum oxide-silicon oxide hydrate), silica, cellulose (usually microcrystalline cellulose) or cellulose derivatives, e.g. B. methyl cellulose, sodium carboxymethyl cellulose, sugars such as lactose, starches, for example corn starch or derivatives thereof, for example sodium carboxymethyl starch, starch starch, phosphoric acid salts, for. B. di- or tricalcium phosphate, gelatin, stearic acid or suitable salts thereof, e.g. As magnesium stearate or calcium stearate, talc, colloidal silicon oxide and similar auxiliaries. Examples of active substance-containing formulations according to the invention from different therapeutic classes are given below, which, however, are not limiting for the present invention.

Examples of ACE inhibitors are: benazepril, captopril, cilazapril, enalapril, fosinopril, lisinopril, perinodopril, quinapril, ramipril, trandolopril.

Examples of analeptics are: almitrine, amiphenazole, caffeine, doxapram, etamivan, fominoben, metamfetamine, nicethamide, pentetrazole.

Examples of analgesics (opioids) are: alfentanil, buprenorphine, cetobemidone, dextromoramide, dextropropoxyphene, fentanyl, flupirtine, hydromorphone, levomethadone, levorphanol, meptazinol, morphine, nalbuphin, oxycodone, pentazocinramid, pethidine.

Examples of analgesics (non-opioids) are: acetylsalicylic acid, benzyl almondate, bucetin, ethenzamide, ketorolac, metamizole, morazone, 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, chlorophenamine, clemastine, cyslizine, cyproheptadine, dimenhydramine, doxylamine, fexofenadine, ketotifen midomolininoxinamin, oximinomolininoxin, oximinomolininoxin, oxaminolominaminolamin, oximinomolamin, oxinate, morphine, loramin, oximinomolamin, oxinate, morphine, oxinate , Pheniramine, phenyltoloxamine, spaglumic acid, terfenadine, triprolidine. Examples of antiarrhythmic drugs are: ajmaline, amiodarone, aprindine, quinidine, disopyramide, mexiletine, procainamide, propafenone, tocainide.

Examples of antibiotics / chemotherapeutics are: Amikacin, Gentamicin, Kanamycin,

Paromomycin, Sisomicin, Streptomycin Tobramycin, Chloroquine, Halofantrine, Hydroxychloroquine, Mefloquine, Proguanil, Ethambutol, Isoniazid, Rifabutin, Rifampicin, Cefacetril, Cefaclor, Cefadroxil, Cefalexin, Cefalotefimimine, Cefalotefimimine, Cefalotoliminocef , Cefoxitin, cefpodoxime (proxetil), cefradin, cefsulodin, ceftazidime, ceftizoxime, ceftriaxon, cefuroxime (axetil), latamoxef, cinoxacin, ciprofloxacin, enoxacin, nalidixic acid, norfloxacinoxinocinoxinocinoxinocinoxinomycinocytoxinomycinocytoxinomycinoxinoxinoxinoxinoxinoxinoxinoxinoxinoxinoxinoxinoxinoxinoxinoxinoxinoxinoxinoxinoxinoxinox, , apalcillin, azidocillin, Aziocillin, bacampicillin, benzylpenicillin, carbenicillin, Carindacillin, dicloxacillin, flucloxacillin, Mezlociliin, oxacillin, Phenoxymethypenicillin, piperacillin, pivampicillin, propicillin, ticarcillin, colistin, teicoplanin, vancomycin, cotrimoxazole, Sulfametoxydiazin, doxycycline, oxytetracycline, tetracycline, atovaquone , Chloramphenicol, fosfomycin, imipenem, metron idalzol, nitrofurantoin, pentamidine, taurolidine, trimethoprim.

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

Examples of antidiabetics / antihypoglycaemics are: acarbose, carbutamide, chlorpropamide, glibenclamide, glibornuride, gliclazide, glimepiride, glipizide, gliquidon, glisoxepid, glymidine, guar, insulin, metformin, tolazamide, tolbutamide. Examples of antidiarrheals are: difenoxine, diphenoxylate, loperamide, petin, tannin.

Examples of antidotes are: flumazenil, naioxon, naltrexone.

Examples of antiemetics are: alizapride, betahistine, thiethylperazine.

Examples of antiepileptics are: barbexaclone, carbamazepine, ethosuximide, lamotrigine, mepacrine, mesuximide, phenobarbital, phenytoin, primidone, sultiam, trimethadione, valproic acid, vigabatrin.

Examples of antifibrinolytics are: aminocaproic acid, 4- (aminomethyl) benzoic acid, tranexamic acid.

Examples of antihypertensives are: clonidine, diazoxide, doxazosin, guanethidine, hydralazine, methyldopa, moxonidine, nitroprusside sodium, phentolamine, prazosin, reserpine, tiamenidine, urapidil.

Examples of antihypotonic agents are: dihydroergotamine, dobutamine, dopamine, etilefrin, norepinephrine, norfennefrin.

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, fenticonalzol, fluconazole, griseofulvin, isoconazole, itraconazole, tioconazole, oxifazonazole, miconazonazole, miconazonazole, tolnaftate. Examples of anti-rheumatic drugs are: acemetacin, azapropazon, benorilat, bumadizon, carprofen, choline salicylate, diclofenac, diflunisal, etofenamate, felbinac, fenbufen, fenoprofen, flufenamic acid, flurbiprofen, ibuprofen, indomofamobamone, moxinoxamonamone, melonacidamonamone, melonacidamonamone, melonacidamonamone, melonacidamonamone, melonacidamone, , naproxen, nifenazone, niflumic, oxyphenbutazone, phenylbutazone, piroxicam, pirprofen, proglumetacin, Pyrazinobutazon, salsalate, sulindac, suxibuzone, tenoxicam, tiaprofenic acid, tolmetin, auranofin, aurothioglucose, aurothiomalate, Aurothiopiypeptid, chloroquine, hydroxychloroquine, penicillamine, Ademetionin, 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: amfepramon, fenfluramine, fenproporex, levopropylhexedrine, mazindol, mefenorex, metamfepramon, norephedrine, norpseudoephedrine.

Examples of beta-adrenergic blockers are: Acebutolol, Alprenolol, Atenolol, Betaxolol, Bisoprolol, Bopindolol, Bupranolol, Carvedilol, Celiprolol, Labetalol, Levobunolol, Mepindolol, Metipranolol, Metoprolol, Nadolol, Oxprenolol, Poleololol, Oxprenolol, Poleolol.

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.

Examples of calcium antagonists are: amlodipine, felodipine, isradipine, nicardipine, nifedipine, nilvadipine, nitrendipine, nisoldipine, verapamil.

Examples of cholagoga are: anethole trithione, azintamide, chenodeoxycholic acid, dehydrocholic acid, hymecromone, piprozoline, ursodeoxycholic acid.

Examples of cholinergics / cholinolytics are: aceclidine, acetylocholine,

Carbachol, cyclopentolate, distigmine, edrophonium, emepronium,

Homatropin, methantheline, neostigmine, pilocarpine, propantheline, propiverine, pyridostigmine, tropicamide.

Examples of diuretics are: acetazolamide, amiloride, bendroflumethiazide,

Bumetanide, chlorothiazide, chlorotalidone, clopamide, etacrynic acid, furosemide, hydrochlorothiazide, triamterene, xipamide.

Examples of blood circulation-promoting agents / nootropics are: buflomedil, buphenin, 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, carbocistein, colfosceril, surfactant (from beef liver), surfactant (from pork lungs). Examples of gout agents are: allopurinol, benzbromaron, colchicine, sample oath, sulfinpyrazone.

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

Examples of hemostyptics are: Adreaion, 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, Omipressin, Quinagolid, 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 Kardiaka are: Acetyldigitoxin, Acetylödiagoxin, Convallatoxin, Digitoxin, Digoxin, Gitoformat, Lanatosid, Meproscillarin, Metildigoxin, Pengitoxin, Peruvosid, Proscillaridin, Strophanthin, Thevetin, Amrinon, Enoximon, Milrinon

Examples of coronary agents are: carbocromes, isosorbide dinitrate, nitroglycerin, pentaerythrityl tetranitrate. Examples of Laxantia are: bisacodyl, Dantron, docusate, glycerol, lactulose, magnesium sulfate, sodium picosulfate, sodium sulfate, paraffinum subliqiudum,

Phenolphthalein, castor oil, sorbitol.

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

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

Examples of local anesthetics are: Articaine, Benzocaine, Bupivacaine, Butanilicain, Chloroethane, Cinchocaine, Cocaine, Etidocaine, Fomocaine, Lidocaine, Mepivacaine, Myrtecain, Oxetacaine, Oxybuprocaine, Polidocanol, Prilocaine, Procaine, Proxymainocaine, Quaincaine.

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

Examples of migraine drugs are: Ergotamine, Lisurid, Naratriptan, Pizotifen, Sumatriptan, Zolmitriptan.

Examples of muscle relaxants are: Alcuronium, atracurium, baclofen, carisoprodol, chlormezanon, clostridium toxin botulinum toxin A, examples of parathyroid therapeutic agents / calcium metabolism regulators are: clodronic acid, dihydrotachysterol, glandulae parathyroidoid, pamidronate. Examples of neuroleptics are: Benperidol, Chlorpromazin, Droperidol, Flugeanzin, Haloperidol, Melperon, Promethazin, Zuclopenthixol.

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

Examples of psychostimulants are: Amfetaminil, Deanol, Fencamfamin, Fenetyliin, Kavain, Methylphenidat, Pemolin, Prolintan.

Examples of thyroid therapeutics are: carbimazole, thyroid gland, iodine, iodide, levothyroxine, liothyronine, methylthiouracil, ^■ perchlorate, prolonium iodide, propylthiouracil, radio iodine, thiamazole.

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

Examples of sex hormones are: chlorotrianisen, clomiphene, clostebol, cyproterone, drostanolone, epimestrol, estradiol, estriol, estrone, ethinylestradiol, flutamide, fosfestrol, conjugated estrogens, medroxyprogesterone, mesterolone, mestranol, oxestronolone, methylolonolone, methylstrol Stanozolol, testosterone.

Examples of antispasmodics are: atropine, butylscopolamine, flavoxate, glycopyrronium, mebeverine, methyiscopolamine, oxybutynin, tiropramide, Trospiun. Examples of platelet aggregation inhibitors are: abciximab, acetylsalicylic acid, dipyridamole, ticlopidine.

Examples of transquilizers are: Alprazolam, Bromazepam, Brotizolam, Buspiron, Camazepam, Chlordiazepoxid, Clobazam, Clonazepam, Clorazepat, Clotiazepam, Diazepam, Flunitrazepam, Flurazepam, Hydroxyzin, Ketazolam, Loprazolam, Lorazepamzepam, Lorazepamepam, Lorazepamepam , Oxazepam, oxazolam, prazepam, temazepam, tetrazepam, triazolam.

Examples of urologicals are: finasteride.

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

Examples of venous agents are: aescin, calcium dobesilate, coumarin, diosmin, rutoside, troxerutin.

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, riboflavocinophene, transiolamine, thiolamine.

Examples of cytostatics are: aclarubicin, altretamine, aminoglutethimide, amsacrine, asparaginase, bleomycin, buserelin, busulfan, carbopiatin, camnustine, chlorambucil, cladribine, cisplatin, cyclophosphamide, cytarabine, dacarbazine, daunorubicinidodinolodirid, duborolubicin, epidirubicin, epidurolubidol, dorodorubicin, dorodorubicin, dodorylubicin, dodorylbenzolin, dodorylbenzolubin, dodorylbenzolin, dodorylbenzolin, dodorotylbenzidol , Fluorouracil, Gemcitabine, goserelin, hydroxycarbamide, idarubicin, ifosfamide, lomustine, melphalan, mercaptopurine, mesna, methotrexate, miltefosine, mitomycin, mitoxantrone, panorex, paclitaxel, plicamycin, tamoxifen, tegafur, thioteporotinotin, tinvinininininblinin, vinoganinininotin, vinoganininin zorubicin.

According to the invention, the active substances mentioned can be in the form of a powder, a paste, a film, a solution or a melt and are preferably applied to the carrier material using the designated adhesion promoter. The active ingredients described and / or active ingredients contained in ginseng can also be incorporated into the carrier material.

Under certain circumstances, depending on the type of structure of the agent, i.e. H. Type of application, application or application of the active ingredients, in addition a delayed release of the active ingredient or long-lasting, delayed dosing can be achieved.

As already explained above, it can be ensured through the selection of the adhesion promoters that are preferably used that the

Dissolve the active ingredients contained in the ginseng and / or possibly the other active ingredients in the stomach and, if necessary, directly in the

Stomach. In addition, further layers of active substance may be present, which may be connected to the layer of active substance underneath by way of adhesion promoters. In this way, a combination of

Active ingredients can be achieved, which are under the conditions of

Dissolve gastric milieus and may have their effect directly in the intestine, while the carrier material as a result of it

Volume increase remains in the stomach and causes a satiety effect there. Depending on the type of active ingredient, it is also possible that it at least partially dissolves in the stomach and so only partially or not at all gets into the intestine. If additional active ingredients are applied to the carrier, any other treatments can be carried out. Among other things, a sustained release effect can also be achieved. Multilayer active ingredient structures are also conceivable, in which some of the adhesion promoters dissolve in the stomach and some do not.

In this way, any combination of active ingredients can be produced, for. T. in the stomach and z. T. unfold their effect in the intestine.

Claims

claims

1. Means for producing a satiety effect and for weight reduction containing at least one active ingredient contained in ginseng and a material which increases or increases volume and is insoluble or poorly soluble in gastrointestinal fluids and / or body fluids.

2. Composition according to claim 1, characterized in that the at least one active ingredient contained in ginseng is a ginsenoid.

3. Composition according to claim 1 or 2, characterized in that the at least one active ingredient contained in ginseng is at least partially bound to the surface of the volume-increasing material.

4. Agent according to one of claims 1 to 3, characterized in that the at least one contained in the ginseng

Active ingredient is bound to the surface of the volume-increasing material by means of an adhesion promoter that is at least partially soluble in the stomach.

5. Agent according to one of claims 1 to 4, characterized in that the adhesion promoter contains thread-like and / or fabric-like substances.

6. Agent according to one of claims 1 to 5, characterized in that the carrier material is in compressed form.

7. Composition according to one of claims 1 to 6, characterized in that it has a further formulation containing active ingredient.

8. Composition according to claim 7, characterized in that the active ingredient-containing formulation has customary auxiliaries and additives.

9. Composition according to claim 1, characterized in that the at least one active ingredient contained in the ginseng is introduced into the volume-increasing material.

10. Composition according to one of claims 1 to 9, characterized in that it is in the form of powders, granules, adsorbates, beatlets, compressed products or tablets, capsules, dragees.

11. Agent according to one of claims 1 to 10, characterized in that it contains conventional auxiliaries and additives.

12. Composition according to one of claims 1 to 11, characterized in that the volume-increasing material contains natural, semi-synthetic or synthetic polymers.

13. Composition according to one of claims 1 to 12, characterized in that the volume-increasing material contains polysaccharides.

14. Composition according to one of claims 1 to 13, characterized in that the volume-increasing material contains compressed sponge-like substances.

15. A process for the preparation of an agent for producing a saturation effect and for weight reduction, characterized in that on at least part of the surface of a gastrointestinal fluid and / or

Body fluids insoluble or sparingly soluble, volume-increasing material, possibly under pressure and high Temperature at least one active ingredient contained in ginseng is applied.

16. The method according to claim 15, characterized in that the at least one active ingredient contained in ginseng is used as a ginseng extract.

17. The method according to claim 15 or 16, characterized in that an at least partially stomach-soluble adhesion promoter is applied to at least part of the surface of the volume-increasing material and the at least one active ingredient contained in the ginseng is applied to the adhesion promoter.

18. The method according to any one of claims 15 to 17, characterized in that the adhesion promoter layer is applied to the layer containing the active ingredient contained in ginseng.

19. The method according to any one of claims 15 to 18, characterized in that the coupling agent in liquid or solid form or in the form of a powder, a paste, a film, as a solution, as a melt and / or combination thereof on the volume-increasing material and / or the layer containing the active substance and / or the active substance contained in the ginseng is applied.

20. The method according to any one of claims 15 to 19, characterized in that the at least one ginseng-containing active ingredient is introduced into the volume-increasing material.

21. The method according to any one of claims 15 to 20, characterized in that the volume-increasing material is soaked in a liquid ginseng-containing active ingredient.

22. Use of an agent according to any one of claims 1 to 14 for producing a satiety effect and for weight reduction.

23. Use of an agent according to any one of claims 1 to 14 for the manufacture of a composition for producing a satiety effect and for reducing weight.

24. Use of an agent according to one of claims 1 to 14 for the preparation of a composition for producing a time-delayed release of at least one active ingredient contained in the ginseng in the stomach and / or intestine.