SI20007A - Agent for producing a long-lasting saturation effect - Google Patents

Abstract

The present invention relates to an orally administered agent, containing material which is insoluble or poorly soluble in water and gastro-intestinal fluids, existing in the shape of a spongy formed body composed of an elastic material, which can be deformed by mastication and deglutition, reduced in form and compressed, so that it can pass through the oesophagus and can be decompressed once it has left the oesophagus in drinking liquids and gastro-intestinal fluids, thereby increasing the volume in the stomach, producing an effect of physiological saturation during its time in the stomach and causing delayed release of integrated active substances and constituents, and which then leaves the body via the intestine after several hours in the stomach in an unabsorbed or poorly absorbable state.

Description

BEISEL Gunther

A means of creating a lasting effect of satiety

The present invention relates to an oral administration agent containing in water and gastrointestinal fluids insoluble or hardly soluble material in the form of a sponge formation, to a process for its preparation and its use for the preparation of agents for satiating effect, as well as for the preparation of medicaments, additives for foods or foods with a delayed and mild release of the active substance that can be administered orally.

Numerous attempts have been made to medically break down excess fat in the human body or body. prevented their formation. There are e.g. i.e. anti-flow agents that attempt to suggest to the body in a biochemical manner resistance to food intake. However, in some cases these agents have significant adverse side effects.

In addition to the many well-known dietary suggestions, mechanical and electromechanical agents are also available to assist in the intended breakdown of fats and / or fat. muscle strengthening. The impact of such funds is highly doubtful.

DE 4025912 is known from the German patent file for oral administration, which consists of a container which can dissolve in the stomach and release its contents. It is filled with a substance that, after being released in the stomach, increases its volume, thus filling the body with a feeling of satiety.

The disadvantage of this system is that it has to be prepared with a special coating. Thus, some time passes before the agent can develop its effect in the stomach. In addition, the preparation of the coating and the compressed form of the agent are associated with higher costs.

Therefore, it is an object of the present invention to make available a means of satiety for oral administration which does not have the disadvantages of the present agents. In particular, the cost of preparing the compressed form and allowing consumption similar to that for food should be reduced.

This task is solved so that the agent consists of an elastic material,

- which can be transformed in chewing and palatal swallowing, has a diminutive shape and can be compressed so that it can pass through the esophagus,

- which, after leaving the esophagus, can be decompressed in the drinking and gastrointestinal fluids in the stomach to form a volume

- which, while contained in the stomach, produces the physiological effect of satiety and releases the bound substances and constituents with restraint, and

- which remains unabsorbed after a few hours in the stomach, or can only be resorbed slightly, leaves the body again through the intestines.

In other words, in simple chewing and swallowing, and in the absorption of fluid during passage through the human esophagus, it is compressed and, after leaving the esophagus, decompressed in water as well as in the gastrointestinal fluids in the stomach, where it predominantly regains its original volume.

Spongy formulations are understood to mean, according to the invention, foams consisting of gas-filled cells shaped like a ball-polyhedron and bounded by high viscosity or solid cell tissues. According to the invention, both natural mushrooms and synthetically prepared mushroom formulations are useful.

Preparation of sponges or sponge-shaped formations are made by processes known per se from the prior art. Depending on the starting material used, foam can be obtained in the simplest case by blowing, punching, shaking, spraying or stirring in a suitable gas atmosphere. For polymers, a foamy structure is formed based on chemical reactions. Thus, the polyurethanes are foamed by the addition of expanding agents which decompose at a certain temperature during processing upon gas formation, or by the addition of liquid solvents during polymerization. The foaming takes place either when leaving the extrusion device, e.g. after extrusion or injection molding, or in open models. Curing takes place under conditions specific to the particular chemical compound of the material.

A necessary assumption for the usability of the material of the invention and the sponge structure is that the material is compressible without destroying the cellular tissue. In order for the material of the invention to be used for oral administration, it must be foamed or molded. foam material capable of being compressed when passing through the esophagus. Especially when passing through the esophagus, no damage can occur.

Furthermore, for the choice of material and the method of foam formation, it is important that it remains able to swell without damaging the cellular tissue. After passing through the esophagus, the foam formation is expected to occupy at least the same size as it had before entering the esophagus. Optionally, the material may swell to a size that exceeds the original volume.

A O

The volume of the decompressed sponge formation is 2 cm, preferably 40 cm. However, the volume in the compressed state is 0.5 cm ³ , preferably 3 cm ³ .

The sponge-like formation may have any shape in decompressed state. However, squares or rectangular or circular shapes are preferred. The surfaces are in this

And in the case of 6 to 60 cm.

Preferably, the material is constructed such that the sponge formation is compressible to 1/2 to 1/20, preferably 1/4 to 1/10 of its volume, or. its size. Under physiological conditions, chewing and swallowing of the form should allow the reduced and compressed material to expand in the stomach, preferably at its 2- to 20-fold volume, especially preferably at its 4- to 10-fold volume, after leaving the esophagus.

As sponge-forming materials, natural, semi-synthetic or synthetic polymers are suitable for use in the invention. Examples of suitable synthetic polymers are: polyurethanes, polyacrylates, poly (meth) acrylic acid esters, homo- and copolymers of vinyl acetate. Natural and semi-synthetic polymers include, but are not limited to, cellulose, ether, diethylcellulose or cellulose esters such as cellulose diacetate, cellulose triacetate, cellulose acetate propionate and cellulose acetate butyrate. According to the invention, e.g. suitable cellulose derivatives, especially suitable ether, e.g. methylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose or sodium carboxymethyl cellulose (preferably such compounds having higher viscosities); certain polymers, such as polyacrylic acid and its salts; natural (anionic) mucus, e.g. xanthan gum, guarantor gum, tragacanth or alginic acid and its salts and the like. In addition, the use of insoluble polysaccharides such as chitin and / or polysaccharides is also possible. chitin derivative or microcrystalline cellulose. In the invention, linear high molecular weight polymers are particularly preferred. In particular, polymers having a fibrous structure are useful in the invention. Examples of such substances are scleroproteins such as keratin, concagin, fibrin, elastin, chitin and collagen. The latter is particularly preferred in the invention. The agent of the invention may comprise, inter alia, pharmaceutically effective substances, foods, or food additives - minerals, e.g. vitamins, ballast substances, proteins, as well as other food substances or flavors.

In addition to these substances, other excipients may be added to the carrier material. Among other things, retention agents may additionally be considered when pharmaceutically effective substances are used.

In addition, the agents of the present invention may further comprise fillers, disintegrants, binders and lubricants as well as carriers.

The present invention also relates to a process for the preparation of the agent described above. In principle, a suspension of the sponge-forming material is first prepared, which is then lyophilized. Optionally, the sponge-forming material is pre-crushed and / or subjected to alkaline and / or acid pre-treatment. The lyophilization is preferably carried out at -50 to -150 ° C, especially at -80 to -120 ° C.

Prior to, during or after the preparation of the sponge formation, a material with the above pharmaceutically effective substances, foodstuffs, or substances may be treated. food additives mineral substances, e.g. vitamins, ballast substances, proteins as well as other food substances or flavors. That is why all ordinary procedures come into play. In the simplest case, this can take place during the preparation phase of the sponge formation by mixing the carrier material and the active ingredient. Medicinal products, flavors or sweeteners such as e.g. chocolate, sugar glaze or similar substances.

The purpose of the process of the invention is to provide a material that is sufficiently compressible when passing through the esophagus and does not disintegrate upon prolonged retention in the stomach. This objective is achieved by the process steps indicated. Unlike other food products / supplements for foodstuffs / dietary or medicinal products, which, in a short time, gastric juice breaks down or enters the stomach already in a broken state, thus passing through (leaving) the stomach in a short time, retains the foamy ah foam a formation consisting of synthetic fibers and prepared in the manner described above, owing to the special cross-linked sites, for several hours, takes its original shape by passing through the stomach only after several hours. The fibrous mushroom is not resorbed in the stomach but eliminated unabsorbed.

In one embodiment of the process of the invention, soluble collagen from the skins of young cattle or sows (Live) can be used. The soluble collagenous parts of the animal's skin, however, are getting smaller as the age of the organism decreases, because collagen with intermolecular crosslinking forms an insoluble three-dimensional network. Crosslinking sites are solid chemical bonds between individual collagen molecules.

For the preparation of the necessary collagen suspensions for the preparation of mushrooms, the skins must therefore come from 1 to 2 years old Lives (bulls). Even these already form a collagen insoluble network. Strong alkaline and acidic pretreatment of the skin and mechanical forces in the preparation of the sponge suspension can cause the individual chemical and physical crosslinking sites to dissolve in collagen.

When the mushroom is dried by lyophilization, preferably at temperatures up to -120 ° C, new crosslinking sites are introduced into the sponge material due to relatively high temperatures. This affects the long-term insolubility of the sponge formation in gastric juice. This relative insolubility in gastric juice is a condition for the satiety effect resulting from the long retention of the mushroom in the stomach.

The present invention is not limited to the process described, but is also applicable to any other process in which mushrooms or mushroom-like bodies are prepared, which, owing to the relative insolubility in water and gastric juice, and thereby the resulting long retention in the stomach, may or may achieve long-lasting the effect of satiety.

The agent of the invention is taken orally. The solid sponge or solid foam formation proceeds by the addition of drinking fluid as well as by light chewing ah swallowing through the oral-esophageal and esophageal passages and again swells due to gastric fluid in the stomach, preferably to its original volume. Optionally, the volume may be ah smaller than the original volume.

By oral administration of the agent of the invention, it is achieved that the solid sponge ah solid foam formation is retained in the stomach for several hours due to its poor solubility. This can result in a prolonged feeling of fullness and full fatigue.

Depending on the desired level of satiety, 1 to 15 spongy formations may be taken daily at different times. Fatigue sensors that respond to the volume of the mushroom in the stomach create, through the midbrain, the effect of satiety, which is first reduced only when the stomach is emptied. Thus, the duration of satiety can be controlled by the length of retention and the size of the mushroom volume.

Hereinafter, the present invention is explained in more detail with reference to the figure:

1. A foamy cube resistant to gastric juice and water.

2. By injecting some liquid, the dry foam cube loses its solid shape and can be easily swallowed in its water-slippery form.

3. A slippery deformed foam cube passes through the esophagus.

When the mushroom arrives in the stomach, it absorbs the stomach and drinking fluid contained in it and takes up its previous volume.

5. The foam cube is retained in the stomach for 2-20 hours due to its special, non-digestible fiber structure, maintaining its volume. Because of its volume, it does not pass through the pylorus.

6. The mushroom loses its cube shape only by constant movement of the stomach (peristalsis, 1-20 hours) and the action of gastric acid (without being resorbed), so that it can first pass through the pylorus after 1-20 hours in order to she removed herself through the gut. Normal foods such as meat or vegetables break down and dissolve in stomach acid for a short time and then pass through the pylorus after a few minutes. Due to the specific fiber structure described above, the gastric agent of the invention retains its original volume due to its resistance to gastric juice, such that it is biologically (physiologically) conditioned for several hours to persist and such a saturable gastric retention.

For

BEISEL Gunther:

Claims (14)

PATENT APPLICATIONS 1. An oral preparation comprising an insoluble or hardly soluble sponge-like material in water and gastrointestinal fluids, characterized in that it consists of an elastic material which can be transformed by chewing and palatal swallowing, in a form which it can shrink, and it can be compressed so that it can pass through the esophagus, and after leaving the esophagus it can be decompressed in water and gastrointestinal fluids in the stomach to form a volume. An agent according to claim 1, characterized in that after leaving the esophagus, it can be decompressed to about the size it was before entering the esophagus by oral administration. Agent according to claim 1 or 2, characterized in that the sponge formation is compressible to 1/2 to 1/20, preferably 1/4 to 1/10 of its size. An agent according to any one of claims 1 to 3, characterized in that the mushroom formation, after leaving the esophagus, can be decompressed to its size two to twenty times, preferably four to ten times its size in the compressed state. Agent according to one of Claims 1 to 4, characterized in that the sponge-forming material is a viscous sponge. Agent according to one of Claims 1 to 5, characterized in that the sponge-forming material consists of natural, semi-synthetic or synthetic polymers. Agent according to one of Claims 1 to 6, characterized in that the sponge-forming material is composed of long-hairy, linearly colloidal, high molecular weight polymers. Agent according to claim 7, characterized in that the sponge-forming material consists of polymers with a fibrous structure, preferably of proteins. Agent according to claim 8, characterized in that the sponge-forming material is composed of scleroproteins, preferably collagen. Agent according to one of Claims 1 to 9, characterized in that it contains the sponge body of the food and / or medicaments or medicaments. active substances or flavorings and / or coated or covered externally with medicines, varnishes or food substances (sweeteners) such as chocolate, sugar glaze, fruit mass, etc. Process for the preparation of an agent according to any one of claims 1 to 10, characterized in that a suspension of collagen containing material is prepared for the sponge formation and then lyophilized. A method for preparing an agent according to any one of claims 1 to 11, characterized in that the sponge-forming material is crushed and / or subjected to alkaline and / or acid pre-treatment. Process for the preparation of an agent according to any one of claims 1 to 12, characterized in that the lyophilizations are heated at -50 to -150 ° C, preferably at -80 to -120 ° C. Use of an agent according to any one of claims 1 to 13 for the preparation of an agent for satiating effect as well as for the preparation of medicaments, food additives, foods or sweeteners with sustained and gentle release of the active ingredient and contents which can be administered orally.