RU2436415C2 - Composition of biologically active substances based on betulin with regulated rate of releasing components for reducing degree of alcohol intoxication, preventing and relieving alcohol intoxication and alcohol withdrawal syndrome - Google Patents

Abstract

FIELD: chemistry.

SUBSTANCE: invention relates to food industry, particularly to biologically active food additives. The composition of biologically active substances based on betulin with regulated rate of releasing components for reducing degree of alcohol intoxication, preventing and relieving alcohol intoxication and alcohol withdrawal syndrome contains betulin encapsulated in edible fats or wax or mxiture thereof, amber acid - 50%, ascorbic acid - 50%, glutamic acid - 50% and/or sodium glutamate and food additives, with the following ratio of components in wt %: betulin 1-10, microcapsulated amber acid 50% 1-40, microcapsulated ascorbic acid 50% 1-40, microcapsulated glutamic acid 50% and/or sodium glutamate 50% 2-75 and food additives 1-95.

EFFECT: invention enables to obtain a novel composition, having complex prolonged effect for protecting the body upon consumption of alcohol, for preventing and relieving alcohol intoxication and alcohol withdrawal syndrome, which reduces development of pathological phenomena of alcohol withdrawal syndrome, as well as alcohol tolerance before, during and after consumption.

5 cl, 1 dwg, 10 ex

Description

The invention relates to the food industry, in particular for the manufacture of various biologically active food additives. The invention lies in the fact that the composition contains betulin, succinic, ascorbic and glutamic (or monosodium glutamate) acids and food additives as active ingredients. This composition has physiological activity associated with the consumption of alcohol, and is used to solve the problem of reducing the degree of intoxication, prevention and removal of alcohol intoxication and hangover. The regular use of this composition in cases of alcohol consumption gives a secondary effect (elimination of a hangover syndrome provoking a drunken state), which is expressed in a decrease in craving for alcohol.

Biologically active food additives can be both an independent product and the basis for the creation of specialized (functional) food products intended for dietary correction of pathological conditions and diseases associated with alcohol abuse.

Alcohol is a natural metabolite for the human body - a metabolic product. Its content in a healthy body can reach up to 100 mg per 1 liter of blood, without posing a danger to the body.

Depending on the concentration of alcohol in the blood, there are three degrees of poisoning of the body:

- Light degree - at a concentration of 0.5-1.5 g / l of blood.

- Strong degree - at a concentration of 1.5-3.0 g / l of blood.

- Severe poisoning occurs when the concentration of alcohol in the blood is 3.0-5.0 g / l.

Concentrations above 5.0 g / l can cause death.

Alcohol that enters the body along with alcoholic beverages is absorbed into the blood in less than a minute and penetrates the cells. After another minute, it begins to penetrate the brain, which is subjected to the most significant toxic effects. During the oxidation of alcohol, the liver experiences a large load, where up to 90% of alcohol is oxidized. Small amounts are oxidized in the lungs, nerve tissue, kidneys and muscles, which also negatively affects these organs. A factor contributing to the hangover is the intermediate conversion of ethyl alcohol by the liver to acetaldehyde using the enzyme alcohol dehydrogenase. With an excess of alcohol in the blood, enzyme systems do not cope with complete conversion, as a result, an intermediate product is accumulated - more toxic than alcohol. Currently, there are quite a few biologically active drugs that reduce the negative effects of alcohol on the body. The most effective and harmless to the body are drugs designed for the metabolic therapy of alcohol intoxication. Such therapy is carried out by introducing metabolites into the body that protect cell membranes and stabilize the functioning of enzyme metabolism systems. Intoxication and especially alcohol intoxication, and the subsequent hangover syndrome are accompanied by the development of a number of severe subjectively and objectively observed symptoms, acute alcohol intoxication and, to an even greater extent, chronic alcoholization exacerbate many chronic diseases.

The intake of significant doses of alcohol is accompanied not only by a violation of the neuropsychiatric status as a result of the direct action of ethanol, but by the toxic effect of increasing concentrations of acetaldehyde and acetic acid. So, acetaldehyde provokes the release of catecholamines and indolamines, causes an avalanche-like activation of lipid peroxidation of biological membranes, disrupts many receptor processes. An excess of acetaldehyde forms adducts with hemoglobin, plasma proteins of the brain and other organs, inhibits the transfer of reduction equivalents along the mitochondrial respiratory chain.

Anti-alcoholic dietary supplements can be divided into dietary supplements based on succinic acid and the rest of dietary supplements of natural plant origin. The first ones were created as a result of research that began back in Soviet times, while the latter are related to the so-called traditional medicine. About 30 years ago, the famous Soviet biochemist Marina Kondrashova established that succinic acid can be a “fuel” for mitochondria - the energy “organs” of cells. And acetaldehyde (the poison formed from alcohol) inhibits all redox processes in the mitochondria, disrupts the accumulation of energy and leads to the accumulation of unoxidized products. Means containing amber acid - “Bison”, “Antipohmelin”, “Yantarite”, “Alcohol”, etc. The composition “Alcohol” uses dry water-soluble extracts of ten herbs produced by the original low-temperature water extraction and low-temperature freeze-drying, and also a complex of vitamins and minerals, amino acids, citric and succinic acids, etc. The dietary supplement "TresVit" containing succinic acid, vitamin C, citric acid and fructose. Vitamin C (ascorbic acid), which is part of TresVita; It is an antioxidant and at the same time a substance that protects other antioxidants (in particular vitamin E and beta-carotene) from being destroyed by free radicals. Vitamin C is essential for maintaining healthy gums, teeth, bones, and blood vessels. It protects the stomach from nitrates and nitrites coming with water and food, strengthens the immune system, helps the absorption of iron from plant foods - raisins, vegetables, beans. Protects the body from heart disease, cancer, colds, scurvy, as well as the harm caused by smoking and air pollution. Contained in citrus fruits, strawberries, seaweed, pepper, cauliflower and red cabbage, currants, rose hips. Ascorbic acid - Vitamin C - is an active water-soluble antioxidant, an activator of the adrenal cortex and provides an anti-stress effect of various factors on the body, including alcohol.

Every day, our body produces about 200 mg of succinic acid and uses it for its own needs. Succinic acid, which it produces or receives with food, is quite enough for a healthy body. However, under adverse conditions, when stress or a sharp change in physical activity leads to stresses in the metabolic chain, the consumption of succinic acid increases, there is a deficiency, followed by a feeling of fatigue and malaise. The therapeutic effect of succinic acid and its compounds is based on a modifying effect on the processes of tissue metabolism - cellular respiration, ion transport, protein synthesis.

Known pharmaceutical composition for the prevention, treatment of intoxication and alcohol withdrawal syndrome (RU patent N 2039556, CL A61K 31/19, 1995). It consists of: 0.1-0.3 g of succinic acid and 0.025-0.085 g of citric acid. This drug, called "Lemontar" should be taken 3-5 times a day at the rate of 3-5 mg / kg of body weight. Lemontar can be taken at home. It has an adaptogenic, antihypoxic and detoxifying effect, in some cases, after taking it, withdrawal symptoms disappear in 12-18 hours.

The molecular mechanism of detoxification using Lemontar during alcoholic intoxication is based on a decrease in the level of acetaldehyde (AcA). After taking ethanol, an increase in the concentration of AcA is observed, which leads to disruption of redox processes, depriving the cell of its ability to oxidize a number of substrates (isolimonic, malic, glutamine acids, including AcA). In this case, the accumulation of energy in the form of ATP occurs mainly due to the oxidation of succinic acid (succinate-dependent respiration), and at a high concentration of AcA it can also inhibit amber-dependent respiration, which corresponds to the appearance of the drug phase of intoxication.

Known means to reduce intoxication, prevention and removal of alcohol intoxication and hangover (patent RU No. 2160589, CL A61K 31/375, 2000). The specified tool contains as an active substance a component based on succinic acid, L-glutamic acid, (sodium mono-L-glutaminate), ascorbic acid and an energizer selected from the group consisting of aspartic acid, sodium aspartate, glycine, one of the amino acids, sorbic acid, in addition, additionally contains at least one sweetener selected from the group consisting of sucrose, glucose, sorbose, sorbitol, fructose, saccharin, aspartame, xylitol, sorbitol, with the following amount of these components in based on 1000 mg:

succinic acid 10-400 L-glutamic acid component 10-400 fumaric acid component 2-300 vitamin C 1-300 sweetener and energizer up to 1000

The disadvantages of the known agent is its low efficiency, due to the fact that succinic, ascorbic and glutamic acids, due to their high solubility, enter the bloodstream almost immediately, i.e. up to 15 minutes, which leads to their rapid inclusion in the enzyme cycles of the liver and rapid withdrawal from the body. It is known that ethyl alcohol can be in the blood of a person for more than a day, therefore, in order to have an effect, taking tablets with acids must be carried out repeatedly.

Recently, a number of valuable pharmacological properties of betulin and its derivatives (anti-cancer, anti-HIV, hepatoprotective, anti-tuberculosis and a number of others) have been experimentally confirmed along with the absence of toxicity.

The use of betulin as a hepatoprotector is known, where it reduces the activity of alanine aminotransferase and aspartate aminotransferase, alkaline phosphatase, the content of malondialdehyde, prevents the decrease of cytochrome P450 and the inflammatory process in the liver, and also has a choleretic effect (Pharmacological properties of triterpenoids of birch bark, Yu.K. V.F.Semechenkov, L.M. Frolova et al. Experimental and Clinical Pharmacology, 1993, vol. 56-4, 53-55).

The effectiveness of known methods of using betulin is explained by the fact that it is absorbed in the duodenum, enters the liver, where it increases the level of cytochrome P450, which helps prevent acute intoxication.

Betulin takes about 15 minutes to 1 hour to penetrate the blood and enter the liver cells (hepatocytes), depending on the amount and fat content of the food taken. Succinic, ascorbic and glutamic acids due to their high solubility quickly enter the bloodstream and are also quickly excreted from the body. While ethyl alcohol can be in the blood of a person for more than a day, therefore, in order to have an effect, it is necessary that the tablet lasts for several hours.

Figure 1 shows a graph showing the content of betulin in the blood of mice after a single oral administration of a suspension of betulin (200 mg / kg). From this graph it is seen that the average concentration of betulin in blood plasma after the first hour was 55 μg / ml. At the same time, the drug was released into the blood with a delay of about 10 minutes. The peak concentration of betulin is reached by 2 hours and is 95 μg / ml. Then, from 2 to 4 hours, the content of betulin in the blood decreases by 75.6%, and by 16 hours the concentration of the drug is 9% of the maximum.

The closest in technical essence and the achieved result is a composition for protecting the body when taking alcohol based on betulin (patent RU No. 2184772, class A61K 35/78, A61P 25/30). The essence of the application is that betulin is injected directly into alcoholic beverages. A disadvantage of the known composition is its low effectiveness for relieving alcohol syndrome.

Thanks to microencapsulation of acids in food waxes and fats, it became possible to regulate the content of these acids in the blood from 0.5 to 6 hours, which provides the simultaneous effect of betulin and these ingredients on the liver, which ensures their complex effect on protecting the body after drinking alcohol. The prolonged (up to 6 hours) presence of active ingredients in the blood provides the prolonged action of a new dietary supplement.

The aim of the present invention is to provide a composition of a comprehensive prolonged effect on the protection of the body when taking alcohol to prevent and relieve alcohol intoxication and a hangover syndrome, which reduces the development of pathological phenomena of a hangover syndrome, as well as improves the tolerability of alcohol before, during and after alcohol intake.

The problem is solved in that a composition of biologically active substances based on betulin is created with a controlled release rate of components to reduce the degree of alcohol intoxication and a hangover syndrome, characterized in that it additionally contains microencapsulated in edible fats or waxes or a mixture of succinic acid from them - 50% , ascorbic acid - 50%, glutamic acid - 50% and / or monosodium glutamate - 50% and food additives in the following ratio of components, wt.%:

betulin 1-10 microencapsulated succinic acid 50% 1-40 microencapsulated ascorbic acid 50% 1-40 microencapsulated glutamic acid 50% 2-75 and / or monosodium glutamate 50% 2-75 nutritional supplements 1-95

A composition of biologically active substances based on betulin with a controlled release rate of components to reduce the degree of alcohol intoxication and a hangover syndrome according to claim 1, characterized in that an extract of crushed white birch bark is used as a source of betulin.

The composition of biologically active substances based on betulin with a controlled release rate of components to reduce the degree of alcohol intoxication and a hangover syndrome according to claim 1, characterized in that stearic acid and / or esters based on it are used as edible fats or waxes for microencapsulation of these components (mono-, di-, and / or triglycerides of stearic acid), and / or polyethylene glycol, and / or beeswax, and / or microcrystalline wax, or mixtures thereof.

The composition of biologically active substances based on betulin with a controlled release rate of components to reduce the degree of alcohol intoxication and a hangover syndrome according to claim 1, characterized in that water and / or food-grade surfactants (emulsifiers) are used as food additives, and / or colorants and / or flavors and / or vitamins and / or disintegrants and / or sweeteners and / or sugars and / or minerals and / or acids and / or alkali and / or salts and / or microcrystalline cellulose ", and / or gelling agents, silt mixtures thereof.

A composition of biologically active substances based on betulin with a controlled release rate of components to reduce the degree of alcohol intoxication and a hangover syndrome according to claim 1, characterized in that it is a powder mixture, or a granular mixture, or a tablet, or a capsule, or dragee, or lozenge or gel or suppository or suspension.

The composition can be administered orally or rectally no later than 30 minutes before drinking or while taking alcohol, 1-2 tablets or dragees, or capsules.

Due to the fact that the concentration of betulin in the blood is maintained in the range from 0.5 to 5 hours, it is of interest that the concentrations of known anti-alcohol substances (succinic, glutamic and ascorbic acids) are also in the blood in the same time interval.

For this, ground powders (25-100 μm) of these acids were microencapsulated by spraying in a melt of edible fats or waxes or a mixture of them. At a 50% content of each acid (ascorbic, glutamic or succinic) in the stearic acid matrix, the rate of their release is practically independent of the nature of the acid and is shown in FIG. 2.

It can be seen that after 2 hours about 60% of the acid is released, which corresponds to the maximum release of betulin in the blood. Those. it turns out that betulin and a mixture of acids protect the liver at the same time and for from 0.5 to 6 hours.

The composition for protecting the body when taking alcohol is prepared as follows:

In a heated reactor, edible fat or wax, or mixtures of them, are melted at a temperature of 55-65 ° C, then crushed acid powder is added, mixed until homogeneous, other additives are added. The resulting suspension is fed to a spray turbine. The resulting droplets freeze in the air and are collected in a receiving device, the resulting powder passes through sieving on a sieve and is packed in an airtight container. The granule size is controlled by the speed of rotation of the turbine and varies from 0.1 to 1 mm. Technology according to the patent of the Russian Federation No. 2311953.

A significant difference of the proposed composition is the use of edible fats and waxes, as well as mixtures of them as a shell of microcapsules for acids. As food fats or waxes, stearic acid and esters based on it (mono-, di- or triglycerides), polyethylene glycol, beeswax, microcrystalline wax or mixtures thereof are used.

The composition of the composition can also be additionally introduced permitted food additives (flavorings, colorants, sweeteners, emulsifiers, etc.) and mixtures thereof.

Compared with the analogue (patent RU No. 2160589, class A61K 31/375, 2000), the use of microencapsulated succinic, glutamic and ascorbic acids due to their gradual release from the shell of microcapsules has a less irritating effect on the mucous membranes of the gastrointestinal tract, does not cause hypertensive effect, prevents, and not only stops, the development of hypoxia, ischemia, contributes to an active decrease in the concentration of ethanol and acetaldehyde in the body.

It should be noted that the use of the described components separately, even in shock doses, does not lead to an equally tangible effect. The proposed composition by the combination of its ingredients due to their mutual influence provides a synergistic effect, which is expressed in reducing the development and elimination of the pathological phenomena of the hangover syndrome, as well as in improving the tolerance to alcohol.

Compared with the closest analogue (patent RU No. 2184772, class A61K 35/78, A61P 25/30), the proposed composition more effectively protects the body from alcohol, because due to the encapsulation of acids in food waxes and fats, it became possible to regulate the content of these acids in the blood from 0.5 to 6 hours, which provides the simultaneous effect of betulin and these ingredients on the liver, due to their complex effect on protecting the body after drinking alcohol. The prolonged (up to 6 hours) presence of active ingredients in the blood provides the prolonged action of a new dietary supplement.

The technical result to which the invention is directed is to improve tolerance to alcohol, reduce the degree of intoxication, prevent or effectively relieve alcohol intoxication and withdrawal (hangover) syndrome. The specified technical result is achieved through the use of biologically active substances in certain amounts in the composition and the use of technology for their microencapsulation in order to regulate the rate of absorption in the gastrointestinal tract and prolong their action.

The effectiveness of this composition has been proven by clinical trials conducted on the basis of the addiction department of St. Petersburg City Hospital No. 40.

On the basis of the department of the State Health Institution “City Hospital No. 40” of St. Petersburg and the Department of Pharmacology of the Medical Academy named after I.I. Mechnikov conducted clinical trials of the effectiveness of a biologically active food supplement (dietary supplement "Alkoshchit"), which is a composition of biologically active substances based on betulin with an adjustable release rate of components to reduce the degree of intoxication, prevention and removal of alcohol intoxication and hangover . The aim of the study was to study the ability to eliminate post-toxic functional disorders of the gastrointestinal tract and hepatobiliary disorders by adding this dietary supplement to standard anti-alcohol therapy. Dietary supplement for food “Alkoshchit”, manufactured by JSC “SNS-pharma”, St. Petersburg, is a tablet or hard gelatin capsules of 300 mg.

The object of the study was to study the speed and completeness of the reduction of postintoxication somato-vegetative, neuropsychiatric disorders and biochemical parameters most common in patients with alcoholic disease (AZ).

The study involved 30 men aged 40 to 70 years, with the limitation of alcohol withdrawal syndrome (AAS) from 5 to 30 years, who underwent planned anti-alcohol treatment in the drug treatment department of the City Hospital No. 40. The vast majority of the surveyed group was repeatedly treated on an outpatient and inpatient basis. In the past, about 30% of them had remissions for more than a year; about 70% of patients suffered acute alcohol psychoses. Alcohol type personality changes were predominantly explosive, epileptoid, astheno-depressive, and astheno-apathetic. All patients of the study group were admitted to the department with AAS symptoms of varying severity. The status presented the whole spectrum of psycho-neurological and somato-vegetative disorders characteristic of both AAS and chronic alcohol intoxication, including a moderately and intensely expressed pathological attraction to alcohol (PVA). This was evidenced by complaints of patients, their behavioral reactions, affective disorders and somato-vegetative disorders. Upon admission, blood was taken from all patients for general clinical analysis and standard biochemical parameters: sugar, bilirubin, aspartate- (ACT) and alanine (ALT) - aminotransferases. As a result of the first study, all patients of the study group revealed elevated blood sugar, bilirubin, as well as ACT and ALT.

From the first day of treatment, all patients received a standard set (see “Standards for Narcological Assistance”, 2003) of detoxification and symptomatic therapy, as well as dietary supplements “Alkoshchit” in a standard dosage: 2 capsules × 3 times a day with meals during next 15 days. Specific (sensitizing, conditioned reflex or psychotropic) anti-alcohol treatment was not carried out for patients. Clinical observation showed that after 2-3 single doses of “Alcohol Shield” there was a significant improvement in appetite, and by the end of 2 days, patients not only ate the standard set of food offered in the hospital, but many had manifestations of bulimia. In the control group (15 patients corresponding to the examined group by age and clinical manifestations, but who received only the standard therapeutic kit), anorexia was reduced on the 5-6th day of treatment.

The results of clinical observations showed that in all 30 patients (100%) of the study group, the disappearance of anorexia occurred two times faster than in patients who did not receive Alcohsite, satisfactory in terms of treatment (without the targeted use of psychotropic therapy) reduction of affective disorders, and also the successful elimination of asthenic symptoms in the vast majority of patients. Dynamic laboratory observation (at admission and at discharge) revealed an increase in hemoglobin of 10-20 g / l in almost all patients, a decrease in leukocytosis and a decrease in ESR by 5-7 mm. Normalization of biochemical parameters (total bilirubin, blood sugar, ACT and ALT activity) was observed in 100% of patients. In the general analysis of urine during discharge, pathological changes were noted.

Given the specifics of monitoring drug addiction by patients, their attention, of course, was focused on the relevance of alcoholic experiences in patients. Perhaps that is why numerous (24 patients) reports of patients about the weakening of alcohol experiences by the end of the 2nd day of treatment attracted attention. By the end of 4 days, all 30 patients denied alcohol addiction.

The invention is illustrated by examples.

Example 1

A 50 wt.% Stearic acid melt is prepared in a stirred reactor at a temperature of 60-65 ° C., then 50 wt.% Powder of milled succinic acid or ascorbic acid, or glutamic acid and / or monosodium glutamate are separately charged. The mixture is stirred until a uniform suspension is obtained for 0.5 hours. After that, the composition is sprayed on a turbine to obtain a free-flowing encapsulated product. Thus obtained three powders of encapsulated organic acids in a predetermined ratio are used to prepare a powder mixture. The composition is prepared by mixing the ingredients in the following ratio of components (wt.%):

betulin 5 microencapsulated succinic acid 50% twenty microencapsulated ascorbic acid 50% twenty microencapsulated glutamic acid 50% twenty monosodium glutamate 50% twenty nutritional supplements (magnesium stearate and microcrystalline cellulose) fifteen

The obtained powder composition can be used for the manufacture of tablets by compression.

Example 2

A melt of a mixture of stearic acid mono- and diglyceride of 50 wt.% At a temperature of 60-65 ° C is prepared in a stirred reactor, then 50 wt.% Of powder of ground succinic acid or ascorbic acid or glutamic acid are loaded with stirring. The mixture is stirred until a uniform suspension is obtained for 0.5 hours. After that, the composition is sprayed on a turbine to obtain a free-flowing encapsulated product.

To prepare a powder mixture for gelatin capsules, a composition is prepared by mixing the ingredients in the following ratio of components (wt.%):

betulin one microencapsulated succinic acid 50% one microencapsulated ascorbic acid 50% one microencapsulated glutamic acid 50% 2 nutritional supplements (magnesium stearate, vitamins B1, B2, B6, PP, lactose, fructose, glycine, menthol, baking soda, food coloring) 95

The resulting powder composition can be used for loading in gelatin capsules.

Example 3

In a reactor with a stirrer, a melt of a mixture of beeswax 40 wt.% And polyethylene glycol 10 wt.% Is prepared at a temperature of 60-65 ° C, then 50 wt.% Of powder of milled succinic acid or ascorbic acid or glutamic acid are loaded with stirring. The mixture is stirred until a uniform suspension is obtained for 0.5 hours. After that, the composition is sprayed on a turbine to obtain a free-flowing encapsulated product.

To prepare a powder composition for drazhirovany prepare a mixture of ingredients in the following ratio of components (wt.%):

betulin 10 microencapsulated succinic acid 50% 40 microencapsulated ascorbic acid 50% 10 microencapsulated glutamic acid 50% 10 nutritional supplements (magnesium stearate, sucrose, fructose, flavoring, TWIN-80, food coloring, calcium carbonate, sodium sorbate, sodium aspartate, water) thirty

The resulting powder composition can be used for the manufacture of dragees.

Example 4

A 50 wt.% Microcrystalline wax melt is prepared in a stirred tank reactor at a temperature of 60-65 ° C., then 50 wt.% Powder of milled succinic acid or ascorbic acid or glutamic acid is loaded with stirring. The mixture is stirred until a uniform suspension is obtained for 0.5 hours. After that, the composition is sprayed on a turbine to obtain a free-flowing encapsulated product.

To prepare a composition for suspension, a mixture of ingredients is prepared in the following ratio of components (wt.%):

betulin 5 microencapsulated succinic acid 50% 5 microencapsulated ascorbic acid 50% 40 microencapsulated glutamic acid 50% 25 nutritional supplements (maltose, glycerin, sodium alginate flavoring TWIN-60, food coloring, aspartame, water) 25

The resulting powder composition can be used to make the suspension.

Example 5

In a stirred reactor, a melt of a mixture of mono- and diglyceride 25 wt.% And stearic acid 25 wt.% Is prepared at a temperature of 60-65 ° C, then 50 wt.% Powder of milled succinic acid or ascorbic acid or glutamic acid is loaded with stirring. The mixture is stirred until a uniform suspension is obtained for 0.5 hours. After that, the composition is sprayed on a turbine to obtain a free-flowing encapsulated product.

To prepare a pastilles mixture, the composition is prepared by mixing the ingredients in the following ratio of components (wt.%):

betulin 5 microencapsulated succinic acid 50% 5 microencapsulated ascorbic acid 50% 5 microencapsulated glutamic acid 50% 60 food additives (flavoring, xanthan gum, water, food coloring, glycerin, citric acid) 25

The resulting powder composition can be used for the manufacture of lozenges.

Example 6

In a stirred reactor, a melt of a mixture of stearic acid triglyceride of 10 wt.% And 40% of stearic acid is prepared at a temperature of 60-65 ° C, then 50 wt.% Of powder of ground succinic acid or ascorbic acid, or glutamic acid and sodium glutamate are loaded. The mixture is stirred until a uniform suspension is obtained for 0.5 hours. After that, the composition is sprayed on a turbine to obtain a free-flowing encapsulated product. To prepare a tablettable mixture, a composition is prepared in the following ratio of components (wt.%):

betulin 10 microencapsulated succinic acid 50% 25 microencapsulated ascorbic acid 50% 25 microencapsulated glutamic acid 50% fifteen monosodium glutamate 50% 5 nutritional supplements (magnesium stearate and microcrystalline cellulose) twenty

The obtained powder composition can be used for the manufacture of tablets by compression.

Example 7

A 50 wt.% Polyethylene glycol melt is prepared in a stirred tank reactor at a temperature of 60-65 ° C., then 50 wt.% Of powdered milled succinic acid or ascorbic acid or glutamic acid is loaded with stirring. The mixture is stirred until a uniform suspension is obtained for 0.5 hours. After that, the composition is sprayed on a turbine to obtain a free-flowing encapsulated product.

To prepare a mixture for suppositories, a composition is prepared in the following ratio of components (wt.%):

betulin 10 microencapsulated succinic acid 50% 5 microencapsulated ascorbic acid 50% 5 microencapsulated glutamic acid 75 food additives (glycerin and microcrystalline cellulose) 5

The resulting composition can be used for the manufacture of suppositories.

Example 8

A 50 wt.% Stearic acid melt is prepared in a stirred tank reactor at a temperature of 60-65 ° C., then 50 wt.% Powder of milled succinic acid or ascorbic acid or glutamic acid is loaded with stirring. The mixture is stirred until a uniform suspension is obtained for 0.5 hours. After that, the composition is sprayed on a turbine to obtain a free-flowing encapsulated product.

To prepare the mixture for the gel, the composition is prepared in the following ratio of components (wt.%):

betulin 10 microencapsulated succinic acid 50% thirty microencapsulated ascorbic acid 50% thirty microencapsulated glutamic acid 50% fifteen nutritional supplements (water, xanthan gum, vitamin E and aspartame) fifteen

The resulting powder composition can be used to make gels.

Example 9

A 50 wt.% Stearic acid melt is prepared in a stirred tank reactor at a temperature of 60-65 ° C., then 50 wt.% Powder of milled succinic acid or ascorbic acid or glutamic acid is loaded with stirring. The mixture is stirred until a uniform suspension is obtained for 0.5 hours. After that, the composition is sprayed on a turbine to obtain a free-flowing encapsulated product.

To prepare a granular mixture, a composition is prepared in the following ratio of components (wt.%):

betulin 8 microencapsulated succinic acid 50% twenty microencapsulated ascorbic acid 50% fifteen microencapsulated glutamic acid 50% thirty nutritional supplements (calcium carbonate, sodium bicarbonate and water) 27

The resulting powder composition can be used to make a granular mixture.

Example 10

A 50 wt.% Stearic acid melt is prepared in a stirred tank reactor at a temperature of 60-65 ° C., then 50 wt.% Powder of milled succinic acid or ascorbic acid or glutamic acid is loaded with stirring. The mixture is stirred until a uniform suspension is obtained for 0.5 hours. After that, the composition is sprayed on a turbine to obtain a free-flowing encapsulated product.

To prepare a powder mixture, a composition is prepared in the following ratio of components (wt.%):

betulin 10 microencapsulated succinic acid 50% fifteen microencapsulated ascorbic acid 50% twenty microencapsulated glutamic acid 50% 25 nutritional supplements (sugar, orange oil, guar gum, citric acid and b-carotene) thirty

The resulting powder composition can be used to make tablets by compression or to fill gelatin capsules.

Claims (5)

1. A composition of biologically active substances based on betulin with a controlled release rate of components to reduce the degree of alcohol intoxication and a hangover syndrome, characterized in that it additionally contains microencapsulated in edible fats or waxes or a mixture of them succinic acid - 50%, ascorbic acid - 50 %, glutamic acid - 50% and / or monosodium glutamate and food additives in the following ratio of components, wt.%:
betulin 1-10 microencapsulated succinic acid 50% 1-40 microencapsulated ascorbic acid 50% 1-40 microencapsulated glutamic acid 50% and / or monosodium glutamate 50% 2-75 nutritional supplements 1-95 2. A composition of biologically active substances based on betulin with a controlled release rate of components to reduce the degree of alcohol intoxication and a hangover syndrome according to claim 1, characterized in that an extract of crushed white birch bark is used as a source of betulin. 3. The composition of biologically active substances based on betulin with a controlled release rate of components to reduce the degree of alcohol intoxication and a hangover syndrome according to claim 1, characterized in that stearic acid and / or esters are used as edible fats or waxes for microencapsulation of the above components basis (mono- and / or di- and / or triglycerides), and / or polyethylene glycol, and / or beeswax, and / or microcrystalline wax, or mixtures thereof. 4. A composition of biologically active substances based on betulin with a controlled release rate of components to reduce alcohol intoxication and a hangover syndrome according to claim 1, characterized in that water and / or food-grade surfactants (emulsifiers) are used as food additives, and / or colorants and / or flavors and / or vitamins and / or disintegrants and / or sweeteners and / or sugars and / or minerals and / or acids and / or salts and / or microcrystalline cellulose, and / or gelling agents, or mixtures thereof. 5. The composition of biologically active substances based on betulin with a controlled release rate of the components to reduce the degree of alcohol intoxication and the hangover syndrome according to claim 1, characterized in that it is a powder mixture, or granular mixture, or tablet, or capsule, or dragee, or lozenge, or gel, or suppository, or suspension.

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