The means for lowering the alcohol, the prevention and removal of alcohol intoxication and hangover and the way to reduce alcohol, prevention and removal of alcohol intoxication and hangover using this tool

 

(57) Abstract:

The invention relates to medicine and relates to means for reducing alcohol intoxication. The invention lies in the fact that the product contains as active ingredients component-based succinic acid, at least one component on the basis of L-glutamic acid selected from the group consisting of L-glutamic acid, mono - and L-glutaminate sodium, di-L-glutaminate sodium, mono-L-glutaminate ammonium, di-L-glutaminate ammonium, mono-L-glutaminate and potassium di-L-glutaminate potassium, at least one component based on fumaric acid, selected from the group consisting of fumaric acid, monopolarity sodium, difumarat sodium, monopolarity ammonium, difumarat ammonium, monopolarity potassium, difumarat potassium, ascorbic acid and at least one energization selected from the group consisting of aspartic acid, sodium aspartate, glycine, one of the amino acid, sorbic acid, in addition, contains at least one sweetener selected from the group consisting of sucrose, glucose, sorbose, sorbitol, fructose, saccharin, aspartame, celata, sorbitol, at a certain specified number of withdrawal intoxication and hangover. The invention provides improved portability of alcohol, ensure the effectiveness of impact tools before, during and after alcohol at home without qualified medical supervision. 2 S. and 6 C.p. f-crystals, 7 PL.

The invention relates to medicine and can be used as food oriented as biologically active food supplements and drugs to solve the problem of reducing the severity of alcohol withdrawal alcohol intoxication and hangover, and also to reduce craving for alcohol.

Intoxication and especially alcohol intoxication and subsequent hangover accompanied by the development of a number of heavy subjectively and objectively observable symptoms: discomfort, inadequate perception, headache, impaired long-term memory formation, thirst, apathy (and sometimes hyperactivity, agitation, removable depression, impaired coordination, reduced reaction rate and a number of other abnormalities of varying severity physiological, psychological, neurological and somatic nature.

Even acute alcohol intoxication and even more XP is isbalanced and weakening of the immune system, occur or begin to progress new and previously hidden disease, reduced resistance to impact loads and extreme environmental factors. Often and especially dangerous disorders of the cardiovascular system, manifested in the development of ischemic and spastic changes in blood flow not only to the heart muscle, and brain, almost all parenchymatous organs and limbs, until the effects of acute cardiac insufficiency. Often repeated alcohol intoxication are the direct cause expressive malignant course of hypertension and diseases of the kidneys and liver, acute and latent progression of existing diabetes mellitus.

Depending on individual sensitivity, largely determined genetically programmed set of enzymes and their activity, up to a certain threshold dose intake of alcohol may not be accompanied by the development of significant physiological dysfunction and the appearance of a dangerous pathological changes. The magnitude of this "safe" threshold due to activity, primarily alcoholdehydrogenase, a specific set of them and is particularly a sufficient number of other substrates of energy metabolism, finally, the activity of antioxidant systems. In other words, the activity of those systems that provide utilization of ethanol and its oxidation products of acetaldehyde and acetic acid, is continuously formed as a result of normal metabolic transformations of human consumption of food.

The excess of the individual threshold - receiving significant doses of ethanol, accompanied not only a violation of the neuropsychiatric status in the result of direct action of ethanol, but the toxic effect of increasing concentrations of acetaldehyde and acetic acid. So, acetaldehyde induces the release of catecholamines and indolamines, causes an avalanche activation of lipid peroxidation of biological membranes, violates many of receptor processes. Excess acetaldehyde forms adducts with hemoglobin, plasma proteins of brain and other organs, leading to inhibition of migration remedial equivalents for the respiratory chain of mitochondria.

Consequently develops a number of pathological processes. First, there are multiple hypoxic and ischemic phenomena, increasing and acquiring sustainable with increasing conc the maintenance ability of sperm breaks the function of the oocytes and the integrity of the mitochondrial DNA of the egg, resulting in infertility or the occurrence of mutations, which is born of non-viable offspring or suffering from diverse diseases of different severity. Third, impaired synthesis of nuclear and mitochondrial DNA in somatic cells, which leads to organic lesions, accelerating decrepitude of the body and the early acquisition of the diseases of old age. Fourth, repeated use of alcohol develops sustainable alcohol dependence. Finally, there is the fluidization of cell membranes, resulting in damage and increased permeability of blood-brain barrier, which dramatically increases the penetration into the brain of toxic endogenous products and significantly reduces the toxic threshold of perception of ethanol.

Given that 90% of the Caucasian population consume alcohol, and in Russia up to 40% of the male population suffer from alcohol dependence in some degree, the severity of these problems is obvious. Hence clear the urgent need to find means for the reduction and elimination of consequences of alcohol consumption.

On segodnyashniy reducing the rate of supply of ethanol and facilitate its oxidation products to carbon dioxide and water due to the additional sustain energy and plastic metabolism of exogenous substrates. Next, as a rule, marinades, coffee, fruit drinks, kvass and other foods that help to carry out partial detoxification, promoting diuresis, to restore hormone balance. But the effectiveness of domestic funds are clearly insufficient.

In the development of special means of protection of the body from alcohol can be divided into two main trends:

- search for dosage forms that allows emergency medical care (transfusions gemodeza, protein-salt and enriched with amino acids and glucose solutions, the use of clonidine, cytochrome C, Kelantan and others)

- search of food or drugs "OTC" forms of adjustment of status, used without medical supervision or in the form of biologically active additives to food.

Widely known drug Alka-Seltzer, containing one tablet 0,324 g of acetylsalicylic acid as an active ingredient, 0,965 g of citric acid as an auxiliary means and 1,625 g of sodium bicarbonate to neutralize the acid with carbon dioxide when dissolved and creating the effect of sipacate" get a drink (information leaflet prescription drug Alka-Seltzer, the firm Miles, UK). This drug for the pressure and partially relieves headache. However, the drug Alka-Seltzer does not relieve the main symptoms of alcohol intoxication and not restores.

Known to be the remover of alcohol (RF patent N 2012350, MKI A 61 K 35/78, 1994), containing 20 drops of the alcoholic tincture of peppermint or 2 drops of peppermint oil, 1 g of succinic acid, 10 grams of sugar or fructose, the rest water. This drug can only partially remove heavy consequences arising from intoxication.

Renowned pharmaceutical composition for the prevention and treatment of alcohol intoxication and alcohol withdrawal syndrome (RF patent N 2039556, MKI A 61 K 31/19, 1995), taken as a prototype. It includes: 0.1-0.3 g of succinic acid and 0.025-of 0.085 g of citric acid. This drug is called Lemonte should take 3-5 times a day at the rate of 3-5 mg/kg of body weight. Lemonte you can take home. He has adaptogenic, antihypoxic and detoxifying effect, in some cases, after receiving abstinence disappears for 12-18 hours.

We can conclude that to date, there are no available medicines or food supplements that not only remove the problem, svyazannim alcohol.

Actually this leads to the application as the most effective means of re-use of alcohol (hung over), which is a mandatory stage in the development of alcoholism.

The present invention is the task of creating a means to reduce alcohol, prevention and removal of alcohol intoxication and hangover in the form of biologically active food additives, minimizing development and the elimination of pathological phenomena hangover, and improved portability of alcohol and reduction of alcohol, prevention and removal of alcohol intoxication and hangover, providing effective tools before, during and after alcohol at home without qualified medical supervision.

The problem is solved in that the means for lowering the alcohol, the prevention and removal of alcohol intoxication and hangover, containing as active ingredient a component-based succinic acid, according to the invention, as active substances further comprises at least one component on the Oia, di-L-glutaminate sodium, mono-L-glutaminate ammonium, di-L-glutaminate ammonium, mono-L-glutaminate and potassium di-L-glutaminate potassium, at least one component based on fumaric acid selected from the group consisting of fumaric acid, monopolarity sodium, difumarat sodium, monopolarity ammonium, difumarat ammonium, monopolarity potassium, difumarat potassium, at least one energization selected from the group consisting of aspartic acid, sodium aspartate, glycine, one of the amino acid, sorbic acid, in addition, further comprises ascorbic acid and at least one sweetener selected from the group consisting of sucrose, glucose, sorbose, sorbitol, fructose, saccharin, aspartame, xylitol, sorbitol, with the following number of specified components based on 1000 mg:

succinic acid - 10-400 mg;

component on the basis of L-glutamic acid - 10 - 400 mg;

component-based fumaric acid - 2 - 300 mg;

ascorbic acid - 1 mg - 300;

the sweetener and energization to 1000 mg.

As a component-based succinic acid means may include at least one salt of succinic acid, selected from the group consisting of MES is crenata potassium or a mixture of the mentioned salts with succinic acid.

For the formation of fizzy drink on 1000 mg of the mixture means further comprises 20% of the amount of sodium bicarbonate, equimolar quantity of acids.

According to the claimed invention, the tool is a powder mixture or granulated mixture, or tablet, or capsule, or pills.

The problem is solved in that in the method of reducing alcohol, prevention and removal of alcohol intoxication and hangover by introducing a medicinal product according to the invention, as drug use tool according to any one of the preceding paragraphs, suitable for use before and/or during and/or after alcohol.

The tool can be entered orally or no later than 30 minutes before drinking alcohol or while alcohol 1 -2 tablets or pills, or capsules, or one glass of fizzy drink or after acceptance of alcohol 1-4 tablets or pills, or capsules or 1-2 glasses of fizzy drink.

All major active components (succinate, fumarate and L-glutaminate) are endogenous substrates involved in the main loop of intracellular metabolism - the cycle Crassamentum including weak energization.

All components are well studied and are standard components of food products.

Compared with the nearest functional equivalent (mixture of succinic and citric acids) of the proposed tool has a less irritating effect on the mucous membranes of the gastrointestinal tract, does not cause hypertensive effect, prevents (and not only eliminates) the development of hypoxia, ischemia, actively reduces the concentration of ethanol and acetaldehyde in the body.

Succinate are adaptogens that are specific antidotes against acetaldehyde, mitochondrial antioxidants, detoxicate, anti-ischemic and antihypoxic agents, antimutagens and effective energization.

L-glutaminate are highly effective energization, effectively slowing down the process of utilization of ethanol.

Fumarate together with succinate ensure the sustainability of the membranes stabilize the circulatory system, providing a powerful, time-stretched antihypoxic effect.

Ascorbic acid - vitamin C - active water-soluble antioxidant, an activator of the adrenal cortex, which provides stress among the enforcement of energization. This pharmokinetic and the length of wire used various substances and provide sustainable long-term effect.

It should be noted that the application of the described components separately even shock doses did not lead to an equally noticeable effect. Offer means the aggregate of its constituent ingredients due to their mutual influence provides a synergistic effect in terms of the reduction of development and the elimination of pathological phenomena hangover, and improved tolerance of alcohol.

According to the claimed invention, as one of the active ingredients the product contains succinic acid or at least one salt of succinic acid selected from the group consisting of mononucleate ammonium, disuccinate ammonium, monosaccate sodium, disuccinate sodium, monosaccate potassium, disuccinate potassium, or a mixture of the mentioned salts with succinic acid. As active substances the product contains at least one component on the basis of L-glutamic acid selected from the group consisting of L-glutamic acid, mono-L-glutaminate sodium, di-L-glutaminate sodium, mono-L-glutaminate ammonium, di-L-glutaminate Ancelotti, selected from the group consisting of fumaric acid, monopolarity sodium, difumarat sodium, monopolarity ammonium, difumarat ammonium, monopolarity potassium, difumarat potassium. As EnergyStar taken at least one component selected from the group consisting of aspartic acid, sodium aspartate, glycine, one of the amino acid, sorbic acid. In addition, the claimed means further comprises ascorbic acid and at least one sweetener selected from the group consisting of sucrose, glucose, sorbose, sorbitol, fructose, saccharin, aspartame, xylitol, sorbitol, with the following number of specified components based on 1000 mg:

component-based succinic acid - 10 - 400 mg;

component on the basis of L-glutamic acid - 10 - 400 mg;

component-based fumaric acid - 2-300 mg;

ascorbic acid - 1 mg - 300;

the sweetener and energization to 1000 mg.

The tool may further comprise 20% of the amount of sodium bicarbonate equimolar quantity of acids.

According to the claimed invention, the tool is a powder mixture or granulated mixture, or tablet, or capsule, or d is dry with subsequent dry pelletizing, dragonavenger or kapsulirovaniem.

The process of obtaining the proposed funds in the form of pellets is carried out in the following sequence: a sweetener and ascorbic acid dissolved in distilled water, evaporated to obtain a viscous mass, salt podbresova before the formation of a pea. The resulting pea dragonaut in the sugar mass and dried to equilibrium moisture.

The following examples of compositions a means to reduce alcohol, prevention and removal of alcohol intoxication and hangover in no way limit the invention, but is shown merely to illustrate it.

Example 1

Used tablet offer tools "Antipolis" 500 mg composition:

100 mg of succinic acid;

100 mg of mono-L-glutaminate sodium;

37.5 mg fumaric acid;

25 mg of ascorbic acid;

237,5 mg of glucose.

Method of preparation - tableting powder.

Example 2

Used powder composition weight 1000 mg ingredients:

200 mg of succinic acid:

200 mg L-glutamic acid;

75 mg of fumaric acid;

40 m is for make sipacate").

Method of preparation - dry mixing.

Example 3

The capsule contains tools:

400 mg monoacrylate ammonium;

10 mg of di-L-glutaminate potassium;

300 mg of monopolarity sodium;

1 mg of ascorbic acid;

up to 1000 mg - 50% sorbitol and 50% of aspartame.

Method of preparation - dry mixing followed by kapsulirovaniem.

Example 4

Tablet contains tools:

400 mg of a mixture of disuccinate potassium (70 mg) and monosaccate sodium (330 mg);

10 mg of mono-L-glutaminate ammonium:

2 mg of difumarat potassium;

300 mg of ascorbic acid;

up to 1000 mg of a mixture of glycine and aspartate sodium, taken in equal proportion.

Method of preparation - mix all except glycine and mono-L-glutaminate ammonium, then joint adulteration of glycine and salts and mixtures. The mixture is moistened to 7 wt. % moisture, is passed through a granulator, and dried to 2 wt.% moisture and tabletirujut.

Example 5

The product contains:

300 mg disuccinate sodium;

50 mg of a mixture containing 10 mg of di-L-glutaminate sodium and 40 mg L-glutamic acid;

120 mg of a mixture of 20 mg of monopolarity ammonium and 100 mg of fumaric acid;

200 mg of ascorbic acid;

up to 1000 mg what is dry mixing.

Example 6

The product contains:

80 mg of a mixture of 70 mg of succinic acid and 10 mg of disuccinate ammonium;

250 mg of a mixture containing equal proportions of mono-L-glutaminate potassium and mono-L-glutamine sodium;

160 mg of monopolarity potassium;

250 mg of ascorbic acid;

up to 1000 mg of a mixture of xylitol, sorbose and saccharin, taken in equal proportion.

The method of preparation. Mix separately 80 mg of a mixture of 70 mg of succinic acid and 10 mg of disuccinate ammonium, 250 mg of a mixture containing equal proportions of mono-L-glutaminate potassium and mono-L-glutamine sodium and 160 mg of monopolarity potassium. Separately mix the ascorbic acid and sugar substitutes.

The way to reduce alcohol, prevention and removal of alcohol intoxication and hangover is carried out by oral administration of the above agents, suitable for use before and/or during and/or after alcohol.

Tests in the examples below were carried out on groups of volunteers to assess the proposed compositions for subjective and objective performance.

The tests were performed under the following conditions.

the alcohol in the home has permitted the admission of other alcoholic beverages according to individual preferences.

The evaluation was performed:

1. when taking 50 ml of vodka on an empty stomach (laboratory conditions)

2. when drinking at home no fixed minimum or maximum dose

3. when mild hangover the next morning after the maximum possible intake of alcohol in the home.

All studies were recorded subjective state (based on survey) and was conducted objective control status of the subject on the parameters of the dynamics of the rhythms of the electroencephalogram, electrocardiogram, the volume of short-term and long-term memory, variational pulsometry and electrocardiography.

Additional biochemical studies were conducted to determine the status of carbohydrate metabolism, the degree of anaerobic activation of glycolysis and the development of acidosis.

Three volunteers mass by a spectroscope had determined the rate of ethanol oxidation on the rate of release of13C isotope carbon dioxide in breath after ingestion on an empty stomach 20 ml vodka, which was additionally added 40 μl of enriched isotope13C natural ethanol.

When testing was used pills "Lamentar" (prototype), 250 mg, sasaram 1 and 2, respectively.

Test 1

In laboratory conditions, a volunteer group of 12 persons of both sexes (5 men and 7 women) who do not use systematically alcohol, took 50 ml of vodka. Two types of surveys were carried out on an empty stomach:

a) pre-admission within 30 minutes alternately each species compositions and without receiving random by day (4 tablets of Lemontea", 2 tablets "Antionline" 3 g "effervescent composition on a water glass);

(b) receiving similarly to the previous directly with vodka or 30 minutes after taking vodka if desired.

Each volunteer took the vodka in the laboratory 7 times with an interval of a week without drugs, with each of the songs in the queue to receive (a), with each of the songs in the queue during or after administration of (b).

As can be seen from tables 1 and 2 data, the claimed means significantly contributed to the improvement of the subjective condition and objectively registered parameters of brain activity, including improving short and long term memory, cardiovascular system, glucose homeostasis and ischemic changes, most commonly caused by alcohol. Detected positive developments characterize the significant the rises sharply as in the preliminary, and during the next 30 minutes taking the offered means.

Test 2

When receiving vodka at home (no limit dose) volunteers took composition (4 tablets of Lemontea", 2 tablets "Antionline" 3 g "effervescent composition to a glass of water) immediately before a meal or at the beginning of the feast. According to the agreement, each examinee was required to drink at least 300 ml of vodka. In the survey participated 10 healthy men aged 40-63 years who regularly consume alcoholic drinks (on average 1 to 2 times a week), but do not have the craving for alcohol and can be a long time to lead a sober lifestyle.

Marked changes are shown in tables 4 and 5.

Test 3

The same group, as in example 2, the same conditions the alcohol, but the reception compositions in the morning (8 tablets "Lemontea", 4 tablets of Antionline", 6 g "effervescent composition to a glass of water).

Marked changes are shown in tables 6 and 7.

As can be seen from examples 1-3, the composition Actionline" in example 1 of the most completely removes the harmful effects of alcohol, the composition according to example 2 is slightly worse, but more comfortable at the reception. Both compo is about equivalent.

1. The means for lowering the alcohol, the prevention and removal of alcohol intoxication and hangover, containing as active ingredient a component-based succinic acid, characterized in that an active substance further comprises at least one component on the basis of L-glutamic acid selected from the group consisting of L-glutamic acid, mono-L-glutaminate sodium, di-L-glutaminate sodium, mono-L-glutaminate ammonium, di-L-glutaminate ammonium, mono-L-glutaminate and potassium di-L-glutaminate potassium, at least one component based on fumaric acid selected from the group consisting of fumaric acid, monopolarity sodium, difumarat sodium, monopolarity ammonium, difumarat ammonium, monopolarity potassium, difumarat potassium, ascorbic acid and at least one energization selected from the group consisting of aspartic acid, sodium aspartate, glycine, one of the amino acid, sorbic acid, in addition, contains at least one sweetener selected from the group consisting of sucrose, glucose, sorbose, sorbitol, fructose, saccharin, aspartame, xylitol, sorbitol, the next time the specified number to the - 10 - 400

Component-based fumaric acid - 2 - 300

Ascorbic acid - 1 - 300

The sweetener and EnergyStar Up to 1000

2. Means under item 1, characterized in that as component-based succinic acid contains at least one salt of succinic acid (succinate), selected from the group consisting of mononucleate ammonium, disuccinate ammonium, monosaccate sodium, disuccinate sodium, monosaccate potassium, disuccinate potassium or a mixture thereof with succinic acid.

3. Means on one of the PP.1 and 2, characterized in that it further contains 20% of the amount of sodium bicarbonate, equimolar quantity of acids.

4. A tool according to any one of paragraphs.1 and 2, characterized in that it is a powder mix, or granulated mixture, or tablet, or capsule, or pills.

5. Means on p. 3, characterized in that it is a fizzy drink.

6. The way to reduce alcohol, prevention and removal of alcohol intoxication and hangover by introducing medicines, characterized in that as a drug use tool according to any one of the preceding paragraphs, suitable for adsto administered orally at least 30 minutes before drinking alcohol or while alcohol 1 - 2 tablets, or pills, or capsules, or one glass of fizzy drink.

8. The method according to one of paragraphs.6 and 7, characterized in that the tool is administered orally after drinking alcohol 1 - 4 tablets, or pills, or capsules, or 1 - 2 cups of fizzy drink.

 

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