Agent eliciting hepatoprotective and anti-encephalopathic property for reducing alcoholic intoxication, prophylaxis and removing alcoholic intoxication and withdrawal syndrome

FIELD: medicine, narcology.

SUBSTANCE: invention relates to hepatoprotective and anti-encephalopathic agent used for reducing alcoholic intoxication. Invention comprises components based on succinic, fumaric, glutamic acids and, additionally, at least one vitamin of B group. Agent can comprise additionally vegetable extracts or their mixture, L-carnitine, glycine, L-arginine, taurine and/or their mixture, methylsulfonylmethane, dihydroquercitin, dimethylsulfoxide or their mixture, nicotinamide or nicotinic acid or their mixture, energy source and sweetening agent. Also, invention proposes a method for reducing alcoholic intoxication, prophylaxis and removing withdrawal syndrome, liver protection, among them, in non-alcoholic intoxication and protection against encephalopathy. Invention provides described effects without qualifying medical control.

EFFECT: valuable medicinal properties of agent.

16 cl, 3 tbl

 

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, to reduce the craving for alcohol withdrawal encephalopathies, as well as hepatoprotector, including at pathologies not related to alcohol intake.

Intoxication and, especially, alcohol intoxication and subsequent hangover accompanied by the development of a number of severe subjective and objective 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 psychological, neurological and somatic in nature. Particularly noteworthy is the weight of the developing, and the systematic use of alcohol in transition in the chronic form of hepatitis and encephalopathy.

Acute alcohol intoxication and even more chronic alcoholism cause exacerbation of many chronic diseases associated with hormonal imbalance and what lublinie immunity, 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 failure and ischemia of organs. 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. Due to the fact that more than 90% of ethanol is oxidized in the liver and all the acetaldehyde is oxidized also the liver, the main toxic shock accepts this authority. In the case of the presence of characteristic lesions of the liver in the background of any chronic toxicity, including alcoholic cirrhosis of the liver. When the overload device acetyldihydrocodeine, especially among the Mongoloids, develops acetaldehyde poisoning, which leads to liver damage and brain damage. Finally, there is the fluidization of cell membranes, leading to violations the human processes of excitation, braking and transmission of nerve impulse breakdown of thermogenesis and sleep, as well as 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. In this case, because of adverse environmental conditions and low quality of life in childhood more than 30% of the population of Russia acquires various forms of liver disease. Hence clear the urgent need to find means to reduce and eliminate the effects of alcohol.

Today, the Arsenal of tools is rather limited. At the household level is first of all a hearty appetizer, that reduce 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 efficiency is the efficiency 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.

Currently, there is a biologically active food Supplement “Antipas” (trade mark “Antipolis” and “EN 21”)produced by the RF patent №2160589 from 20.12.2000, that solves the task and which is the closest analogue of the proposed tools. But it has significant drawbacks:

- due to the individual characteristics of metabolism helps only 70-75%;

- low effect in relation to the recovery of active detoxification functions of the liver;

- there is no measurable reduction encephalopathy, especially in developed alcohol withdrawal syndrome;

is not effectively eliminates developed a hangover.

We can conclude that to date, there are no available reinfusion drug or food Supplement that not only the rent problem associated with overdose of alcohol, but also effectively prevent the development of these problems before, during or after alcohol intake, while the effective protection of the liver and preventing or removing encephalopathy. This is especially important when using low-quality drinks or mixes vodka with beer, etc.

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 first problem to be solved by the present invention is to provide a food composition in the form of biologically active food supplements that are suitable to reduce the degree of alcohol intoxication, the prevention and removal of alcohol intoxication. The second task consists in reducing the development and elimination of pathological phenomena hangover. The third task is the ability to effectively influence additives before, during and after alcohol at home without qualified medical supervision. At the same time solves the problem of improving portability of alcohol. The fourth challenge is the increasing portability of a mixture of drinks. The fifth task is to increase the percentage of population that adequately responds to the action of the additive. The sixth task - improving the efficiency of actions in the face of alcohol online is Xocali and hangover, activation of the detoxification process of the body. The seventh goal is to protect the liver in case of any pathological effects, including alcohol. The eighth task - reduce severity of the symptoms of encephalopathy.

These problems are solved proposed tool designed to reduce alcohol, prevention and removal of alcohol intoxication and hangover, and prevent adverse effects on the liver and the brain that contains the components on the basis of succinic, fumaric and glutamic acid, and at least one component of the vitamin b group and a number of extracts and amino acids.

Compared with the closest analogue to the proposed remedy affects not less than 90% of people has a higher detoxification properties, capable of quickly enough to stop alcohol intoxication and alcohol withdrawal syndrome, is a highly effective hepatoprotector, not only during alcohol intoxication, but in any pathological effects on the liver, and is antianaphylactic means. In addition, the new structure can significantly increase the stability of the tool during storage, due to, including, with the exception of ascorbic acid.

It should be noted that the application of the described components separately, even in the ary doses did not lead to an equally noticeable effect.

According to the claimed invention, the means for lowering the alcohol, the prevention and removal of alcohol intoxication and hangover, and to prevent adverse effects on the liver and the brain contains as active ingredient in addition to the components on the basis of succinic, fumaric and glutamic acid, at least one vitamin b-group.

The tool can optionally contain

to 30.0 wt.% (in terms of dry extract) at least one extract of medicinal plants selected from the group of: an extract of schisandra (Schizandra Chinensis), Siberian ginseng (Eleutherococcus senticosus), sweet clover (Melilotus Officinalis), Rhodiola rosea (Rodiola rosea), ginseng (Pulanna schin-seng Nees) and/or their mixture;

up to 80 wt.% substance selected from the group: L-carnitine, glycine, L-arginine, taurine and/or their mixture;

up to 80 wt.% substance selected from the group: methylsulfonylmethane, dihydroquercetin, dimethylsulfoxide or a mixture thereof;

nicotinamide or nicotinic acid in who allowed amounts.

The tool may further comprise a component selected from sodium bicarbonate, sodium carbonate, potassium bicarbonate, potassium carbonate, ammonium bicarbonate, ammonium carbonate, or a mixture thereof in a quantity equimolar to the acid content.

The tool is a powder mixture, or granulated mixture, retabled, or capsule or pills.

Also the tool can be a drink or fizzy drink, while components can be diluted in juice or beverage, including carbonated.

The tool can optionally contain up to 1000 wt.% sweetener and EnergyStar and/or filler selected from the group of sucrose, glucose, sorbose, sorbitol, fructose, saccharin, aspartame, xylitol and other sweeteners, aspartic acid, aspartate, sodium, amino acids, sorbic acid, potato starch, corn starch and/or their mixture.

The tool can be used to reduce alcohol, prevention and removal of alcohol intoxication and hangover by oral administration before and/or during and/or after administration of alcohol in the form of a powder or granules, or tablets, or capsules, or pills, or drink or fizzy drink.

The tool is administered through the mouth, not later than one hour before receiving alcohol or while alcohol on 25-5000 mg of powder or granules, or 1-10 tablets, or pills, or capsules, or one glass of fizzy drink, and after drinking alcohol on 50-10000 mg of powder or granules, or 1-20 tablets, or pills, or capsules, or 1-3 cups of drink or fizzy drink.

All components are well studied and are standard components of food and pharmaceutical products the AI.

The following examples do not limit the invention, but merely illustrate it.

Example 1. (Nearest equivalent). Applied pill “ANTIPAS” 500 mg of the composition, 100 mg of succinic acid, 100 mg of mono-L-glutaminate sodium 37.5 mg fumaric acid, 25 mg of ascorbic acid and 237,5 mg glucose, corresponding to the patent of the Russian Federation 2160589.

Example 2. Used tablets offer a means of 1000 mg composition:

300 mg of succinic acid

200 mg of fumaric acid

200 mg of mono-L-glutaminate sodium

150 mg of taurine

50 mg of L-arginine

25 mg of L-carnitine

- 7 mg dry extract of schisandra

- 45 mg glycine

0.5 mg of vitamin B1

- 0.6 mg vitamin B2

- 0.6 mg vitamin B6

- 21,3 mg aspartame

Method of preparation - direct mixing with subsequent dry pressing.

Example 3. Used effervescent beverage containing a mixture of 3000 mg:

600 mg of succinic acid

400 mg of fumaric acid

400 mg of mono-L-glutaminate sodium

300 mg of taurine

100 mg of L-arginine

50 mg of L-carnitine

15 mg of the extract of schisandra

85 mg of glycine

0.5 mg of vitamin b 1

- 0.6 mg vitamin B2

- 0.6 mg vitamin B6

300 mg of ammonium bicarbonate

- 723,3 mg soda

25 mg of aspartame

The method of obtaining direct dry mixing to obtain a mixture in the mixer type “drunken barrel”. If necessary, the mixture is tabletirujut, or granularit, or Packed in powder form.

Example 4. Used tablets composition per 1000 mg of active start:

150 mg of potassium succinate

100 mg of fumaric acid

150 mg of a mixture of 2 parts of glutaminate sodium and 1 part glutamic acid

150 mg of taurine

25 mg of L-carnitine

25 mg of glycine

300 mg of sorbitol

- 0.2 mg vitamin B1

- 0.3 mg vitamin B6

- 99,5 mg of fructose

The mixture is produced by direct mixing, then moisturize to 10 wt.% and granularit. The obtained granules are dried, calibrate and obtain granules of medium weight, 100 mg of the Obtained granules dragonaut by the conventional methods.

Example 5. Used powder composition weight 1000 mg of active ingredients composition:

250 mg of ammonium succinate

200 mg fumarata ammonium

50 mg glutamic acid

200 mg of methylsulfonylmethane

150 mg of taurine

50 mg of L-carnitine

30 mg aspartame

0.5 mg of vitamin B1

0.8 mg vitamin B2

10 mg of a mixture of nicotinic acid and nicotinamide 1:1

- 8,7 mg of an extract of Rhodiola rosea

50 mg of glucose

The mixture is produced by direct mixing, then dissolved in grape juice prior to concentration of the mixture of 5% to 1 litre.

Example 6. Used capsule containing 400 mg of the composition according to example 5.

Example 7. Research proposed facilities was conducted in two stages: preclinical (inanimals) and clinical.

For the comparative test the effectiveness of the proposed means and the BAD TOGETHER, a study was conducted on rats male Wistar breed weighing 190-230 g

Test 1.

Initially each animal landed in an airtight exchange cell with a given flow of air, and within 5 minutes was going exhaled air for subsequent analysis on the content of endogenous CO2. Then each animal was administered intragastrically 2.5 ml of water, with the addition of 1 mg 13C-ethanol and 120 minutes were collected 8 air samples to determine the speed of the metabolism of injected ethanol to carbon dioxide labeled SO2. The isotopic composition was measured mass spectrometrically. The obtained data were normalized by the maximum value of the content SO2in the exhaled air. For each animal was based experimental curve using nonlinear regression Sigma-Raft was carried out the curve with the value of regression coefficient of at least 0,9967, and determined the parameters a, b, C from equation describing the curve excretion SO2depending on time t:

f=a· tb·e-ct

To illustrate the accuracy of the method will give the values for these parameters for one of the curve indicating the standard error of each parameter, the values of t for the T-test and p-level-is ereatest (in this case, the reliability) of the definition of each option:

a=0.7272; Art. error 0,1653; t=4,3985; p=0,0046

b=1.3195; Art. error 0,0842; t=15,6798; p<0,0001

C=0,0346; Art. error 0,0019; t=17,7988; p<0,0001

For further characteristics of the metabolism of ethanol for each animal used to be the most reliable parameter, has the sense of the rate of ethanol oxidation in animals: the higher the value, the higher the rate of metabolism of ethanol.

The next day the animal was introduced into the stomach of 2.5 ml of an aqueous solution containing ethanol from the calculation of 0.25 g per kg body weight and 1 mg 13C-ethanol (sample load). And again determined the dynamics of exhalation and excretion curve SO2for the subsequent calculation of felcini C.

Then the animals were divided into groups.

In the first group within 7 days, the animals received the intragastric ethanol based 2.5 g of ethanol per kg of body weight daily when the volume of the injected solution of 2.5 ml.

The second group was also sealed the animals within 7 days, but in a solution of ethanol was added BAD Antipolis rate of 200 mg per kg of body weight.

In other groups were also sealed the animals within 7 days, but in a solution of ethanol was added to the proposed composition (one song - one group) at the rate of 200 mg per kg of body weight.

After 7 days of repeated study, the above - metabolism of ethanol without load, and the next day repeated the experiments is of the metabolism of ethanol with the load.

The data obtained are summarized in table 1.

As can be seen from table 1, there is a substantial decrease of liver function on the background of chronic seal, however, when you receive funds in examples 2-6 liver function on the background of the ethanol load recovered completely and without load partially (30%to 60%), whereas Antipolis not have a significant impact.

Test 2.

When normal liver from the normal therapeutic dose geksenala introduced intraperitoneally, dogs sleep an average of 18-20 minutes. After double injection of 0.1 LD50 doses of chetyrehhodovogo carbon duration geksenalovy sleep increases by 2-3 times. This reduction detoxification functions of the liver holds about 1.5-2 months before the animal will not die. Two groups of rats were injected in the described dose of carbon tetrachloride, after which divided the animals into groups of 12 rats control on each sample group of 12 animals. In the experience of each of the examples of the reception of hepato started on the next day after administration of carbon tetrachloride at a dose of 25 mg/kg of body weight and the duration geksenalovy sleep was determined by the recovery of the liver after toxic hepatitis. As can be seen from table 2, in the control and after 21 days duration was on average of 53.2 min, for example 1, the situation is better, but only slightly, 44,2 Minprirody 2-6 show the high efficiency of the proposed hepatoprotector, fully restoring liver function. At the same time marked the recovery of animals in experiments in examples 2-6.

Test 3.

Isolated perfusely solution of Krebs-Henseleit (all salts, as in the blood plasma and 10 mm glucose) slice of the hippocampus of the rat brain were subjected to two types of damaging effects:

anoxic - by cessation of oxygen in the perfusion solution,

and toxic - by entering in the perfusion solution (12 mm) of ethanol and 0.1 mm acetaldehyde.

After 10 minutes of perfusion specified vozdeistvia caused suppression of 60% (average) electrical activity of the hippocampus slices. After 20 minutes "affecting perfusion was restored to the original composition of the perfusion solution and observed for 60 minutes, the kinetics of recovery of electrical activity. After anoxic exposure after 30 minutes was observed 90% recovery after toxic exposure 45-50 minutes was observed in 80% recovery of electrical activity.

When testing drugs for examples of the final drug concentration in the perfusion solution was 0.2% (on the basis that, when taking 2 g of the drug and dissolving it in 5 l of blood, the maximum concentration of drug in plasma when the hematocrit 40 can reach 0.5 to 0.6%). Anoxic impact on the background of the drug Antipolis caused 57% suppression, when the th activity of hippocampus slices, and toxic by 58% reduced aktivnosti slices. After restoring the original song (without drug Antionline without damaging vozdeistvii") after 30 minutes was not observed full recovery of slices of the hippocampus. With use of the preparations according to examples 2-6 anoxic exposure suppressed the electrical activity by 10%, and toxic 15-20%, while after 30 minutes after the impact of the drug there was a full recovery of the slices of the hippocampus, which shows distinct protivoepilepticheskih properties funds for examples 2-6.

Tests on groups of volunteers to assess the proposed compositions for objective efficiency

The tests were performed under the following conditions:

As the alcohol used high-quality vodka “Gzhelka” single party. When the alcohol in the home has permitted the admission of other alcoholic beverages according to individual preferences.

The evaluation was performed:

1) in 50 ml of vodka on an empty stomach (laboratory conditions)

2) when drinking at home no fixed minimum or maximum doses

3) when relieving hangover on the morning after the maximum possible intake of alcohol in the home.

In all studies, the wire is the very objective control status of the subject on the parameters of the dynamics of the rhythms of the electroencephalogram, electrocardiography, the volume of short-term and long-term memory, variational pulsometrii and ramachandiran.

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

When the trials used the pill “Antionline” (nearest equivalent) and the composition in the form of marketable products for examples.

Test 4.

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

a) preliminary acceptance for 60 minutes, turn each species compositions and without taking random days (2 tablets “Antionline”, 2 tablets or capsules of examples 3 g “effervescent composition to a glass of water) or 2 g of dry composition in the juice;

(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 the table 3 data, the inventive tool), the public contributed to the improvement objectively registered parameters of brain activity, including the improvement of short and long term memory, cardiovascular system, glucose homeostasis and ischemic changes, most commonly caused by alcohol. Detected positive changes characterize a significant decrease in the degree of intoxication by alcohol on an empty stomach, despite the fact that the rate of utilization of ethanol increases dramatically as in the preliminary and subsequent after 30 minutes of receiving the proposed tools.

Test 5.

When receiving vodka at home (no limit dose) volunteers took composition (4 tablets of Antionline”, 2 tablets, or capsules, or pills, or 3 g “effervescent composition to a glass of water, or 2 g of the composition in the juice for examples) immediately before a meal or at the beginning of the feast. According to the agreement each examinee had to drink at least 300 ml of vodka. In the survey participated 12 healthy men aged 35-65 years who regularly consume alcoholic drinks (on average 1-3 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 table 3.

Test 6.

The same group as in test 4, the same conditions the alcohol, but the reception compositions in the morning (6 tablets “Antionline”, 3 tablets, or 3 capsules, or 4 DRA is e, or 5 g “effervescent composition to a glass of water, or 3 g of the composition in the juice for examples).

Marked changes are shown in table 3.

For tests 4-6 characteristically, the volunteers noted a more rapid, soft and comfortable proposed compositions compared to Antiformalism. It was also noted that the day after drinking alcohol reaction was more confident, especially when driving.

As can be seen from the examples, the compositions of the present invention are most fully remove the harmful consequences of alcohol consumption. All songs are objectively stronger than composition “Antipolis”adopted as the nearest functional equivalent, with a pronounced hepatoprotective and antianaphylactic action.

1. The tool that has hepatoprotective and antianaphylactic properties designed to reduce alcohol, prevention and removal of alcohol intoxication and hangover, and prevent adverse effects on the liver, containing as active substances the STW components on the basis of amber, fumaric and glutamic acids, characterized in that it contains at least one vitamin b-group.

2. The tool according to claim 1, characterized in that it contains additionally up to 30.0 wt.% (in terms of dry extract) at least one extract of medicinal plants selected from the group of extract of schisandra, eleutherococci, clover, Rhodiola rosea, ginseng and/or their mixture.

3. The tool according to claim 1 or 2, characterized in that it contains additionally up to 80 wt.% substance selected from the group of L-carnitine, glycine, L-arginine, taurine and/or their mixture.

4. The tool according to claim 3, characterized in that it contains additionally up to 80 wt.% substance selected from the group methylsulfonylmethane, dihydroquercetin, dimethylsulfoxide or a mixture.

5. The tool according to claim 1 or 2, characterized in that it contains additionally nicotinamide or nicotinic acid, or their mixture.

6. The tool according to claim 3, characterized in that it contains additionally nicotinamide or nicotinic acid, or their mixture.

7. The tool according to claim 4, characterized in that it contains additionally nicotinamide or nicotinic acid, or their mixture.

8. The tool according to claim 1 or 2, characterized in that it is a powder mix, or granulated mixture, or tablet, or capsule, or pills, or drink.

9. The tool according to claim 4, or 6, or 7, characterized in that it is the way the second powder mixture, or granulated mixture, or tablet, or capsule, or pills, or drink.

10. The tool according to claim 9, characterized in that it is a fizzy drink.

11. The tool of claim 10, characterized in that it contains a component selected from sodium bicarbonate, sodium carbonate, potassium bicarbonate, potassium carbonate, ammonium bicarbonate, ammonium carbonate, or a mixture thereof in a quantity equimolar to the acid content.

12. The tool of claim 8, characterized in that it additionally contains up to 1000 wt.% sweetener and EnergyStar and/or filler selected from the group of sucrose, glucose, sorbose, sorbitol, fructose, saccharin, aspartame, xylitol and other sweeteners, aspartic acid, aspartate, sodium, amino acids, sorbic acid, potato starch, corn starch and/or their mixture.

13. The tool according to claim 9, characterized in that it additionally contains up to 1000 wt.% sweetener and EnergyStar and/or filler selected from the group of sucrose, glucose, sorbose, sorbitol, fructose, saccharin, aspartame, xylitol and other sweeteners, aspartic acid, aspartate, sodium, amino acids, sorbic acid, potato starch, corn starch and/or their mixture.

14. The method of protection, reduction of alcohol, prevention and removal of alcohol intoxication and hangover by introducing biological engineering is active funds characterized in that such a use of the tool according to any one of the preceding claims 1-13, suitable for use before and/or during and/or after alcohol.

15. The method according to 14, characterized in that the tool is inserted through the mouth at least an hour before drinking alcohol or while alcohol on 25-5000 mg of powder or granules, or 1-10 tablets, or pills, or capsules, or one glass of fizzy drink.

16. The method according to 14, characterized in that the tool is inserted through the mouth after drinking alcohol on 50-10000 mg of powder or granules, or 1-20 tablets, or pills, or capsules, or 1-3 cups of drink or fizzy drink.



 

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FIELD: organic chemistry, chemical technology.

SUBSTANCE: invention relates to an intermediate compound, i. e. tert.-butyl-(E)-(6-{2-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]-pyrimidine-5-yl}-(4R,6S)-2,2-dimethyl[1,3]dioxane-4-yl]acetate that can be used in synthesis of compound of the formula (IV)

eliciting inhibitory effect on activity of HMG-CoA-reductase and, therefore, can be used for preparing pharmaceutical agents for treatment, for example, hypercholesterolemia, hyperproteinemia and atherosclerosis. Also, invention relates to a method for preparing indicated intermediate compound by reaction of the new parent compound - diphenyl-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidine-5-ylmethyl]phosphine oxide with tert.-butyl-2-[(4R,6S)-6-formyl-2,2-dimethyl-1,3-dioxane-4-yl]acetate in the presence of a strong base in simple ether or aromatic solvents or their mixtures at temperature in the range from -200C to -900C. Also, invention relates to a method for preparing of compound of the formula (IV) wherein R1 means hydrogen atom or pharmaceutically acceptable cation and to a method for preparing intermediate compounds of the formula (VI):

wherein each P1 and P2 represents independently (C1-C4)-alkyl or group:

and wherein P3 represents (C1-C8)-alkyl. Applying new intermediate compounds and proposed methods provide enhancing quality and yield of compounds.

EFFECT: improved preparing methods.

9 cl, 1 tbl, 8 ex

The invention relates to new derivatives of 4-phenylpyrimidine and their pharmaceutically acceptable acid additive salts, which possess the properties of receptor antagonists neirokinina(NK-1), and can be used to treat diseases, oposredstvovanii NK-1 receptor, for example, headache, Alzheimer's disease, multiple sclerosis, cardiovascular changes, oedema, chronic inflammatory diseases and so on

The invention relates to new compounds of the formula (I)

in which Ar1means pyrazole which may be substituted by one or more groups R1, R2or R3; Ar2means naphthyl, tetrahydronaphthyl, each of which is optionally substituted by 0-1 groups R2; X means5-C8cycloalkenyl, phenyl, optionally substituted by a hydroxy-group or1-C4alkoxygroup, furan, pyridinoyl, pyrazolyl, pyridinyl, optionally substituted by a hydroxy-group or1-C4alkoxygroup, piperidinyl; Y represents a bond or a saturated branched or unbranched1-C4the carbon chain, with one methylene group is optionally replaced with NH, or and Y is optionally independently substituted by oxopropoxy; Z means morpholine, group, pyridinyl, furanyl, tetrahydrofuranyl, thiomorpholine, pentamethylbenzene, pentamethylbenzene, secondary or tertiary amine, the nitrogen atom of the amino group covalently linked to the following groups selected from a range that includes the C1-C3alkyl and C1-C5alkoxyalkyl; R1means31-C6alkyl which is optionally partially or fully galogenidov, halogen; R3means phenyl, pyrimidinyl, pyrazolyl, which is substituted by one branched or unbranched1-C6the alkyl, and pyridinyl, optionally substituted C1-C3alkoxygroup or amino group, W denotes O and its pharmaceutically acceptable salts

The invention relates to the field of pharmaceutical industry and relates to solid dosage forms of drugs that have a protective effect against the development of atherosclerosis and coronary heart disease, and is effective for the treatment of benign prostatic hyperplasia

FIELD: medicine, pharmacy.

SUBSTANCE: invention proposes an agent for removing the post-narcosis depression after combined anesthetic assistances with applying sedative and narcotic preparations. As such agent the preparation "Reamberin" is used based on succinic acid that is a natural metabolite in human body. The preparation provides reducing time for adequate spontaneous breathing and awaking time by 1.5-fold and the absence of complications and negative adverse responses.

EFFECT: valuable properties of agent.

4 dwg, 3 ex

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