Means for reducing unfavorable consequences of acute alcohol intoxication

FIELD: medicine.

SUBSTANCE: means comprises amber acid and/or its salts, fructose, dry extraction of Saint John's wort, magnesium ion sources, potassium ion sources as active bases and auxiliary substances, carriers and/or fillers when needed.

EFFECT: enhanced effectiveness of treatment.

4 cl, 4 tbl

 

The invention relates to the field of creation of medicines, can reduce the adverse effects of acute alcohol intoxication-symptoms postintoksikatinom alcohol syndrome.

Alcohol abuse is a significant part of the population causes a whole range of social and medical problems. Excessive one-time intake of alcoholic beverages can lead to acute poisoning, the development of toxic encephalopathy and coma. However, such effects are observed less frequently, and the problem of cultural and moderate consumption of alcoholic beverages is primarily social in nature.

On the other hand, with increase of the dose of alcohol increases the concentration in the blood is the main product of the metabolism of ethanol is acetaldehyde, the accumulation of which leads to disruption of the functioning of all organs and body systems. It is well known that the most adverse effects of alcoholic excess appear in the hangover, when developed postintoksikatinom alcohol syndrome. The weakening of, removal or prevention of pathological manifestations postintoksikatinom alcohol syndrome is already full medical problem.

Development postintoksikatinom alcohol syndrome leads to pathologic the civil consequences and conditions of discomfort, occur after intoxication in persons as suffering from alcoholism, and not suffering from this disease.

To eliminate unpleasant subjective manifestations postintoksikatinom alcohol syndrome at the household level have long used the juices, kvass, marinades, fruit drinks, and other food liquids and beverages, contributing partial detoxification of the body and fill fluid loss as a result of dehydration.

Developed and proposed a series of drugs, not only eliminating or decreasing the discomfort in patients hangover, but also reduces the toxic manifestations of acetaldehyde.

One of the first in this series is the product Alka-Seltzer, containing as active principle acetylsalicylic acid [Leaflet to medicine Alka-Seltzer, manufactured by Miles, England]. This drug, in particular, reduces the phenomenon of swelling of the plasma membranes of blood vessels, lowers intracranial pressure contributes to the weakening of hypoxia, reduces the headache.

Described pharmaceutical preparation containing acetylsalicylic acid, aspirin, caffeine-sodium benzoate, aminophylline, sodium bicarbonate, citric acid and sucrose. The drug has the ability to ease symptoms postintoksikatinom alcohol syndrome, including n maliseet basic functions of the body, impaired by alcohol excess, leading to an objective improvement in General condition and subjective sensations of the patient [RF Patent 2123845 And 61 To 31/22, 1998].

Known non-pharmacological means “Amethyst”, containing Apple juice, glycerin, aqueous extract of sage, choline and mineral salts [RF Patent 2005391, And 23 L 2/00, 1994]. Drink eliminates feelings of weakness, thirst, fatigue, helps to eliminate cardiac abnormalities, swelling of the face, normalizes sleep [VP, Tezikov E.B., assumption AU Amethyst is a new non-pharmacological treatment for postintoksikatinom alcohol syndrome. The addiction issues. - 1995. No. 4. - C.22-27].

As a means of decreasing the severity of postintoksikatinom alcohol syndrome, the recommended sodium salt of [poly-(2,5-dihydroxy-phenylene)]-4-thiosulfonate, which prevents full-scale development postintoksikatinom disorders and pathological changes in organs and tissues, in particular actively reduces the severity of the syndrome of ethanol, has a hepatoprotective effect manifests antihypoxic activity [RF Patent 2177320 And 61 To 31/765, 2000].

For the prevention and treatment of ketosis is one of the manifestations postintoksikatinom alcohol syndrome, the recommended tool comprising sodium salt of [poly-(2,dihydroxy-phenylene)]-4-thiosulfonate, an aqueous solution of glycerin and magnesium [Application for the grant of a patent of the Russian Federation 2001-106.199/14 And 61 To 31/185, 2001].

Patented pharmaceutical composition comprising succinic acid and citric acid, applicable to the treatment postintoksikatinom alcohol syndrome. The composition has a toxic effect, increasing the excretion of alcohol from the body, shows the antihypoxic effect, improves the General condition, normalizes sleep. The drug should be taken 3-5 times a day at the rate of 3-5 mg/kg body weight [RF Patent 2039556, a 61 K 31/19, 1995]. It should be noted that this song is most rational to apply to development postintoksikatinom alcohol syndrome, because the development of this condition the activation of the process of elimination of alcohol already is not significant.

Formally closest to the proposed invention can be recognized as a means to reduce alcohol, prevention and removal of alcohol intoxication and hangover, having the following composition:

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 1-300 mg

The sweetener and energization to 1000 mg.

As a component-based succinic acid can be ispolzovanie - or di-substituted sodium, ammonium or potassium salts of succinic acid or a mixture of salt with succinic acid.

As component on the basis of L-glutamic acid can be used L-glutamic acid, mono - or di-substituted sodium, ammonium or potassium salts of L-glutamic acid.

As components on the basis of fumaric acid can be used fumaric acid, mono - or di-substituted sodium, ammonium or potassium salts of fumaric acid.

As EnergyStar can be used aspartic acid, sodium aspartate, glycine, one of the amino acid, sorbic acid.

As a sweetener can be used sucrose, glucose, sorbose, fructose, saccharin, aspartame, xylitol, sorbitol.

The tool can be used before and/or during and/or after alcohol.

The use of this tool leads to an increase in the rate of utilization of ethanol, to reduce the degree of intoxication by alcohol, to improve the subjective and the objective condition of the patients. This tool, therefore, reduces both narcotic and toxic effects of ethanol and toxic effects of acetaldehyde [RF Patent 2160589 And 61 To 31/375, 2000].

The procedure is aimed at speeding up the metabolism of ethanol, which, as follows from the description of the image is the shadow, “removes the harmful consequences of alcohol consumption” (hangover), and the consequences of postintoksikatinom alcohol syndrome, caused by toxic effects of acetaldehyde. In the specified approval there is a contradiction, since we know that the increase in the rate of ethanol oxidation is accompanied by increased production of acetaldehyde, which determines the severity postintoksikatinom disorders.

To solve the first problem, this tool includes additional sources of energy, which should contribute to the promotion of the process of degradation of ethanol.

For the second objective, it includes succinic acid and/or its salts, which are specific antidotes against acetaldehyde, which together with fumaric acid and/or its salts provide a powerful and time-stretched antihypoxic effect.

Despite the data on a sufficiently high efficiency of action of the drug, it cannot be considered ideal.

As shown by studies of the applicant, the content of components on the basis of succinic and fumaric acids in a known means (10-400 mg of each in 1000 mg of funds) is not enough for the most pronounced suppression postintoksikatinom complications of alcoholic excess.

As one of the active principles are described by means of COI is lsout L-glutamic acid or its salt, related to high-performance energization actively accelerating the process of utilization of ethanol. However, there is an extensive range of scientific publications, questioning the safety of using glutamate (monosodium salt of glutamic acid).

There is information about the adverse effect of glutamate on sight. In particular, it is noted that long-term consumption of excess glutamate sodium with food leads to an increase in the concentration of glutamate in the vitreous body and can cause the destruction of cells in the retina [Ohguro H. et al. A high dietary intake of sodium glutamate as flavoring (ajinomoto) causes gross changes in retinal morphology and function. Exp Eye Res 2002 Sep; 75 (3): 307].

A number of articles shows the adverse effects of glutamate in the Central nervous system. Specifies, for example, that the monosodium salt of glutamic acid in mice causes brain lesions, obesity and other disorders [Olney J.W. Brain lesions obesity, and other disturbances in mice treated with monosodium glutamate. Science 164:719-721, 1969].

Noted: the negative impact of the monosodium salt of glutamic acid on the reproductive function [Pizzi W.J., bārnhart J.E., and Fanslow D.J. Monosodium glutamate administration to the newborn reduces reproductive ability in female and male mice. Science 196:452-454, 1977]; its ability to induce seizures [Jonson GAR Convulsions induced in 10-day-old rats by intraperitoneal injection of monosodium glutamate and related excitant amino acids. Biochem Pharmacol 22:137-140, 1973]; and asthmatic symptoms [Alien D.H., Delohery J. G. Baker, Monosodium L-glutamate-induced asthma. J Allergy Clin Immunol 80: 530-537].

On the Internet on the website WWW.truthinlabeling.org lists about 150 references to scientific publications, showing not the safe use of the monosodium salt of glutamic acid.

Even if we assume that the presence of monosodium salt of glutamic acid and related compounds in the tool for the reduction of alcohol and its consequences for the occasional admission that products containing very low amounts of these compounds that will not cause adverse effects, the mere presence of glutamates this tool can alert consumers and encourage them to stop using it. Given these circumstances, and the absence of rigorous proofs of security the use of moderate doses of glutamate, their presence in the composition of the pharmaceutical compositions and dietary supplements should recognize spam.

From the description of the well-known inventions, it follows that present in the composition known means to sugar substitutes is given the additional function of energization, the main active components they do not belong and are used as fillers.

However, related to sweeteners: sucrose, glucose, sorbose, sorbitol, fructose, saccharin, aspartame, xylitol, not all are biologically inert the mi substances.

Thus, the introduction of the tools designed to mitigate toxic complications caused by acetaldehyde, glucose is very undesirable. After alcoholic kurtosis has been a violation of carbohydrate metabolism. Against this background, the extra glucose can after short-term hyperglycemia (due to additional portions of glucose) to cause reactive hypoglycemia with all its negative manifestations, until he lost consciousness [Guide addiction. M., 2002, Vol. 2, pp.118, T.1, s.89].

On the contrary, the inclusion of such amounts of fructose increases detoxification effect as fructose, on the one hand, is able to prevent in the hangover period, the development of reactive hypoglycemia in healthy people and, on the other hand, the development of reactive hyperglycemia in patients with diabetes.

Included in the known tool analizatory promote a more energetic utilization of ethanol, providing a lower level of alcohol intoxication. At the same time, the intensification of metabolism of ethanol may lead to more rapid accumulation in the blood of acetaldehyde, causing accelerated onset phenomena postintoksikatinom alcohol syndrome.

Ascorbic acid in the composition known means performs the role of an active antioxid the NTA. However, in the accepted concentrations (1-300 mg/1000 mg of the drug) at the organism level of ascorbic acid shows little antihypoxic action that could serve as an argument for its inclusion in the means of reducing the toxicity of ethanol and acetaldehyde.

The present invention is to reduce the adverse effects of alcoholic excess due to the increased activity of the funds aimed at weakening the severity postintoksikatinom alcohol syndrome arising from excessive alcohol consumption.

This object is achieved in that the proposed product contains dry extract of St. John's wort (Hypericum), sources of magnesium and potassium, fructose, succinic and fumaric acid and/or their salts, and optionally excipients, carriers and fillers.

When creating a pharmaceutical composition, it may contain the active agent of the following composition (per dose)in mg:

succinic acid and/or its salt 4,0-1000,0

fumaric acid and/or its salt 3,0-800,0

fructose 10,0-500,0

the dry extract of the herb of Hypericum perforatum

(Hypericum perforatum L.) 50,0-1000,0

the source of magnesium ions,

providing the content of Mg++0,3-150,0

the source of potassium ions,

providing the content of ions To+3,0-300,0

and, if necessary the spine physiologically acceptable(s), the carrier and/or excipient and excipient in the required quantities.

Sources of magnesium ions and potassium partially and completely, if necessary are the corresponding salts of succinic and fumaric acids.

Tool used before alcohol consumption during their use or after alcoholic excess.

The advantage gained from the use of the present invention is to enhance therapeutic action of the proposed means to reduce the adverse effects of acute alcohol intoxication.

The basic idea underlying the present invention is to create a composition of active principles, with a high potential elimination or attenuation of the toxic effects caused by acetaldehyde, and at the same time minimizing the impact on the initial phase of the metabolism of ethanol to acetaldehyde.

To reduce the adverse effects of acute alcohol intoxication means includes, as active principles of connection, more actively eliminating or weakening the main manifestations of the toxic effects of acetaldehyde, and, in contrast to the known means of similar composition contains no additional sources of energy, stimulating the transformation of ethanol into acetaldehyde.

The difference of the means from the well-known is another functional activity, in other principesaudi and substantial difference in composition.

Selection of the listed active ingredients proposed facilities was determined inherent in each of them biological and functional activity, cumulatively and synergistically providing the desired tool's efficiency. In particular, consideration was given to the following:

succinic acid and its metabolic buffer - fumaric acid are the Central participants of the tricarboxylic acid cycle, and adding them contributes to a more effective functioning of this cycle in the presence of ethanol and acetaldehyde [Kosenko E.A., Kaminsky OUT Carbohydrate metabolism, liver and alcohol. - Pushchino, 1988. - 150 S.]. Found that the effective content of succinic and fumaric acid in a dose of total funds should be increased to 300-1000 mg;

fructose is able to adjust and normalize the metabolism, impaired by alcohol excess, and, due to their ability to provide antiketogenic effect [Kryshen PF, Rates NI Sorbitol, xylitol, glycerol and their application in medicine. - Kiev, 1979. - 326 S.], in contrast to glucose and sucrose, has no negative effect on carbohydrate metabolism during alcohol intoxication and postintoksikatinom period;

the dry extract of the herb St. John's wort herb (Hypericum perforatum L.), as shown by the study authors, showed itself as an active means weakening ol the phenomenon postintoksikatinom alcohol syndrome;

sources of ions of Mg++and+restore disturbed by alcoholic excess salt and water balance and prevent the development of disorders of the Central nervous system, skeletal muscles and myocardium, due to a change in the excitability of the cell structures [C. Wright, Talbott J.D. The use of carbohydrate-electrolyte supplements in residential treatment of chemical dependence. // J.Psychoact. Drugs. - 1988. - V.20, No. 3. - P.337-348; Harris R.A. Metabolism of calcium and magnesium during ethanol intoxication and withdrawal. // In: Biochemistry and pharmacology of ethanol. Ed. E.Majchromier, E.P.Noble, Plenum Press, N.-Y.-L, 1979, V.2, P.27-41].

The combination of these active ingredients ensures the elimination of a wider range of symptoms postintoksikatinom alcohol syndrome than it is able to make each of your connections separately.

As salts of succinic and fumaric acids can be used any water-soluble salt.

As sources of ions of Mg++and+can be used water-soluble salts of magnesium and potassium which are all non-toxic acids. Especially, it is advisable to use the corresponding salts of succinic and fumaric acids. If the content of magnesium and potassium salts of succinic and fumaric acids is insufficient to provide the desired concentration of ions of Mg++and+their deficiency can be compensated by adding these salts of other acids.

p> As the dry extract of the herb St. John's wort herb (Hypericum perforatum L.) or other species of Hypericum (Hypericum sp.) can be used condensed alcohol, water, carbon dioxide and received by other extracts, but preferred the dry aqueous extract.

The optimum content of the dry extract of St. John's wort dose of the proposed tools is 50-1000 mg

The product can be standardized to hypericin content as described, for example, H.L. Kim, L. Streltzer, Goebert D. [St. John's wort for depression: a meta-analysis of well-defined clinical trials. J. Nerv. Ment. Dis., 1999, 187: 532-538].

The herb St. John's wort is one of the oldest traditional medicines, and in the official medicine is used for preparing decoctions and tinctures. Decoctions and infusions prescribed for internal use, as an astringent and antiseptic, and to rinse in dental practice [Mashkovsky PPM Medicines. M, “Medicine”, 1988, Vol.2, s].

The surge of interest in recent years to drugs on the basis of the herb Hypericum perforatum due to the establishment they have antidepressant activity.

In particular, clinical studies have shown that the effect of St. John's wort preparations is comparable to the effect of low doses of tricyclic antidepressants, but the frequency of side effects was twice lower [H.L. Kim, L. Streltzer, Goebert D. St.John''s wort for depressio: a meta-analysis of well-defined clinical trials. J. Nerv. Ment. Dis., 1999, 187: 532-538].

For most cases, so-called minor or moderate depression effective doses based ethanol or methanol extract of the herb St. John's wort was 600-900 mg tablets extract with standard (0,3%) content of hypericin [Kasper, S., Schuiz V. Johanisskraut-Extract als pflanzliches Antidepressivum. Schweiz Rundsch Med-Prax, 2000 Dec 21, Vol.89 (51-52), pp.2169-77].

These data consistently confirmed in later surveys related to the clinical efficacy of St. John's wort, when the antidepressant activity States according to the generally accepted standardized international tests [e.g. Whiskey E., Wemeke U., Taylor D. A systematic review and meta-analysis of Hypericum perforatum in depression: a comprehensive clinical review. Int. Clin. Psychopharmacol. 2001 Sep, 16 (5): 239-52].

Almost all of these drugs are produced on the basis of extracts obtained with organic solvents (ethanol or methanol). Water extracts and preparations based on them are considered to be less effective antidepressant [Katzenstein L. St. John's Wort against depression, or the secrets of the herbs of St. John the Baptist. M, crown Press, 1998].

In parallel with the antidepressant activity of extracts of Hypericum in a series of publications have shown that these extracts reduce alcohol consumption in alcohol-preferring” lines of experimental animals under conditions of free choice ALCO is Olya, or water, that is the basis for further research in creating treatments for alcoholism [e.g., Roby CA, Andersen G.D., E. Kantor, Dryer D.A., Burstein A.H. St. Jon's wort effect on CYP3A4 activity. Clin. Pharmacol. Ther, 2000, 67: 451-457].

Reduction of alcohol consumption in alcohol-preferring” rats” took place when using the methanol extract of the herb of Hypericum perforatum, and when applying the extract obtained using liquefied carbon dioxide [Perfumi M, Panocka I., Ciccociopp R., Vitali D., Froldi R., Massi M. Effects of methanolic extract and a hyperforin-enriched CO2extract of Hypericum perforatum on alcohol intake in rats. Alcohol Alcohol, 2001 May-Jun, 36 (3): 199-206].

Such behavior could be explained by the fact that “alcohol-preferring animals special lines have genetic disorders and are in a state of permanent depressivnopodobnogo status and alcohol is a means of mitigating this condition. The antidepressant action of Hypericum extract reduces the need for animals in alcohol.

On the other hand, it is noted that the antidepressant action of extracts of Hypericum, which is manifested only after the re-assignment of Hypericum extract, and reduction of alcohol consumption in alcohol-preferring” rats observed after a single intragastric reception are independent effects, not rigidly connected to each friend is m [Perfumi M., Ciccocioppo R, Angeletti, S., M. Cucculelli, Massi M. Effects of Hypericum perforatum extraction on alcohol intake in Marchigian Sardinian alcohol-preferring rats. Alcohol Alcohol, 1999 Sep-Oct, 34 (5): 690-698].

It is also known that aqueous extract of the herb St. John's wort in experiment shows: radioprotective (prophylactic and therapeutic) action, that is, protects against radiation damage to the bone marrow and small intestine; causes nonspecific amplification factors of the immune system; reduces the duration of alcoholic coma, that is, has a sobering effect of acute alcohol poisoning [Dobrovolsky YU., Diordiychuk CENTURIES, Voitenko CENTURIES, Kornienko T.N., Lipkan GN. A sobering effect of aqueous extract of Hypericum perforatum for acute alcohol poisoning. 2nd national conference on medical botany. Kiev, 1988, s-348].

Found that a decoction of the herb St. John's wort can have a sobering effect with alcohol and to reduce the time regression withdrawal syndrome [Ed. Mon. The USSR 1795581, a 61 K 35/78, 1990].

Proposed in the present invention means described composition is intended for oral administration and can be prepared in the form of conventional pharmaceutical forms, such as powders, granules, tablets, encapsulated drugs, pills, solutions, including, in the form of solid dosage forms, dissolution in water which is accompanied by what gazoobrazovaniem. This tool can be made as a medicine or as a dietary Supplement.

A single dose of the proposed tools can be contained in a single unit dosage form (for example, in one powder) or may consist of multiple units of the dosage form (for example, can be divided into 2-4 tablets that should be taken simultaneously).

A valid use of the proposed tools in the form of candles with appropriate adjustment of the dose of active principles.

For the preparation of specific pharmaceutical forms can be used the necessary auxiliary substances in the required quantities.

The proposed tool can be used before alcohol consumption during their use or after alcoholic excess. Increasing the period of time from completion of alcoholic excess and to receive funds reduces its effectiveness. Optimal reception is offered funds during, directly after the completion of alcoholic excess, or shortly thereafter.

All the active ingredients of the proposed remedies do not have side effects, and the tool may in highly expressed manifestations postintoksikatinom alcohol syndrome be taken again.

The effectiveness of the proposed tools, syrause what about the adverse effects postintoksikatinom alcohol syndrome, confirmed, in particular, the following Examples only illustrate the practicability of the invention and its advantages, and may not be considered limiting.

EXAMPLE 1.

In the experiment on animals evaluated the impact of the proposed funds, some funds for the Patent of the Russian Federation 2160589 and dry aqueous extract of Hypericum perforatum on the severity postintoksikatinom condition caused by acute alcohol intoxication.

Postintoksikatinom condition was modeled recommended method [V.P. et al. assessed the severity postintoksikatinom state, provoked acute alcoholic intoxication in the experiment on animals. // Science news and technology. VINITI. Series Medicine. Vol. Alcoholic disease. - 2000. No. 7. - P.1-6].

The study were subjected to:

Sample 1: the proposed tool (composition)containing:

succinic acid 0.4 mg; fumaric acid 0.3 mg; fructose - 0.45 mg; extract of Hypericum perforatum - 50.0 mg; potassium chloride and 0.40 mg; magnesium sulfate hydrogenated to 0.3 mg.

Sample 2: a well-known composition comprising: succinic acid 400 mg; L-glutamic acid - 400 mg; fumaric acid 300 mg; ascorbic acid 300 mg; aspartic acid 40 mg; glucose - 455 mg.

Sample 3: Hypericum extract containing dry aqueous extract of zveroboj the perforated - 500 mg

All samples immediately before the experience was dissolved in 36 ml of water.

Rats male Wistar per day to experience coached at the "spinning rod" and then were subjected to initial testing. After one day of pre-starving for 9 hours the rats were introduced into the stomach of a 30%solution of ethanol in a dose of 6 g/kg After 12 hours after administration of ethanol was administered intragastrically 3 ml of water (group 1) or 3 ml of a solution containing the Sample 1 (group 2), or 3 ml of a solution containing Sample 2 (group 3), or 3 ml of a solution containing the Sample 3 (4th group). Animals of the control group (5) instead of ethanol intragastrically injected equiano amount of water and after 12 hours - 3 ml of water. The number of animals in each group of 12 individuals. After 17-18 hours after administration of ethanol or water, the condition of the animals was evaluated using a test “spinning rod”. The results of the study are presented in Table 1.

The obtained results show that the retention time on the rotating rod control animals increases, and rats exposed to ethanol - reduced. Sample 2 (known composition according to the Patent of the Russian Federation 2160589), and Sample 3 (Hypericum extract) were equally likely to have increased retention time on the rod rats exposed to alcohol. However, Sample 1 (PR is degema composition) had a significantly stronger positive effect.

EXAMPLE 2.

The study was performed on 12 healthy subjects were volunteers aged 20-26 years. Study design: an open cross-sectional study with the inclusion of the control group. Subjects were alternately been proposed composition (Sample 1), a well-known composition according to the Patent of the Russian Federation 2160589 (Sample 2), St. John's wort extract (Sample 3) and placebo (control).

Sample 1: the proposed composition containing succinic acid - 900 mg; fumaric acid 300 mg; fructose - 300 mg; extract of St. John's wort 300 mg; potassium chloride 300 mg; magnesium sulfate hydrogenated - 150 mg

Sample 2: known composition containing succinic acid 400 mg; L-glutamic acid - 400 mg; fumaric acid 300 mg; ascorbic acid 40 mg; aspartic acid - 300 mg; glucose - 455 mg.

Sample 3: Hypericum extract containing dry aqueous extract of Hypericum perforatum - 500 mg, starch (filler) - 800 mg xylitol (flavoring) - 50 mg, sodium chloride (flavoring) - 50 mg, and a powder mass of 1400 mg

The placebo used a powder mass of 1400 mg, representing starch (1300 mg) with the addition of flavorings in the form of xylitol (50 mg) and sodium chloride (50 mg).

Just spent four cycles of research. Each subject participated in research with an interval of 3-4 days. On sledovatelnot inclusion of subjects in the different cycles of the studies differed. On the morning of the study, subjects were exposed to the source of psychophysiological research. 17.00-18.30 the same day they ate metered quantity of alcohol in the form of vodka at a dose of 1.45 g/kg and standardized components and the number of dinner. At 21.00, before going to sleep each of the subjects received in one cycle research powder placebo, in another cycle of research - sample 1, in the third Sample 2 and the fourth Sample 3 with a small amount of water. The next morning, at 7.30 subjects repeatedly been used before placebo or Sample 1, Sample 2 or Sample 3 with a small amount of water. 9.30-11.00 morning after Breakfast, subjects were exposed to psycho-physiological testing and completed the survey, which recorded their own sense of characterizing the severity postintoksikatinom state (hangover).

Psychophysiological testing included the following methods: check tremor brush of the right hand (the ability to hold the metal pin in the narrow metal glass without touching the walls of the latter), simple visual-motor reaction time complex visuo-motor reaction (choice reaction to visual stimulus), short-term (operational) memory (digits), and the ability to switch attention (to the ACLs-black table Schulte-Platonov).

Used in the study questionnaire was a standard questionnaire “PASS” (postintoksikatinom alcohol syndrome) [rapid diagnosis (screening) chronic alcohol intoxicatie in patients with somatic profile. Ministry of health guidelines of the Russian Federation No. 99/174. - M - 2001].

The results of the study are presented in Tables 2 and 3.

From Table 2 it follows that the subjects on the background of placebo in postintoksikatinom a period of four tests significantly (statistically) deteriorated indicators of their psychophysiological state. The exception was only the indicator “simple reaction time”. On the background of the Sample 1 reactions of subjects enrolled in postintoksikatinom period, were not statistically different from similar reactions recorded during initial testing all tests and were significantly better than the control. On the background of the Sample 2 reactions of the subjects were significantly worse than during the initial testing. For example, in the three tests they were statistically significantly different from those in the original testing. On the background of the Sample 3 noted a definite improvement in the ability of subjects to perform the proposed tests. This is evidenced by the absence of statistically significant differences with the figures recorded during the original testing you during the filling up of the three tests.

From Table 3 it follows that the subjects, on the background of placebo, and Samples 1, 2 and 3, experienced subjectively unpleasant sensation, typical of the state of hangover weak degree. Most often these feelings were recorded on the background of a placebo, at least - on the background Samples 2 and 3. Most often these feelings occurred in subjects on the background of the Sample 1. Moreover, on the background of the Sample 1 in subjects lacked such manifestations postintoksikatinom status as “nervous tension, anxiety and excitement”, “lack of appetite” and “facial flushing”. On the contrary, on the background of the Sample 2, as well as on the background of the placebo, these manifestations were recorded. On the background of the Sample 3, as well as on the background of the Sample 1, there was no such manifestations as “nervous tension and anxiety and excitement.” It should be noted that Sample 1, compared with Sample 2, weakened such manifestations hangover state, as excessive thirst, malaise and fatigue, dry mouth, and trembling of the fingers” (specified symptoms on the background of the Sample 1 was rarer).

EXAMPLE 3.

Nine healthy male volunteers aged 29-48 years were offered at home to experience the effect of the proposed composition (Sample 1), a famous song by the Patent RF 2160589 (Sample 2) and placebo (control).IN one of the important conditions of the experiment were asked to perform tests in maximum standardized by the amount of alcohol consumed and snacks conditions.

Sample 1: the proposed tool (composition)containing succinic acid 150 mg; fumaric acid 50 mg; fructose - 50 mg; dry aqueous extract of Hypericum perforatum - 50 mg; potassium chloride 50 mg; magnesium sulfate hydrogenated 30 mg, and represents a tablet weight of 380 mg.

Sample 2: a known composition containing succinic acid 400 mg; L-glutamic acid - 300 mg; fumaric acid 300 mg; ascorbic acid 200 mg; glucose - 400 mg; starch - 400 mg, and represents a tablet weight of 2000 mg

The placebo used a tablet weight of 2000 mg containing starch with added flavouring ingredients: xylitol (75 mg) and sodium chloride (75 mg).

During one of the friendly parties (first cycle studies) part of the subjects took one tablet of placebo at bedtime for another pill placebo, and in the morning, immediately after waking up for another tablet. Another part of the subjects in the same time intervals took tablets containing the Sample 1, and the third part of the subjects took tablets containing the Sample 2. During the second and third rounds of tests conducted under similar conditions, the subjects changed tablets placebo tablets with the Sample 1 or Sample 2, or Vice versa, so that all nine people had experienced all three types of tablets.

Alcohol is the first drink, used in all three cycles of the test consisted of vodka in the number of 350-700 ml for the evening. The burden of alcohol ranged from 1.5-2.0 g/kg and slightly differed in the same subjects in different test cycles. Snack on its composition and the number was about the same.

The next day, after every meal, subjects were briefly described their health and completed the form, where noted their sensations (symptoms). The questionnaire contains 35 questions. A positive response to each of the contained questions was estimated at one point. The amount of points used to characterize the severity of experienced subjects postintoksikatinom state. The results of the observations are summarized in table 4.

From Table 4 it follows that the Sample 2 is about 25% weakening of the state hangover in subjects (statistically significant differences from placebo are not available). On the contrary, Sample 1 two times (statistically significantly) reduces the severity of the manifestations of the condition of a hangover.

The effectiveness of the proposed tools is determined by the interaction of all its active components, the choice of which of the large number of known biologically active compounds, theoretically potentially suitable for attenuating postintoksikatinom alcohol syndrome, it has not been obvious. Sovocool the active principles of the proposed tool has not been previously described and used. Fame all began active proposed facilities, including their use in compositions known means for the attenuation of alcohol and its consequences, does not disprove the original proposal.



Table 1

The retention time of rats in the test “spinning rod
Groups of animals NNIndicators (M±S.D.)
 Retention time in the initial test (s)The change in Retention time of rats with repeated testing (Δs)
N 1 (ethanol + water)227±92-97±641
N 2 (ethanol + sample N 1)240±118+67±741,2,3,4
N 3 (ethanol + sample N 2)252±88-22±571,5
N 4 (ethanol + sample N 3)231±77-17±611,5
N 5 (control)244±111+163±71
Note:1- p<0,001 compared to the 5-th group;

2- p<0,001 compared to the 1st group;

3- p<0,01 compared to the 3-rd group;

4- p<0.05 when avanyu 4-th group; < / br>
5- p<0,01 compared to the 1st group;





Table 2

Psychophysiological indicators of subjects Placebo
TestsInitial testingTesting during posthistorical
 MS.D.MS.D.P
Red-black table, 115,036,674,243,20,033
The simple reaction time, MS241,532,2211,235,90,106
The reaction time choice, MS316,360,3400,355,60,040
Tremor, time/s2,70,61,80,60,024
Memory %83,326,171,418,20,038

Sample No. 1
TestsInitial testingTesting during Potentate the emission
 MS.D.MS.D.P
Red-black table, 114,875,995,559,80,078
The simple reaction time, MS224,530,9227,0of 45.70,845
The reaction time choice, MS327,051,4326,732,40,973
Tremor, time/s2,50,82,31,20,612
Memory %85,626,777,8to 25.30,141

Sample # 2
TestsInitial testingTesting during posthistorical
 MS.D.MS.D.P
Red-black table, 110,320,779,848,40,124
The simple reaction time, MSto 220.324,9268,839,70,044
The reaction time choice, MS305,760,3420,553,50,014
Tremor, time/s2,40,72,21,10,714
Memory %87,120,471,321,10,040

Sample # 3
TestsInitial testingTesting during posthistorical
 MS.D.MS.D.P
Red-black table, 112,342,0to 89.554,20,094
The simple reaction time, MS231,129,5275,051,80,106
The reaction time choice, MS320,554,4431,5to 49.30,031
Tremor, time/s2,40,82,00,90,608
Memory %88,924,872,823,30,038

Table 3

Structure (frequency in %) manifestations postintoksikatinom status, developed by the subjects on the background of placebo proposed and known compositions.SymptomsPlaceboSample 1Sample 2Sample 3Excessive thirst58,316,733/325Malaise and fatigue33,32533,333,3Dry mouth58,316,65050Headache2525258,33Trembling fingers258,3316,725Memory lapses about yesterday8,338,338,338,33Nervous tension16,7 16,7 Excessive appetite16,716,733,333,3Anxiety and agitation25 25 Dizziness 8,338,3316,716,7Lack of appetite8,33 8,338,33Irregular bowel movements (diarrhea, constipation)16,78,338,338,33Swelling face16,7 8,338,33The need to smoke16,716,716,716,7Staggering gait16,7 8,338,33Pallor (cold, moist skin)8,33   Nausea or vomiting8,33   Excessive sweating8,338,338,338;33Hyperemia (redness) of the face8,33 8,338,33The change in skin sensitivity8,33   Need to take medication8,338,338,338,33Irritable the path and   8,33 Bitterness    Increased Department saliva8,338,338,338,33Shortness of breath8,33   

Table 4

The severity postoxidation status of the subjects on the background of placebo offered and known compositions.
 Points
Subject NNPlaceboSample 1Sample 2
1846
2211
31059
4424
5633
6635
71147
8434
97 4
Average scores (M±S.D.)6,4±2,93,1±1,2*4,8±2,3
Note: * - p<0,01 compared with placebo.

1. Means for reducing the adverse effects of acute alcohol intoxication, characterized in that it contains succinic acid and/or its salts, fumaric acid and/or its salt, fructose, dry extract of the herb St. John's wort (Hypericum), the source of magnesium ions and a source of potassium ions as the active principles and, if necessary, excipients, carriers and/or excipients.

2. The tool according to claim 1, which contains the active substance in the following ratio of components (per dose), mg:

Succinic acid and/or its salt of 0.4-1000,0

Fumaric acid and/or its salt is 0.3 to 800,0

Fructose 10,0-500,0

The dry extract of the herb of Hypericum perforatum

(Hypericum perforatum L) 50,0-1000,0

The source of magnesium ions,

providing the content of Mg++0,3-150,0

The source of potassium ions,

providing the content of ions To+3,0-300,0

3. The tool according to claims 1 and 2, in which the ion sources of magnesium and potassium in part and, if necessary, completely are the corresponding salts of succinic and fumaric acids.

4. The tool p., used before alcohol consumption during their use or after alcoholic excess.



 

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22 cl, 12 tbl

FIELD: veterinary science, veterinary surgery.

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1 ex, 1 tbl

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3 ex

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2 cl, 1 ex, 1 tbl

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1 ex

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3 cl, 3 ex

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