RU2503457C2 - Agent for extreme performance stimulation - Google Patents

Abstract

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, namely to an agent for extreme performance stimulation. The agent represents a mixture of peptides of molecular weight 2000-5000 Da prepared of the infant cattle and/or swine brain, namely of the ventral and dorsal hippocampus of cingulate sulcus (sulcus cinguli) of amygdaloid body (nucleus amygdalae) of the limbic system, as well as of caudate nucleus (nucleus caudatus) and hypothalamus in the concentration of the mixture of peptides in the agent of 5.0-10.0 mg/ml of the aqueous solution or 5.0-10.0 mg/g in the witepsol suppository.

EFFECT: group of inventions provides higher performance efficiency and tolerance in trained individuals at least by 10-12% as compared with the reference group.

1 cl, 9 tbl, 2 dwg

Description

The invention relates to medicine and relates to medical devices for a specific effect on body functions.

Known technical solutions made at the level of inventions, which increase the performance and endurance of persons subject to intense physical exertion. [1-3]

The indicated technical solutions are a food product [1] enriched in phospholipids or protein-amino acid food products [2] or protein-peptide modules for food production [3] for nutrition of athletes or other persons leading an active lifestyle.

It is characteristic that the above foods or food additives, firstly, do not significantly increase working capacity and endurance, and only after prolonged (2-3 months or more) consumption of these products, and, secondly, increasing health and stamina occurs mainly due to an increase in muscle mass and, thirdly, these foods are not stimulants of performance and endurance as such, i.e. do not meet the necessary requirements for work in extreme conditions.

In the available scientific, technical and patent literature, no analogues and prototype are found that meet the proposed stimulator for working in extreme conditions.

The technical result, the achievement of which the creation of this invention is aimed, is to increase the working capacity and endurance when working in extreme conditions (extreme and transcendental and prolonged physical exertion, stressful situations, etc.), for example, during special operations and similar critical events requiring maintaining high performance in conditions of extreme psycho-emotional stress.

The technical result achieved is achieved by the fact that the claimed tool for stimulating work in extreme conditions is a fraction of peptides with a molecular weight of 2000-5000 Da obtained from the ventral and dorsal hippocampus (hippocampus) of the sulcus (sulcus cinguli) amygdala complex (nucleus amygdalae) of the limbic system , caudate nucleus (nucleus caudatus) and hypothalamus (hypothalamus) of the brain of cattle or pigs under the age of one year, when the concentration of the mixture of peptides in the agent is 5.0-10.0 mg / ml in an aqueous solution or 5.0 -10.0 mg / g in suppositories based on Vitepsol.

As raw materials for producing peptides, parts of the brain departments of slaughtered cattle and / or pigs (cattle) not older than 1 year are used: the ventral and dorsal hippocampus (hippocampus) of the sulcus (sulcus cinguli) of the amygdala complex (nucleus amygdalae) of the limbic system of the brain, caudate nucleus (nucleus caudatus) and hypothalamus (hypothalamus).

The hydrolysis of the crushed parts of the brain is carried out in an acidic environment (acetic acid + zinc chloride).

The separation of the active components of the agent during the hydrolysis and separation of the hydrolyzate is carried out by ultrafiltration and preparative chromatography.

The proposed tool for stimulating work in extreme conditions is an aqueous solution of a fraction of peptides with a molecular weight of 2000-5000 Da obtained by preparative chromatography of purified and filtered

the hydrolyzate of parts of the parts of the brain of slaughtered cattle and / or pigs (cattle) not older than 1 year, namely: the ventral and dorsal hippocampus (hippocampus) of the sulcus (sulcus cinguli) amygdala complex (nucleus amygdalae) of the limbic system of the brain, caudate nucleus ( nucleus caudatus) and hypothalamus (hypothalamus) and the concentration of peptides in an aqueous solution is 5.0-10.0 mg / ml or 5.0-10.0 mg / g in a vitepsol suppository.

It should be noted that the claimed tool does not cause either addiction or addiction (addiction).

Another significant feature of the claimed tool is that it can be detected in the blood of the recipient by analytical means only during the first 15-25 minutes. after parenteral administration (and with rectal administration, it cannot be detected at all by modern analytical means). This circumstance is crucial in the practice of stimulating athletes.

Get a tool to stimulate work in extreme conditions as follows.

In slaughtered animals (for example, 11-month-old calves and 8-month-old pigs), the brain is removed, the ventral and dorsal hippocampus of the lumbar fossa of the amygdala complex of the limbic system of the brain are excised, the caudate nucleus and hypothalamus These parts of the brain are frozen at least to -40 ° C and then crushed and homogenized in water, the homogenate is hydrolyzed at 20 ° C in the presence of acetic acid and zinc chloride, extracted

the extract is separated from the ballast substances by separation through materials with a retention capacity of more than 10,000 Da, the hydrolyzate is precipitated with 30% acetic acid solution, the precipitate is washed with acetone, the precipitate is dissolved in water and the 2000-5000 Da fraction is separated by preparative chromatography (LC-30 Nexera chromatograph, LC- pump 8A, column inner diameter 20 mm), the separated fraction 2000-5000 Da is dissolved in water and dried by lyophilization, then the agent is prepared by dissolving the fraction 2000-5000 Da (A) to a concentration of 5.0-10.0 mg / ml in water or by introducing a fraction into vitepsol to the content of 5.0-10.0 mg / g, followed by the formation of suppositories.

The study of the impact of the claimed funds on improving adaptogenic activity, performance and endurance of humans (and animals) in a state of high physical and psycho-emotional stress is carried out in accordance with GOST R 15.105-2001, according to standard operating procedures of laboratories and according to the "Rules of laboratory practice in the Russian Federation "(Order of the Ministry of Health of the Russian Federation No. 267 of 06/19/2003), as well as the national standard of the Russian Federation" Principles of Good Laboratory Practice "GOST R 53434 - 2009.

Example 1

The change in physical performance of outbred white rats under aerobic power loads is determined.

The influence of the claimed means on physical performance is determined by measuring the duration of the run on the treadmill from the start of the run until the animal develops a state of final refusal to perform physical activity. The duration of one test cycle is 27 days.

The test is carried out as follows. Preliminary training of animals at the stand (treadmill, 1 day, 10 min at an angle of inclination of the treadmill tape 20 ° and its speed 23 m / min), administration of the agent to animals (within 21 days), observation of animals after the termination of administration of the agent (7 days) . A repeated test cycle with the introduction of funds is carried out

Form 2 groups of laboratory rats of 12 animals each. The first group receives the claimed drug, the second (control) - saline. Drugs are administered rectally. Dose of administration: agents 0.5 mg / goal ..

40 minutes after the introduction of the product - run 15 minutes at a speed of 27 m / min and with a tape inclination of 20 °. The voltage is 40 V. The indicators are taken on the 1st, 8th, 15th, 21st and 27th day of the experiment. The main indicator is the total contact time of the rat with the electric platform and the running time.

The endurance of rats when running on a treadmill is presented in Table 1.

Table 1 1st day 8th day 15th day 21st day 27th day The inventive tool running (sec) 263 ± 22 254 ± 20 238 ± 23 205 ± 19 207 ± 15 Control group running (sec) 241 ± 26 203 ± 23 168 ± 21 133 ± 13 143 ± 13

As can be seen from Table 1, the endurance of rats under the action of the claimed funds in comparison with the control group increases significantly.

Figure 1 (see page 8 of the description) presents the effect of the claimed funds on the endurance of experimental animals from the original (100%). The area of 20 days and 30 days on the graph represent the use of the proposed drug and a break in use, respectively. The test time (days) is plotted on the abscissa axis and the change in endurance as a percentage of the original value is plotted on the ordinate axis.

Figure 2 (see page 8 of the description) presents the effect of the claimed funds on the endurance of experimental animals in contact with an electrical stimulating platform treadmill. Test time (days) is plotted on the abscissa axis and contact duration is plotted on the ordinate axis. Lines 1, 2, 3 and 4 show the effect of the claimed drug (A + B), peptides A and peptides B individually and data for the control group, respectively.

Example 2

To identify the pharmacological activity of the claimed drug, a test of "despair" or forced swimming, which reflects the state of depression of animals. The forced swimming test is a combined hard form of stress that combines physical and emotional components.

In the experiment, animals of both groups are subjected to stress - swimming in a pool with a load. Water temperature -24 ° C.

The test results are presented in Table 2

table 2 The inventive tool 1st day 8th day 15th day 22nd day 27th day First swim 84.3 ± 3.9 193.4 ± 4.8 214.3 ± 4.4 227.25 ± 4.5 209.7 ± 6.7 Repeated 64.9 ± 3.9 143.3 ± 3.5 145.2 ± 3.4 159.0 ± 4.28 146.5 ± 4.42 Third 72.7 ± 3.4 160.4 ± 3.0 165.0 ± 3.3 204.6 ± 10.9 175.3 ± 3.0 Control group First swim 63.8 ± 3.3 66.8 ± 2.6 71.0 ± 3.2 71.9 ± 3.9 91.4 ± 3.3 Repeated 49.3 ± 3.5 46.4 ± 2.4 52.7 ± 2.7 54.5 ± 3.0 68.7 ± 3.2 Third 53.9 ± 2.7 54.7 ± 2.2 62.3 ± 3.0 62.3 ± 3.4 79.8 ± 2.9

Example 3

Hypoxia test.

A measure of the sensitivity of animals to acute hypobaric hypoxia is the life expectancy at the "height". Each animal is "raised" to a critical height (11.5 thousand m) at a speed of 165 m / s, where it was located to an agonal state. Designations:

Runway - the time of the first fall (transition to a lying position), characterizing the threshold of the body's reaction to this effect.

VZh - life time at "height" (before the appearance of agonal breathing).

GDP - the time of posture recovery after the animal “descends” from the “height”

KEZ - coefficient of effectiveness of protection (lifetime in experience / lifetime in control)

The test results of acute hypobaric hypoxia are presented in Table 3

Table 3 Indicator 1 day 8 day 15 day 22 day 27 day The inventive tool Runway, sec 7.9 ± 0.7 7.9 ± 0.7 10.4 ± 0.9 15.8 ± 1.0 13.8 ± 1.1 VZh, sec 95.8 ± 7.3 123.3 ± 7.9 239.6 ± 12.0 285.8 ± 9.0 262.1 ± 10.7 GDP, sec 25.4 ± 2.3 22.9 ± 1.7 20.8 ± 1.7 15 ± 1.7 16.3 ± 1.8 Control group Runway, sec 7.92 ± 0.74 8.75 ± 0.65 7.5 ± 0.75 8.75 ± 0.65 10 ± 0.62 VZh, sec 105.8 ± 6.2 92.9 ± 5.5 95.8 ± 3.7 107.1 ± 6.3 97.1 ± 5.1 GDP, sec 24.2 ± 2.6 21.3 ± 1.5 23.3 ± 2.3 25.8 ± 2.0 25.4 ± 1.9

Protection effectiveness indicators (CEC) * for acute hypobaric hypoxia (to its own background indicators) are presented in Table 4

Table 4 Groups KEZ 8 day 15 day 22 day 27 day The inventive tool 1.28 2,50 2.98 2.73 Control group 1,0 1,0 1,0 1,0

Example 4

The impact of the proposed drug on large laboratory animals (mini-pigs) at maximum physical exertion.

Form 2 groups of 6 heads of mini-pigs weighing 18 ± 1.9 kg, males, age 8 months. The first group receives the claimed drug, the second (control) - placebo. The inventive tool is administered rectally. Dose of administration: - 0.56 mg / kg, the rectal form of a placebo is administered to the control group.

Animals are forced to run on a treadmill (Togpeo T-203). The duration of the run and the distance covered are measured.

The endurance indicators of mini-pigs when running on a treadmill are presented in Table 5

Table 5 The inventive tool 1st day 8th day 15th day 21st day 27th day Running Duration (min) 27.0 ± 1.1 28.1 ± 1.0 29.8 ± 0.6 31.6 ± 1.4 31.3 ± 1.2 Distance traveled (m) 2500 ± 100 3100 ± 150 3300 ± 100 4100 ± 150 4000 ± 120 Control group Running Duration (min) 26.6 ± 1.2 27.0 ± 1.4 27.9 ± 1.3 28.2 ± 0.9 28.2 ± 1.9 Distance traveled (m) 2500 ± 120 2600 ± 150 2700 ± 150 2900 ± 150 2900 ± 150

It should be noted that, along with an increase in endurance, mini-pigs also increased their speed of movement.

Example 5

Tests of the effects of the claimed funds are carried out on athletes - volunteers.

Cyclists are selected (12 people with close anthropometric data, age 20-22), divided into 2 groups of 6 people each. The first group receives the claimed drug, the second (control) - saline. Drugs are administered rectally. The dose of administration is 20.0 mg.

The effect of the claimed means on physical performance is determined by measuring the duration of the "races" on a bicycle ergometer with an adjustable load (angle of elevation 20 °) from the beginning of the "race" until the athlete develops a state of final refusal to perform physical activity. Table 6 presents the effect of the claimed funds on the physical performance of cyclists at maximum speed (spurt)

Table 6 The inventive tool 1st day 8th day 15th day 21st day 27th day The duration of the "race" (min) 4.6 ± 0.3 5.7 ± 0.2 6.2 ± 0.1 68 ± 0.2 67 ± 0.3 Control group The duration of the "race" (min) 43 ± 0.3 4,5 ± 0,1 4.6 ± 0.2 4.6 ± 0.5 4,5 ± 0,1

Table 7 presents the effect of the claimed funds on the physical performance of cyclists at the stayer speed

Table 7 The inventive tool 1st day 8th day 15th day 21st day 27th day Distance traveled (m) 7600 ± 100 9800 ± 150 11000 ± 100 12800 ± 150 12300 ± 120 Control group Distance traveled (m) 6300 ± 120 6500 ± 150 6900 ± 100 7100 ± 100 6900 ± 150

Example 7

A test of the effect of the claimed means on the overall physical endurance of swimmers.

The impact of the claimed means is determined by measuring the duration of swimming at a speed of 60-62% of the competition from the start of the swim until the athlete develops a state of refusal to perform physical activity.

Table 8 presents the effect of the claimed funds on the overall physical endurance of swimmers.

Table 8 The inventive tool 1st day 8th day 15th day 21st day 27th day Duration of swimming (min) 24.0 ± 2 27.0 ± 3 310 ± 3 34.0 ± 2 33.0 ± 2 Control group Duration of swimming (min) 24.0 ± 2 25.0 ± 3 240 ± 2 23.0 ± 5 220 ± 4

The influence of the proposed tool on the speed capabilities of swimmers is determined by measuring the distance traveled over 5 minutes of swimming at a speed of presumably ~ 95% of the competition. Table 9 shows the effect of the proposed tool on the speed capabilities of swimmers.

Table 9 The inventive tool 1st day 8th day 15th day 21st day 27th day Speed (km / h at 95% load) 5.0 ± 0.1 6.2 ± 0.15 6.9 ± 0.1 7.6 ± 0.1 7.5 ± 0.1 Control group 4.9 ± 0.1 5.0 ± 0.1 5.1 ± 0.1 5.0 ± 0.1 4.7 ± 0.1 Speed (km / h at 95% load) 4.9 ± 0.1 5.7 ± 0.1 6.3 ± 0.1 6.9 ± 0.1 6.8 ± 0.1

As can be seen from the description, examples of the impact of the claimed tool on performance in extreme conditions (especially when exposed to extreme physical and psycho-emotional stress), as well as from comparison with control examples, the claimed tool stimulates an increase in performance and endurance in trained people by at least 10-12 % compared to the original,

Sources of information taken into account when preparing the application.

1. RU 2370158 C2, M. cl. A23L 1/30, publ. 2010 year

2. RU 2375923 C2, M. cl. A23L 1/30, publ. 2010 year

3. RU 2388350 C2, M. cl. A23L 1/30, publ. 2010 year

Claims (1)

A tool for stimulating work under extreme conditions, characterized in that it is a mixture of peptides with a molecular weight of 2000-5000 Da obtained from the ventral and dorsal hippocampus (hippocampus) of the sulcus (sulcus cinguli) amygdala complex (nucleus amygdalae) of the limbic system, caudate the nucleus (nucleus caudatus) and hypothalamus (hypothalamus) of the brain of cattle or pigs under the age of one year, when the concentration of the mixture of peptides in the agent is 5.0-10.0 mg / ml in an aqueous solution or 5.0-10.0 mg / g in suppositories based on vitepso la

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