RU2601894C1 - Chrono-biological correction agent - Google Patents

Abstract

FIELD: biotechnology.

SUBSTANCE: invention relates to a chrono-biological correction agent. Said agent comprises 34.0-56.8 wt% of spiny eleutherococcus rhizomes and dry extract roots, 18.1-25.0 wt% of amber acid, 4.5-7.9 wt% of pyridoxine hydrochloride and 10.3-43.4 wt% of additive substances.

EFFECT: invention ensures reducing fatigue and sleepiness, normalizes a sleep-wake rhythm, improves physical and mental working efficiency, accelerates discharging of insufficiently oxidized metabolic products.

1 cl, 1 tbl, 4 ex

Description

Technical field

The invention relates to medicine and can be used to correct desynchronism of functions of various organs and systems of the human body caused by professional and technogenic factors (air travel to a different time zone, night shift and shift work, living in the polar regions of the Arctic, chronic light conditions and sleep and wakefulness), as well as related health disorders.

State of the art

One of the most important factors in the deterioration of the health of a modern person is the chronic desynchronosis of various organs and systems of the body due to the mismatch of daily (circadian) biorhythms in connection with the influence of such inalienable factors of modern life as: transmeridial flights, shift working methods and constant interference of factors of the urban environment leading to chronic disturbance of sleep and wakefulness. Violation of the natural structure of biorhythms leads to disruption of the processes of restoration of organs and systems, their overstrain and premature depletion of biological resources, which is currently considered to be one of the most important pre-painful human conditions. With prolonged persistence of desynchronosis and the absence of measures for its prevention and correction, this pre-painful state can turn into chronic diseases, primarily of the nervous, cardiovascular, endocrine systems.

Currently, for the prevention and correction of desynchronosis, pharmacological and physiotherapeutic effects are used, mainly aimed at regulating the nervous and endocrine systems.

Known means and method of correcting desynchronosis of the human body caused by air travel to another time zone (F.A. Iordanskaya. Features of temporary adaptation when flying east and west. Means of correction and prevention of desynchronosis. Theory and practice of physical culture. - 2000. - No. 3 . - S. 6-13). The essence of this approach is the use of various physiotherapeutic methods of a two-phase correction scheme, which, depending on the condition, includes either tonic or sedatives in combination with restorative drugs. With a fairly broad integrated approach, this method has a number of limitations that narrow the spectrum of its application. Firstly, the described means and method are intended solely for correcting short-term desynchronosis caused by transmeridial flights, and does not meet the characteristics of chronic desynchronosis due to professional or urban factors. Secondly, these funds are aimed only at correcting the general structure of circadian rhythms and do not take into account the characteristics of individual biorhythms of individual organs and systems. Thirdly, these funds are aimed at increasing the general biological resistance of the body and do not take into account painful disorders in the functioning of organs and systems of the body developing as a result of chronic desynchronosis.

The drug Melaksen is known, the active substance of which is a synthetic analogue of the hormone pineal gland melatonin, capable of normalizing circadian rhythms by its specific action, i.e. to restore the sleep-wake rhythm (Zamoshchina T.A. Chronobiological basis of the neurotropic effects of lithium salts: diss. Doct. Biol. Sciences / T.A. Zamoshchina. - Tomsk, 1997. - 286 p.). However, this medicine has a number of disadvantages: headache, morning drowsiness, swelling, limitation of activities requiring an increased concentration of attention while taking the drug, symptoms of dyspepsia and a number of contraindications (severe renal dysfunction, autoimmune diseases, leukemia, pregnancy).

Closest to the claimed tool for the correction of chronic dysynchronosis is the tool disclosed in patent No. 2317822, publ. 08/22/2008, including morning and evening complexes, including plant components of a mild tonic and biostimulating effect and a complex of plant adaptogens, and plant components of a mild sedative and sedative effect and stimulating the restoration of cellular resources, respectively. The morning complex of means for correcting desynchronosis includes the roots of Eleutherococcus and pyridoxine hydrochloride (vitamin B6). A disadvantage of the known agent is that it is two-phase, i.e. consists of a morning and evening complex. The use of a wide range of biologically active substances in one dosage form can lead to incompatibility phenomena, both chemical and pharmacological. Each specifically selected complex is designed to correct a certain nature, for example, a decrease in the general biological resistance of the body and the development of general somatic diseases or a violation of the cardiovascular system, or a violation of the central nervous system, or a violation of the liver and biliary tract, or disorders of the supporting -motor system.

Disclosure of invention

The objective of the present invention is to develop means of chronobiological correction based on plant materials, taking into account the entire spectrum of manifestations of desynchronosis and features of individual biorhythms of organs and systems.

The technical result achieved using the chronobiological correction means is to minimize the number of side effects, reduce fatigue and drowsiness, normalize the rhythm of sleep and wakefulness, increase physical and mental performance, do not irritate the gastric mucosa, and accelerate the withdrawal of under-oxidized metabolic products.

The specified technical result is achieved by means of chronobiological correction, including the following components in quantity, wt.%:

prickly rhizome eleutherococcus and root extract dry 34.0-56.8 succinic acid 18.1-25.0 pyridoxine hydrochloride 4,5-7,9 Excipients 10.3-43.4

The tool is a hard gelatin capsule with granules or tablets.

The composition of the active ingredients is selected so that the number of side effects is reduced to an absolute minimum, which allows you to safely take this tool.

Prickly Eleutherococcus (Eleutherococcus senticocus Maxim) is a shrub from the Araliaceae family, 1.5-3 m high. Rhizomes with the roots of wild prickly Eleutherococcus are used as raw materials for obtaining a liquid and dry extract. Currently, Eleutherococcus preparations are widely distributed and are one of the most widely used adaptogens under various extreme conditions that increase the nonspecific resistance of cells to various damaging environmental factors, including desynchronoses of various nature.

The tonic effect of eleutherococcus is manifested with prolonged use and consists in improving the general state of health. It improves basic metabolism, improves the adaptive properties of the body, regulates blood sugar, normalizes the state of the body under stress. A single use of Eleutherococcus has a stimulating effect - fatigue, drowsiness and physical performance increase. Eleutherococcus is one of the most valuable plant stimulants of physical performance. It is used as a medicine and in biologically active additives.

Succinic acid is a natural tool inherent in the human body that provides energy for muscles, brain, heart, nerves. The most important participant in the tricarboxylic acid cycle or the Krebs cycle. The addition of succinic acid (succinate) from the outside activates the Krebs cycle, which allows you to speed up the process of removing under-oxidized metabolic products. Succinic acid is an energizer and, unlike stimulants (coffee, etc.), does not give the effect of aftereffect, that is, reduced performance, mood depression after the action (depression after the stimulation effect).

Vitamin B6 (pyridoxine hydrochloride) - pyridoxine is involved in the exchange of glutamic acid. GABA and serotonin, in the synthesis of catecholamines, has a direct effect on the course of excitation and inhibition in the brain. Vitamin preparations of group B are antihypoxants.

The studies on the selection of the amount of active substances are based on data described in the literature [https://health.mail.ru/drug/eleutherococci_extract/; http://simptom.net/medicaments/yantarnaya_kislota/; http://www.farmrecipe.ru/recipes/sec/118/rec/Piridokhsin].

A study of the pharmacological effect of the dry extract of eleutherococcus, succinic acid and pyridoxine hydrochloride was carried out in the experiment of correction of “light desynchronosis” in groups of experimental animals (white outbred mice, rats) when they were orally administered both individual biologically active compounds and their combinations. Evaluation of the action of the tool was carried out according to the duration of swimming of laboratory animals according to the classical Porsolt method [Karkishchenko NN, Uyba VV, Karkishchenko VN, Shustov EB Essays on sports pharmacology. Volume 1. Vectors of extrapolation / M., St. Petersburg, 2013288 p.] After continuous 24-hour illumination of animals with fluorescent lamps for 14 days; by changing the masses of stress-competent organs (spleen, adrenal glands, liver).

The introduction in the dose range of biologically active compounds in the range of 50-150 mg, 20-70 mg and 5-15 mg, respectively, showed an increase in the duration of swimming of animals by 2% compared with the control group; the mass of stress-competent organs was not significantly different from the mass of the organs of animals that did not receive the test agent.

With the introduction of a dry extract of eleutherococcus, succinic acid and pyridoxine hydrochloride in the dose range of 500-1000 mg, 500-700 mg and 80-200 mg with an increase in swimming time by 10% compared with the results of a group of animals that did not receive the test drug, however, the recovery time animals was about 3 days, animals were lethargic, poorly consumed food, water. The mass of stress-competent organs also differed insignificantly from the mass of the organs of animals that did not receive the test drug. In addition, with the introduction of high doses of succinic acid, an irritating effect on the wall of the gastric mucosa was noted.

The best result was obtained with a combination of doses of eleutherococcus of prickly rhizomes and the roots of dry extract, succinic acid and pyridoxine hydrochloride in the dose range of 150-350 mg, 80-150 mg and 20-35 mg, respectively. The effectiveness of the swimming results of the experimental group increased by 39% compared with the control.

No irritating effect on the gastric mucosa of laboratory animals was found; it was revealed that the mass of stress-competent organs was not significantly different from the mass of the organs of animals that were not exposed to light desynchronosis.

For ease of use, compliance with the accuracy of dosing of biologically active compounds, as well as improving the stability of the dry extract of eleutherococcus of prickly rhizomes and roots, succinic acid, pyridoxine hydrochloride, dosage forms in the form of capsules (tablets) made from granules obtained by adding auxiliary substances to mixtures of biologically active compounds in ratios from 80:20 to 20:80.

As auxiliary substances, both individually and in a mixture were used: potato and corn starch, pregelatinized starch, pregelatinized starch with calcium carbonate, crystalline lactose, lactose monohydrate, mannitol, microcrystalline cellulose, silicified microcrystalline cellulose, colloidal silicon dioxide, colloidal silicon dioxide or magnesium, stearic acid.

As humidifiers, solutions of methyl alcohol, ethyl alcohol, isopropyl alcohol, either alone or with water, solutions of polyvinylpyrrolidone 0.1-10% in solutions of methyl alcohol, ethyl alcohol, isopropyl alcohol with water of various concentrations, as well as aqueous solutions of starch of concentration 0, were used. 25-10%, methyl cellulose 0.1-10%, sugar beet or cane 0.1-10%, pregelatinized starch in a concentration of 0.1-10%.

The ingredients were mixed in mixers of various types, achieving uniformity of composition, moistened with a solution of binders, and a moistened mass was obtained, depending on the type of mixer of varying degrees of humidity. If necessary, the granulate was dried to a constant humidity not exceeding 5%, carried out in an oven, at a temperature not exceeding 40 ° C. Next, the obtained granules were mixed with 0.01-0.5% stearic acid or its calcium or magnesium salt and sent for capsulation into capsules No. 00 or for tabletting 0.29-0.35 g.

The possibility of implementing the claimed invention is shown in examples of specific performance, but is not limited to these examples.

Examples of carrying out the invention

Example 1

Eleutherococcus of prickly rhizomes and roots dry extract - 220 mg;

Succinic acid - 80 mg;

Pyridoxine hydrochloride - 30 mg;

Lactose - 40 mg;

Corn starch - 69 mg.

The mass of the contents of the capsule is 439 mg.

Result: efficiency - finished product / waste ratio - 96/4%, flowability - 5.5 g / s.

Example 2

Eleutherococcus of prickly rhizomes and roots dry extract - 160 mg;

Succinic acid - 150 mg;

Pyridoxine hydrochloride - 20 mg;

Corn starch - 109 mg.

The mass of the contents of the capsule is 439 mg.

Result: efficiency - finished product / waste ratio - 96/4%, flowability - 6 g / s.

Example 3

Eleutherococcus of prickly rhizomes and roots dry extract - 150 mg;

Succinic acid - 150 mg;

Pyridoxine hydrochloride - 20 mg;

Lactose - 119 mg;

Pregelatinized starch - 1 mg.

The mass of the contents of the capsule is 440 mg.

Result: efficiency - finished product / waste ratio - 97/3%, flowability - 5 g / s.

Example 4

Eleutherococcus of prickly rhizomes and roots dry extract - 200 mg;

Succinic acid - 100 mg;

Pyridoxine hydrochloride - 30 mg;

Microcrystalline cellulose - 109 mg;

Pregelatinized starch - 1 mg.

The mass of the contents of the capsule is 440 mg.

Result: efficiency - finished product / waste ratio - 98/2%, flowability - 7 g / s.

The recommended daily dose is 1 capsule per day. The drug favorably affects stress-competent organs (liver, spleen and adrenal glands) and the antioxidant system of human protection by increasing the work of adaptive mechanisms (see table).

Claims (2)

1. A means of chronobiological correction, including the following components in quantity, in wt.%:
dry Eleutherococcus spiny rhizome and root extract 34.0-56.8 succinic acid 18.1-25.0 pyridoxine hydrochloride 4,5-7,9 Excipients 10.3-43.4 2. The tool according to p. 1, characterized in that the excipients are used both individually and in a mixture: potato and corn starch, pregelatinized starch, pregelatinized starch with calcium carbonate, crystalline lactose, lactose monohydrate, mannitol, microcrystalline cellulose, silicified microcrystalline cellulose, colloidal silicon dioxide, polyvinylpyrrolidone, calcium or magnesium stearate, stearic acid.