RU2468812C2 - Agent possessing adaptogenic, tonic and general tonic action, and method for preparing it - Google Patents

Abstract

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to chemical-pharmaceutical industry and represents an agent showing adaptogenic, tonic and general tonic action and containing ascorbic acid, nicotinamide, riboflavin, pyridoxine, differing by the fact that it additionally contains dry guarana extract, magnesium gluconate, magnesium citrate, calcium pantotenate, thiamine hydrochloride, folic acid, fructose, citric acid, aromatiser, sweetening agent, a preserving agent, water with the ingredients found in certain proportions, wt %.

EFFECT: invention provides intensified pharmacological action.

2 cl, 8 ex, 1 tbl

Description

The invention relates to pharmacy, and in particular to medicines for oral use, with adaptogenic, tonic and restorative effect. It can be used to increase the body's resistance to lower oxygen levels, as well as to prevent functional disorders associated with exposure to stress and exhausting factors.

The prior art composition (Application for invention No. 2002106757, publ. 02.27.2003), which has a restorative and tonic effect, containing royal jelly and 40% ethyl alcohol.

A known composition containing succinic acid up to 99.998 wt.%, Vitamin B ₂ (riboflavin) and a pharmaceutically acceptable carrier (RF patent No. 2143265, prior dated 05.12.97, A61K 31/19, publ. 27.12.99) .

The drug of this composition has a limitation in use, since it causes an increase in the acidity of gastric juice.

Known drug "METIOVIT" containing succinic acid, pectin, methionine, glucose, citric acid, ascorbic acid, baker's yeast autolysate (RF patent No. 2105502, prior. 29.03.96, A23L 1/30, publ. 02.27.98 g .).

However, the therapeutic efficacy of such a drug is reduced due to the low bioavailability of the active substances. This is due to the fact that the dosage form does not have an enteric-soluble coating, and the release of active components occurs in the stomach, and not in the intestine, where their absorption would be greatest.

As the closest analogue, a known composition may be indicated containing riboxin, glutamic acid, ascorbic acid, nicotinamide, riboflavin, pyridoxine, potassium chloride (Membrane-stabilizing and antioxidant drug "RZHAVIT", RF patent No. 20066224, A61B 31/00, prior . from 05.06.85, published on 01.30.94).

However, this drug has limitations for use and is contraindicated in case of impaired purine metabolism, a metabolic disorder that manifests itself in kidney damage and leads to the development of nephrosclerosis and renal failure.

The technical task of the invention is the development of a composition with increased pharmacological action.

The task is achieved using a composition containing, in addition to ascorbic acid (vitamin C), riboflavin (vitamin B2), pyridoxine hydrochloride (vitamin B6), nicotinamide (B3), additional guarana extract, magnesium gluconate, magnesium citrate, calcium pantothenate (vitamin B5), thiamine hydrochloride (vitamin B1), folic acid (vitamin B9), fructose, citric acid, flavoring, sweetener, preservative in the following ratio, wt.%:

Dry guarana extract 1-20 Magnesium Gluconate 0.01-5 Magnesium citrate 0.5-6 Ascorbic acid (Vitamin C) 0.1-5 Nicotinamide (Vitamin B3) 0.001-1 Calcium Pantothenate (Vitamin B5) 0.01-1 Pyridoxine Hydrochloride (Vitamin B6) 0.001-0.5 Riboflavin (Vitamin B2) 0.1-0.5 Thiamine Hydrochloride (Vitamin B1) 0.001-0.5 Folic Acid (Vitamin B9) 0.01-0.5 Fructose 1-27 Lemon acid 0,1-10 Flavoring 0.001-0.5 Sweetener 0.001-1.5 Preservative 0.01-1.0 Water rest

An essential distinguishing feature of the invention is the presence of guarana with a high content of active substances in the composition of the dry extract, which makes it possible to expand the pharmacological spectrum of action and increase adaptogenic activity due to synergism.

The tool may additionally contain pharmaceutically and pharmacologically compatible minerals and their compounds, carotenoids, and / or flavonoids, antioxidants, enzymes or other medicinal substances, amino acids, protein, vitamins, hormones (hormone-like substances) and sterols.

The composition may contain one or more pharmaceutically and pharmacologically compatible active substances selected from the groups: carotenoids, flavonoids, vitamins, vitamin-like substances, essential substances, amino acids, proteins, minerals, angiotensin-converting enzyme inhibitors; α-adrenergic agonists; β-adrenergic agonists; α-adrenergic blockers; β-adrenergic blockers (beta blockers); alcohol inhibitors; aldose reductase inhibitors; aldosterone antagonists; amino acids; anabolics; analgesics (both narcotic and non-narcotic); anesthetics; anorexics; antacids; anthelmintic drugs; anti-acne agents; antiallergic drugs; antiandrogens; antianginal agents; sedatives; antiarrhythmics; anti-asthma drugs; antibacterial agents and antibiotics; drugs against alopecia and baldness, anti-amoebic drugs; antibodies; anticholinergics; anticoagulants and blood thinners; anticolytic drugs; anticonvulsants; anti-cystic drugs; antidepressants; antidiabetic agents; antidiarrheal agents; antidiuretics; antidotes; antiemetics; antiestrogens; antiflating agents; antifungal agents; antigens; anti-glaucoma agents; antihistamines; antihyperactive drugs; antihyperlipoproteinemic agents; antihypertensive agents; anti-hyperthyroid agents; antihypertensive drugs; antihypothyroid drugs; anti-infectious agents; anti-inflammatory (both steroidal and non-steroidal) drugs; antimalarial agents; anti-migraine agents; antineoplastics; anti-obesity drugs; antiparkinsonian agents and antidiscinetics; antipneumonic agents; antiprotozoal agents; antipruritic drugs; antipsoriatics; antipsychotics; antipyretics; anti-rheumatic drugs; antisecretory agents; anti-shock medicines; antispasmodics; antithrombotic agents; anti-cancer agents; antitussive drugs; antiulcer drugs; antiviral agents; anxiolytics; bactericidal agents; bone compactors; bronchodilators; calcium channel blockers; carbonic anhydrase inhibitors; cardiotonics and pacemakers; chemotherapeutic agents; choleretic drugs; cholinergic agents; agents for treating chronic fatigue syndrome; CNS stimulants; coagulants; contraceptives; agents for the treatment of cystic fibrosis; decongestants; diuretics; dopamine receptor agonists; dopamine receptor antagonists; enzymes; estrogen; expectorant; agents for treating gastric hyperactivity; glucocorticoids; hemostatic agents; coenzyme A reductase inhibitors of human menopausal gonadotropin; hormones; sleeping pills; immunomodulators; immunosuppressants; laxatives; agents for treating diseases of the oral cavity and periodontal diseases; myotics; monoamine oxidase inhibitors; mucolytic agents; agents for treating multiple sclerosis; muscle relaxants; mydriatics; narcotic antagonists; NMDA receptor antagonists; oligonucleotides; ophthalmic preparations; accelerating agents; peptides, polypeptides and proteins; polysaccharides; progestogens; prostaglandins; protease inhibitors; respiratory stimulants; sedatives; serotonin uptake inhibitors; sex hormones, including androgens; drugs used to combat smoking; smooth muscle relaxants; smooth muscle stimulants; thrombolytics; tranquilizers; urine acidifiers; medicines for the treatment of urinary incontinence; vasodilators; vasoprotectants; chondroprotectors (chondroitin, glucosamine and their salts, hyaluronic acid and its salts), and their combinations.

The water used as a solvent can be deionized, purified, injectable and of other quality that is approved for oral use.

Instead of fructose, it is allowed to use other sugar approved for use in the food industry.

Guarana extract contains guaranine alkaloid, 5.5% amides, 7% resin, 0.6% saponin and traces of amino acids adenine and guanine, sodium, magnesium, potassium, calcium and vitamin B1, as well as caffeine. Thanks to this unique composition, guarana (guarana extract) is a pronounced stimulator of the nervous system that increases energy metabolism. Guarana extract enhances the production of hormones and digestive enzymes.

The technology is as follows: measure the water in which the following is dissolved: fructose, dry guarana extract, magnesium gluconate, magnesium citrate, vitamin C, citric acid, vitamin B3, vitamin B5, vitamin B6, vitamin B2, sweetener, vitamin B1, vitamin B9, flavoring and preservative. Thoroughly homogenize and bring the remaining amount of water to the desired volume, the resulting solution is thoroughly mixed, the mixture is passed through the homogenizer under high pressure, filtered and poured into containers.

The invention is illustrated by the following examples of industrial implementation in a production environment.

Case Study 1

Water is measured in an amount of 50%, in which, in the following sequence, dissolve fructose 5%, dry guarana extract 19%, magnesium gluconate 0.05%, magnesium citrate 1%, vitamin C 1%, citric acid 5%, vitamin B3 0.01 %, vitamin B5 0.05%, vitamin B6 0.05%, vitamin B2 0.3%, sweetener 0.05% (sodium cyclomat 0.025%, sodium saccharin 0.025%), vitamin B1 0.09%, vitamin B9 0 05, flavor 0.1 and preservative 0.3 (potassium sorbate 0.15%, potassium benzoate 0.15%), thoroughly homogenize and bring the remaining amount of water to the desired volume, the resulting solution is thoroughly mixed, the mixture is passed l through a homogenizer under high pressure, filtered and poured into containers.

Case Study 2

Measure water in an amount of 50%, in which, in the following sequence, dissolve fructose 10%, dry guarana extract 10%, magnesium gluconate 0.03%, magnesium citrate 3%, vitamin C 3%, citric acid 2%, vitamin B3 0.05 %, vitamin B5 0.07%, vitamin B6 0.03%, vitamin B2 0.5%, sweetener 1% (sodium cyclomat 0.5, sodium saccharin 0.5), vitamin B1 0.01%, vitamin B9 0 , 07%, flavor 0.2 and preservative 0.5 (potassium sorbate 0.25, sodium benzoate 0.25). Thoroughly homogenize and bring the remaining amount of water to the desired volume, the resulting solution is thoroughly mixed, the mixture is passed through the homogenizer under high pressure, filtered and poured into containers.

Case Study 3

Water is measured in an amount of 50%, in which, in the following sequence, dissolve fructose 5%, dry guarana extract 19%, magnesium gluconate 0.05%, magnesium citrate 1%, vitamin C 1%, citric acid 5%, vitamin B3 0.01 %, vitamin B5 0.05%, vitamin B6 0.05%, vitamin B2 0.3%, sweetener 0.05%, vitamin B1 0.09%, vitamin B9 0.05, 0.01% lutein, 0, 05% rutin, 0.001% tocopherol mixture, 0.1% bromelain, 0.005% caffeine, 0.1% glutamine, 1% protein complex, 0.1% phytosterol, 0.1% flavor and preservative 0.3% (potassium sorbate 0.15%, sodium benzoate 0.15%). Thoroughly homogenize and bring the remaining amount of water to the desired volume, the resulting solution is thoroughly mixed, the mixture is passed through the homogenizer under high pressure, filtered and poured into containers.

Next, the solution is supplied for packaging in bottles of 11 ml and packaging in a shipping container. The solution in appearance is a dark orange cloudy liquid with a sour-sweet taste and a fragrant odor.

Case Study 4

Water is measured in an amount of 50%, in which, in the following sequence, dissolve fructose 5%, dry guarana extract 19%, magnesium gluconate 0.05%, magnesium citrate 1%, vitamin C 1%, citric acid 5%, vitamin B3 0.01 %, vitamin B5 0.05%, vitamin B6 0.05%, vitamin B2 0.3%, sweetener 0.05%, vitamin B1 0.09%, vitamin B9 0.05%, rutin (flavonoid) 0.1 %, lutein (flavonoid) 0.05%, lycopene (carotenoid) 0.1%, apilak 0.01%, arginine 0.1%, caffeine 0.005%, glutamine 0.1%, bromelain 0.1%, coenzyme Q10 0.03%, potassium iodide 0.002%, chromium picolinate (trace element - chromium) 0.001%, soy isoflavones (hormone-like substances) 0.02%, beta kdisteron (sterols) 0.02% phytosterol 0.1%, 0.1% flavorant and 0.3% preservative (potassium sorbate, 0.15%, 0.15% sodium benzoate). Thoroughly homogenize and bring the remaining amount of water to the desired volume, the resulting solution is thoroughly mixed, the mixture is passed through the homogenizer under high pressure, filtered and poured into containers.

Next, the solution is supplied for packaging in bottles of 11 ml and packaging in a shipping container. The solution in appearance is a dark orange cloudy liquid with a sour-sweet taste and a fragrant odor.

Case Study 5

Water is measured in an amount of 50%, in which, in the following sequence, dissolve fructose 5%, dry guarana extract 19%, magnesium gluconate 0.05%, magnesium citrate 1%, vitamin C 1%, citric acid 5%, vitamin B3 0.01 %, Vitamin B5 0.05%, Vitamin B6 0.05%, Vitamin B2 0.3%, Sweetener 0.05%, Vitamin B1 0.09%, Vitamin B9 0.05%, Carnitine 0.1%, Carnosine 0.03%, drug active substance from the group of immunomodulators (thymogen) 0.03%, flavor 0.1% and preservative 0.3% (potassium sorbate 0.15%, sodium benzoate 0.15%). Thoroughly homogenize and bring the remaining amount of water to the desired volume, the resulting solution is thoroughly mixed, the mixture is passed through the homogenizer under high pressure, filtered and poured into containers.

Next, the solution is supplied for packaging in bottles of 11 ml and packaging in a shipping container. The solution in appearance is a dark orange cloudy liquid with a sour-sweet taste and a fragrant odor.

All ingredients included are known and approved for use. The solution is stored in a dry, dark place at room temperature. Shelf life 3 years.

The solution is recommended to take 1 bottle per day at night. There are no contraindications, with the exception of individual intolerance to the components.

Pharmacological tests for the composition according to example No. 3 were carried out on 30 patients with asthenic manifestations of various origins. The age of the subjects ranged from 21 to 56 years. Among the patients there were 8 men and 22 women. The composition was taken orally, while the drug was prescribed 1 time per day - in the evening; course duration 3 weeks. According to the set of diseases, gender and age, the test and control (took the composition of the prototype) groups are identical.

A comprehensive clinical, laboratory and instrumental study showed safety and the absence of a side effect when applied in effective therapeutic doses.

An advantage in comparison with the composition of the prototype was noted both in terms of efficiency and tolerability in patients with chronic liver and gastrointestinal tract pathologies.

Comparison of the adaptogenic effect of drugs in the forced swimming test under stress conditions (cold water).

In the experiment, we studied the effect of the claimed drug and prototype on the development of the process of fatigue of experimental animals during forced swimming in a special bath at a water temperature of 10 ± 0.5 ° C, while using a stopwatch recorded the maximum swimming time until complete depletion and cessation of swimming.

The experiments were carried out on 48 non-linear male mice, divided into three groups: control and two experimental. In the 1st experimental group, the animals were injected with the claimed drug having the claimed composition, and in the 2nd experimental group the animals were injected with a drug made according to the prototype. The drugs were administered 3 hours before the start of swimming intragastrically through an atraumatic probe in appropriate doses. The data presented in table 1 show that in the 1st and 2nd groups the duration of swimming of animals in cold water increased. Moreover, in the 1st group (the claimed drug), the average swimming time is longer compared with this indicator, in the 2nd group (prototype) more than in the control group.

The results of the studies showed that the claimed drug to a greater extent than the prototype, slows down the development of the process of fatigue and increases the endurance of animals in stressful conditions.

Thus, the claimed drug has a more pronounced adaptogenic effect compared with the prototype

The proposed composition contributed to the reduction of the main symptoms of asthenic syndrome in this category of patients (weakness, fatigue, lethargy, etc.), had a general strengthening effect in case of frequent ARVI diseases.

In addition, tests were conducted on volunteers involved in sports. During the tests revealed: the proposed composition is an effective restorative tool that increases overall and physical performance, accelerates its recovery, slows down fatigue during intense training loads in athletes; reduces the manifestations of sport-specific chronic and acute inflammatory diseases (sinusitis, tendovaginitis), reduces the manifestations of hepatic pain syndrome, has good organoleptic qualities.

Example 1

Patient S.K., age 46 years. Complaints of fatigue, weakness, frequent SARS diseases. Appointed: the proposed composition 1 time per day at night for 11 ml for 2 weeks.

After the course, a decrease in relapses of incidence, an improvement in the general condition, an improvement in appetite and an increase in physical performance were noted.

Example 2

Patient S., 38 years old, Complaints of fatigue, weakness, frequent ARVI diseases. Appointed: the proposed composition according to example 2 1 time per day at night for 11 ml for 2 weeks.

After the course, a decrease in relapses of incidence, an improvement in the general condition, an improvement in appetite and an increase in physical performance were noted.

Example 3

Patient P., 41 years old. Complaints of fatigue, weakness, frequent SARS diseases.

Appointed: the proposed composition according to example 3 1 time per day at night for 11 ml for 2 weeks.

After the course, a decrease in relapses of incidence, an improvement in the general condition, an improvement in appetite and an increase in physical performance were noted.

Thus, the proposed composition normalizes vital activity while weakening the body's defenses, including after illnesses or chronic diseases;

increases the body's resistance to physical and mental stress;

increase the digestibility of vitamin and microelement complexes that enter the body with food;

normalize the antioxidant and antihypoxic defense of the body with insufficient and unbalanced nutrition;

has an increased adaptogenic effect.

Table 1 Group Average swimming time, min Control 4.8 ± 0.1 1 experienced 6.2 ± 0.4 2 experienced 5.8 ± 0.2

Claims (2)

1. The tool has an adaptogenic, tonic and general strengthening effect, containing ascorbic acid, nicotinamide, riboflavin, pyridoxine, characterized in that it further contains dry guarana extract, magnesium gluconate, magnesium citrate, calcium pantothenate, thiamine hydrochloride, folic acid, folic acid, acid, flavoring, sweetener, preservative, water in the following ratios, wt.% to 100%:
Dry guarana extract 1-20 Magnesium Gluconate 0.01-5 Magnesium citrate 0.5-6 Ascorbic acid (Vitamin C) 0.1-5 Nicotinamide (Vitamin B3) 0.001-1 Calcium Pantothenate (Vitamin B5) 0.01-1 Pyridoxine Hydrochloride (Vitamin B6) 0.001-0.5 Riboflavin (Vitamin B2) 0.1-0.5 Thiamine Hydrochloride (Vitamin B1) 0.001-0.5 Folic Acid (Vitamin B9) 0.01-0.5 Fructose 1-27 Lemon acid 0,1-10 Flavoring 0.001-0.5 Sweetener 0.001-1.5 Preservative 0.01-1.0 Water Rest 2. The method of obtaining funds according to claim 1, having adaptogenic, tonic and restorative effect, including dissolving in water in the following sequence: fructose, dry extract of guarana, magnesium gluconate, magnesium citrate, ascorbic acid (vitamin C), citric acid, nicotinamide ( vitamin B3), calcium pantothenate (vitamin B5), pyridoxine hydrochloride (vitamin B6), riboflavin (vitamin B2), sweetener, thiamine hydrochloride (vitamin B1), folic acid (vitamin B9), flavoring and preservative, thoroughly homogenize, and bring the remaining amount of water to the desired volume, the resulting solution is thoroughly mixed, the mixture is passed through a homogenizer under high pressure, filtered and poured into containers.