RU2357746C2 - Vitalarix cardio biologically active supplement - Google Patents

Abstract

FIELD: pharmacology.

SUBSTANCE: invention relates to chemico-pharmaceutical industry immediately dealing with preparation of biologically active supplements of herbal material ingredients. VITALARIX CARDIO biologically active supplement has antioxidant, angioprotective, immunoregulatory and antithrombotic values. It contains a bioflavonoid complex extracted from larch-tree wood, B₆ vitamin, cobamamide, folic acid, ascorbic acid and a carrier. The bioflavonoid complex contains dihydroquercetin (with a pureness index at least 95%), dihydrokaempferol and naringenin.

EFFECT: preparation of a biologically active supplement that provides for preventive treatment of cardiovascular and inflammatory diseases as well as food, alcoholic and narcotic intoxication compensation, ultimately enabling human life extension.

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Description

The invention relates to food and chemical-pharmaceutical industries, namely to the production of biologically active food additives based on plant materials.

Dihydroquercetin is known as a drug whose healing properties are due to its high antioxidant and P-vitamin activity. Based on these properties, a number of biologically active substances for food have been created, for example, Flukol B, Kapilar and a number of other drugs.

Known drug "Flukol B" containing a native form flavonoid dihydroquercetin obtained from Siberian larch and Daurian larch. The drug has a wide spectrum of action (see TU 9199-002-70205175-04, Registration number No. 77.99.23..3.U.1527.8.04).

Known biologically active food supplement "Capilar" containing 10 mg of dihydroquercetin. The drug is produced by the factory "Diode" (see www.diod.ru).

Closest to the claimed technical solution is known biologically active additive "BIOSKAN-S" and its production method. The additive contains dihydroquercetin 88-92 wt.% And dihydrocampferol 8-12 wt.%. It is obtained by extraction of crushed larch wood with water during heating, cooling and filtering. Evaporation of the extract and its dissolution in an organic solvent followed by extraction of the target product is carried out by column chromatography of a solution on silica gel. Elution is carried out with a water-alcohol solution. The product was evaporated and crystallized from solution. A dietary supplement is not only an effective food supplement, but also provides effective prevention of many diseases by actively increasing the defenses of the human body (see RF patent 21546967 A23L 1/30 A61K 35/78, 1999).

The technical task of the claimed invention is the development of a multifunctional drug with angioprotective, immunoregulatory and antithrombotic effect.

The problem is solved by a biologically active food supplement, including a bioflavonoid complex obtained from larch wood, with an additional content of vitamin B ₆ , cobamamide, folic acid, ascorbic acid and a filler, while the bioflavonoid complex contains dihydroquercetin with a purity of at least 95%, dihydrocampferol naringenin, in the following ratio of components, wt.%:

bioflavonoid complex 5-50 vitamin b ₆ 0.1-0.6 cobamamide 0.02-0.06 folic acid 0.1-0.3 ascorbic acid 10-20 filler rest

The multifunctional properties of the proposed dietary supplement for food "VITALARIX CARDIO" is due to the fact that it blocks the negative effects of the so-called "oxidative stress" in the body and reduces the level of sulfur-containing amino acid homocysteine in the blood. In aerobic organisms, reactions constantly occur with the formation of reactive oxygen species. An excess of them not only participates in such damaging phenomena as the development of inflammatory and destructive processes, tissue hypoxia, fibrous tissue growth, cell proliferation and malignant cell degeneration, but also activates lipid peroxidation of cell membranes, causing fatal free radical avalanches circulating in the body. This condition is called "oxidative stress" and includes a violation of detoxification and excretion processes, metabolic disorders, immune and regenerative plastic tissue failure, forming a free-radical pathology, which is the root cause of many diseases. Hyperhomocysteinemia that occurs during oxidative stress exacerbates arterial and vein damage and has a prothrombotic effect, increasing platelet adhesion and aggregation, increasing thromboxane A ₂ synthesis, and inhibiting prostacyclin vasodilator synthesis.

The drug inhibits lipid peroxidation of cell membranes, inhibits the damaging effect of free radicals, and inhibits premature aging of cells and the development of various diseases. It prevents the destruction of cell membranes, has a capillar-protective effect, and has antithrombogenic activity. Strengthens the walls of blood vessels, improves microcirculation, normalizes cholesterol, triglycerides and homocysteine levels in the blood. Prevents the development of atherothrombosis, reduces the risk of stroke and heart attack. It improves coronary blood flow, myocardial contractility, reduces the zone of heart muscle infarction, and helps to normalize excitability and conduction. Favorably affects the skin, normalizes the synthesis of collagen, elastane in the skin. It has a hepatoprotective effect, has radioprotective activity, reduces the adverse effects on the body of chemotherapy and radiotherapy.

The selection of components for creating the VITALARIX CARDIO food supplement formulation is determined by the ratio of the weight parts, which in total gives the necessary multifunctional effect.

The bioflavonoid complex contains dihydroquercetin with a purity of at least 95%, dihydrocampferol and naringenin.

The complex was isolated from larch wood and is a highly purified flavonoid dihydroquercetin and its biogenetic precursors of the same chemical structure of the same type: dihydrocampferol and naringenin.

In the Methodological Recommendations of the Ministry of Health of the Russian Federation MP 2.3.1.1915-04 (Recommended levels of consumption of food and biologically active substances), the adequate and upper allowable levels of their consumption per day are, respectively:

dihydroquercetin 25 mg and 100 mg dihydrocampferol 25 mg and 100 mg naringenin 100 mg and 300 mg

The aforementioned requirements for the purpose and purity of dihydroquercetin correspond to a bioflavonoid complex with the trade name "Vesalarix" (2,3-dihydroquercetin), TU 9354-001-33073072-06, SEZ No. 77.99.03.003.T.000678.04.06 dated 04/11/2006. , State registration certificate No. 77.99.23.3.U.3270.4.06 dated April 12, 2006 at the Federal Service for Supervision of Consumer Rights Protection and Human Well-Being.

A bioflavonoid complex with a dihydroquercetin purity of at least 95 wt.% Is produced by extraction of crushed larch wood with an aqueous-alcoholic solution by heating, vacuum-pulse exposure, cooling, filtering and drying of the target product at temperatures of the above processes not higher than 40 ° С.

The main difference from similar products from other manufacturers is the low-temperature method for the preparation of dihydroquercetin while maintaining the native form of its compound, which determines the pronounced biological activity of this flavanoid, which has a crystalline hydrate form.

The drug is a fine crystalline powder from light yellow to white, odorless, slightly bitter taste.

Examples of recipes for dietary supplements "VITALARIX CARDIO"

recipe 1 No. p / p Name of ingredients The content of ingredients, wt.% one bioflavonoid complex 5 2 vitamin b ₆ 0.6 3 Cobamamide 0.02 four folic acid 0.3 5 vitamin C twenty 6 Filler 74.08 recipe 2 No. p / p Name of ingredients The content of ingredients, wt.% one bioflavonoid complex thirty 2 vitamin b ₆ 0.5 3 Cobamamide 0.05 four folic acid 0.2 5 vitamin C fifteen 6 Filler 54.25 recipe 3 No. p / p Name of ingredients The content of ingredients, wt.% one bioflavonoid complex 40 2 vitamin b ₆ 0.6 3 Cobamamide 0.06 four folic acid 0.3 5 vitamin C twenty 6 Filler 39.04 recipe 4 No. p / p Name of ingredients The content of ingredients, wt.% one bioflavonoid complex fifty 2 vitamin b ₆ 0.1 3 Cobamamide 0,03 four folic acid 0.3 5 vitamin C 17 6 Filler 32.57

The claimed composition of dietary supplements for food "VITALARIX CARDIO", including vitamin preparations of group B (vitamin B ₆ cobamamide, which is a coenzyme form of vitamin B ₁₂ ), group C, folic acid and a bioflavonoid complex, was created not by a simple selection of known drugs with known properties, but in strictly scientifically based combination with the manifestation of a synergistic effect.

Pharmacopeia article FS 42-2399-94 of 07.29.1996 acts on dihydroquercetin. It has been included in the encyclopedia of medicines since 2003 (radar station, 10th issue), after a large complex of various clinical trials (pharmaceutical group: 8.2). Pharmacological action - antioxidant, angioprotective, regenerating, detoxifying, decongestant.

It inhibits lipid peroxidation of cell membranes, prevents the damaging effect of free radicals, and inhibits premature aging of cells and the development of various diseases.

Prevents the destruction of cell membranes, has a capillaroprotective effect. Strengthens the walls of blood vessels (including capillaries), improves microcirculation, normalizes cholesterol and triglycerides in the blood. It prevents the development of atherosclerosis, reduces the risk of stroke and heart attack.

Helps maintain the functions of the immune system, has an antitoxic effect. It has gastroprotective activity: it stimulates the regeneration of the gastric mucosa, prevents the development and promotes the healing of stomach ulcers and duodenal ulcers. It has a hepatoprotective (antitoxic) effect, has a radioprotective activity - reduces the adverse effects on the body of chemotherapy and radiotherapy.

Indications. Bronchopulmonary diseases, including acute pneumonia, chronic obstructive bronchitis, bronchial asthma (infectious form) in the acute stage; as part of complex therapy: coronary heart disease (unstable angina), atrial arrhythmia (as part of combination therapy).

After the discovery of A. St. Gyordi in 1936, bioflavonoids with high biological activity were shown to reduce the severity of vitamin C deficiency, reduce the permeability and fragility of capillary blood vessels (possess P-vitamin activity). Among them, the undisputed leader is the flavonoid - dihydroquercetin.

Vitamin C is involved in the regulation of redox processes, carbohydrate metabolism, blood coagulation, tissue regeneration, in the formation of steroid hormones, increases the body's resistance and partially reduces vascular permeability. However, it does not have powerful P-vitamin activity (P-vitamin activity is the effect on blood vessels in two independent parameters - strengthening the walls of blood vessels, increasing their elasticity, and also reducing permeability for oxidized lipids, which form atherosclerotic when they enter the bloodstream on the walls of blood vessels plaques).

Therefore, in the interaction of dihydroquercetin (DHA) and vitamin C, a synergistic effect occurs when DHA releases vitamin C from its unusual functions and the body's need for vitamin C decreases, and their combined effect (biological activity) on the human body increases dramatically. There are reports that the activity of vitamin C when interacting with vitamin P increases up to 20 times. According to the Institute of Neurology of the Russian Academy of Medical Sciences, dihydroquercetin, in addition to affecting the walls of blood vessels, improves the rheological properties of blood, i.e. reduces its viscosity, increases the elasticity of red blood cells. This allows them to penetrate into the smallest capillaries, delivering oxygen to any organs and tissues, while the aggregation of red blood cells and platelets decreases. Due to its capillary-strengthening (vessels that are elastic and strong are more capable of expansion) and diuretic properties, the drug steadily reduces blood pressure, eliminates headache, tinnitus, asthenia, and reduces the possibility of repeated relapses of hypertension.

Academician Chazov E.I. stated that the main epidemic of the century is not atherosclerosis, but atherosclerosis. Atherothrombotic disease, the main complications of which are myocardial infarction and cerebral stroke, takes millions of lives.

It is known that due to the complex of vitamins B ₆ , coenzyme of vitamin B ₁₂ - cobamamide and folic acid - the level of homocysteine in the blood decreases, which counteracts the formation of blood clots, which clog the vessels of the brain, heart and other organs and cause their death. Since thrombosis occurs against the background of atherosclerotic changes in the walls of blood vessels, to prevent their atherosclerotic lesions, the basis of the proposed dietary supplement VITALARIX CARDIO is a complex of ingredients of bioflavonoids with P-vitamin activity and vitamin C (ascorbic acid). These ingredients are synergists, and in combination with the above vitamins, they, in addition to antioxidant anti-atherosclerotic, angioprotective and immunoregulatory effects, create an antithrombotic effect. In connection with the foregoing, the proposed dietary supplement is an effective “cleaner” of blood vessels, and most importantly, with its regular use, the risk of the formation of new blood clots will be reduced.

A deficiency of micronutrients that are not synthesized and do not accumulate in our body is typical for all sectors of society, regardless of income level, due to the fact that the energy consumption of a modern person is reduced to 2000-2300 Kcal and a micronutrient deficiency for a person in the diet is inevitable. Therefore, the primary task should be to expand the list of consumption of trace elements, micro- and macronutrients, minor non-food components (indoles, flavonoids, isoflavones) with high biological activity to provide adaptive capabilities of the body to confront the above-mentioned problems that impede the improvement of human life.

VITALARIX CARDIO, a dietary supplement based on dihydroquercetin, contributes to the prevention of the following diseases: cardiovascular and inflammatory, as well as to neutralize food, alcohol and drug poisoning. This will prevent the influence of negative risk factors on socially dangerous diseases of arterial hypertension and coronary heart disease, which will improve the quality and increase the life expectancy of the population.

Claims (1)

A dietary supplement with an angioprotective, immunoregulatory and antithrombotic effect, including a bioflavonoid complex derived from larch wood, characterized in that it additionally contains vitamin B ₆ , cobamamide, folic acid, ascorbic acid and a filler, and bioflavonoid acid does not contain less than 95%, dihydrocampferol and naringenin in the following ratio of components, wt.%:
bioflavonoid complex 5.0-50.0 vitamin b ₆ 0.1-0.6 cobamamide 0.02-0.06 folic acid 0.1-0.3 vitamin C 10.0-20.0 filler rest