RU2217138C1 - Composite "vitalizin-2" for prophylaxis of atherosclerosis, cardiovascular diseases and maintaining therapy in viral diseases - Google Patents

Abstract

FIELD: medicine, pharmacy. SUBSTANCE: invention relates to the creature of preparations eliciting complex curative-prophylactic effect and to composite used for prophylaxis of atherosclerosis, cardiovascular diseases and maintaining therapy in viral diseases. Proposed composition consists of rutin, ascorbate and lysine. Except for, composite contain L-lysine monohydrochloride. Composite is made as capsules. Invention provides the creature of composite eliciting broad spectrum of pharmacological effect without symptoms of any adverse effect. EFFECT: valuable medicinal properties of composite. 3 cl, 3 tbl

Description

 The invention relates to medicine, namely to the creation of drugs with a comprehensive therapeutic and prophylactic effect.

 It is known that for the prevention of heart disease, you can take sufficient amounts of antioxidants (like vitamins C and E), minerals and trace elements. It is also known that both mono- and poly-compounds containing vitamins A and C have a beneficial effect in all viral infections, especially if they are used in the initial stages of the disease.

 Known biological composition "Lysivit-S" manufactured by "Irwin Naturals" USA, 10549, W, Jefferson Blvd. Culver City, California 90232, Registration Certificate of the Ministry of Health of the Russian Federation 001539.I.840.03.2000. This tablet formulation contains 500 mg of ascorbic acid (vitamin C). The drug is recommended to be used as a general strengthening agent for the prevention of cardiovascular diseases and as an additional source of vitamin C. Recommended dose for adults: preventive - 2-6 tablets / day, therapeutic - 6-12 tablets / day.

 The disadvantage of this composition is a large amount of ascorbic acid, increased doses of which cause side effects: nausea, vomiting, diarrhea, headache, fatigue, burning in the heart, hot flashes, insomnia, formation of kidney stones (crystalluria), especially in people with chronic renal insufficiency, phlebitis. When using such high doses, teratogenic effects are possible.

In large quantities, ascorbic acid binds zinc and copper ions, increases iron absorption, reduces the content of vitamin B ₁₂ , and affects prothrombin time (decrease) when taking oral anticoagulants. There is evidence that it can lead to an increase in deaths due to thrombophlebitis; enhance crystalluria caused by aspirin; reduce reabsorption of antidepressants and tricyclic antidepressants in the tubules of the kidneys; may distort the results of diagnostic tests: glucose in the urine, ethinyl estradiol, occult blood. With a decrease in the concentration of bilirubin in the blood serum under the influence of ascorbic acid, existing liver lesions can be masked ("Drug Safety", Express Information, Bulletin, 2000, 4, p.15).

 The objective of the present invention is to provide a composition with a wide spectrum of pharmacological action without the manifestation of any side effects of its constituent ingredients and intended for various age groups of the population.

This problem is solved by the fact that the proposed composition for the prevention of atherosclerosis, cardiovascular disease and maintenance therapy of viral diseases, consisting of rutin or quercetin, lysine ascorbate in the following ratio, wt.%:
rutin or quercetin - 20-30
lysine ascorbate - the rest
In addition, the composition may contain L-lysine monohydrochloride in an amount of 8-12 wt.% And be made in the form of capsules.

 The proposed composition is called "Vitalizin-2".

 Quercetin flavonoid is a part of almost all vegetable, medicinal plants, fruits, berries, etc. It is the main component of many flavonoids, including citrus flavonoids, rutin, isperidin, which differ from quercetin in that they have sugar molecules attached to the main part of the molecule.

 Biologically active substances (rutin, catechin, quercetin, citrine, etc.) in combination with vitamin C reduce permeability and increase capillary strength.

 Lysine is an essential aliphatic amino acid. L-lysine reduces serum triglycerides. Contained in avocados, peanuts, beef, pork, fish, shrimp, cheese, etc.

 The above components are widely used in clinical practice with peptic ulcer of the stomach and duodenum, atherosclerosis, rheumatism, to enhance immunity, etc. (Pilat T.L. et al. "Biologically active food additives", M., 2002).

 The composition is prepared by mixing the components, followed by encapsulation in the form of powders or granules.

 The experiments were carried out on white mice or rats.

 1. Acute toxicity.

 Doses of Vitalizin were selected taking into account literature data and optimal therapeutic results identified in preliminary experiments (for ascorbic acid 0.7-1.5 mg / kg / day, rutin 0.3-0.6 mg / kg / day and L-lysine 0.6-1.1 mg / kg / day). The mass of the mixture ranged from 1.6 to 3.2 mg / kg / day.

 White male mice weighing 20.0 ± 2.0 g (n = 50) did not respond to a single oral administration of the composition in the dose range from 100 to 5000 mg / kg / day, which, according to the classification of poisons according to S.D. (1967) classifies Vitalizin as non-toxic.

 2. Cumulation.

 Reception of Vitalizin with food by white male mice with an initial body weight of 20.0 ± 2.0 g in doses 10 (n = 10) and 100 (n = 10) times the maximum prophylactic (control group n = 10), for 60 days did not cause the death of animals, changes in behavior, motor activity, coordination of movements, reflexes of position, appetite, volume of water taken and appearance.

 Thus, Vitalizin does not have a cumulative effect.

 3. Chronic toxicity.

 Vitalizin in doses of 3.2 was added to white outbred rats with an initial weight of 140.8 ± 4.5 g each; 32.0 and 320 mg / kg / day.

 The general condition of the animals, body weight, hematological indices, morbidity and mortality were taken into account. It was established that Vitalizin in a possible prophylactic dose of 3.2 mg / kg / day and up to 100 times a larger dose did not change the behavior of rats, appetite, general condition. In this case, an increase in the mass of animals treated with Vitalizin was recorded.

 In the control group over 60 days of experience, body weight increased by 32%. In the group receiving Vitalizin at a dose of 3.2 mg / kg, the weight gain was 43.8%, in the group receiving Vitalizin at a dose of 32.0 mg / kg, 39% and in the group receiving Vitalizin at a dose of 320 mg / kg - 47.9% (Table 1).

 Thus, long-term oral administration of Vitalizin with food does not cause a negative effect on the body and the death of animals and, in comparison with the control, causes an increase in weight by an average of 7% by the end of the observation.

 At the end of the observation period on the 60th day, the state of the main hematological parameters of the blood of animals was evaluated (Table 2), which actually did not change due to the intake of Vitalizin.

 4. Evaluation of lipid-lowering effects.

 Hyperlipidemia in male rats weighing 150, ± 6.2 g was induced by a single oral administration of ethanol (9 g / kg body weight) in the form of a 30-40% solution. The studied groups of animals received Vitalizin for 10 days, and on the day of ethanol administration 20-30 minutes before its administration. After 6 hours, animals were sacrificed and serum cholesterol was determined (Table 3).

 The introduction of ethanol into the stomach at a dose of 9 g / kg of rat body weight was accompanied by an increase in serum cholesterol by 28% compared with the control, preliminary administration of Vitalizin at a dose of 1.6 mg / g caused a decrease in cholesterol by 7%, and at a dose of 3 , 2 mg / kg - by 12%.

 Thus, the proposed composition Vitalizin is non-toxic, has a lipid-lowering effect, lowers blood cholesterol, does not have cumulative properties.

 Vitalizin has no contraindications.

 The advantage of this composition is the positive effect of the essential amino acid L-lysine and vitamins C and P on protein synthesis, carbohydrate absorption and a negative effect on the formation of atherosclerotic plaques.

Vitalizin can be used:
- for the prevention of atherosclerosis and reduce the permeability of the vascular walls,
- to increase the activity of the immune system after the transfer of infectious diseases,
- to increase the absorption of calcium and the prevention of osteoporosis,
- for the prevention and treatment of influenza and herpes, including genital,
- to strengthen and build muscle mass, increase its elasticity and strength during sports,
- to improve memory,
- to enhance sexual function,
as an additional treatment for the cardiovascular system.

 In the absence of other medical recommendations, take 1 capsule 2 times a day for adults, and 1 capsule per day for children under 12 years of age. With increased physical activity, infectious diseases, the dose can be increased by 2-3 times.

 The proposed composition can be used in the form of dietary supplements as a result of filling the lack of appropriate components to reduce the risk of cardiovascular and viral diseases.

 Experimental and clinical data (on volunteers) confirm that the proposed composition in this quantitative and qualitative ratio provides the indicated spectrum of action.

Claims (3)

1. The composition for the prevention of atherosclerosis, cardiovascular disease and maintenance therapy of viral diseases, characterized in that it contains rutin or quercetin and lysine ascorbate in the following ratio, wt.%: Rutin or Quercetin 20-30 Lysine ascorbate Else 2. The composition according to claim 1, characterized in that it further comprises L-lysine monohydrochloride in an amount of 8-12 wt.%. 3. The composition according to claim 1 or 2, characterized in that it is made in the form of capsules.

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