RU2390347C2 - Immunomodulatory and antioxidant drug - Google Patents

Abstract

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to chemical-pharmaceutical industry. An immunomodulatory and antioxidant drug characterised by the fact that it represents Psephellus herb extract containing polyphenols in amount 8-10 mg/ml, polyacetylenes in amount 0.03-0.05 mg/ml, prepared in the relation raw material:extractant 1:5, during 7 days in absence of light, and the extractant is chosen from the group: 40% of alcohol, 5-75% of glycerine, 5-100% of honey and water. The drug can be presented as a capsule, a tablet, a powder, a pill, a dragee, granules, a sachet, gel, paste, syrup, an emulsion, a suspension, a solution, and a chewing gum. The drug can be applied for immune system correction in the patients untreatable with common medications.

EFFECT: production of the immunomodulatory and antioxidant drug.

2 cl, 1 tbl

Description

The invention relates to medicine, namely to herbal medicines with immunomodulating and antioxidant effects.

An immunotropic drug (medicine) is known, which is honey obtained by feeding a composition to bees, including monofleur honey of the family Asteraceae, containing 3-hydroxy-flavone-silybin, extract of flavonoid fractions of propolis, licorice extract, calendula extract, St. John's wort perforated in a certain ratio. The drug induces endogenous α- and β-interferon, has anti-allergic, immunomodulating, antioxidant, anti-inflammatory, antibacterial effects (RU 2241476, 2004).

It is known a medicine containing fat-free fruits of milk thistle, which additionally includes the biomass of the microalgae spirulina taken in a certain ratio. The tool allows you to get a pronounced hepatoprotective effect in comparison with the closest analogue due to the optimal combination of hepatoprotective, immunocorrective and antioxidant properties of substances and their synergism. (RU 2162705, 2001).

A drug is known that has an immunomodulating and antioxidant effect, containing an alcohol-containing tincture of plant material from a mixture of equal amounts of grass and purple echinacea inflorescences, coltsfoot, small-leaved linden flowers and licorice roots (RU 2318530, publ. 2008.03.10, prototype).

The disadvantages of the known drugs are low digestibility, the preservation of a significant amount of free radicals in the patient’s blood, mild stimulation of the humoral immune response tested in laboratory animals, a narrow range of effective use, since the levels of catalase and glutathione peroxidase increase slowly and inadequately.

The technical task of the present invention is the creation of an effective drug with immunomodulating and antioxidant effects, as well as expanding the arsenal of drugs with immunomodulating and antioxidant effects.

The technical result, which provides a solution to the problem, is to increase the immunological and antioxidant activity with a significant increase in the levels of catalase and glutathione peroxidase, normalization of the content of free radicals in the blood of the patient.

The essence of the invention lies in the fact that the drug having immunomodulatory and antioxidant action is an extract of the herb Psefellus, including polyphenols in the amount of 8-10 mg / ml, polyacetylenes in the amount of 0.03-0.05 mg / ml, obtained in the ratio raw materials: extractant 1: 5 for 7 days without access of light, while the extractant is selected from the group: 40% alcohol, 5-75% glycerin, 5-100% honey and water.

In special cases, the implementation of the tool can be made in the form of a capsule, tablet, powder, pill, dragee, granule, sachet, gel, paste, syrup, emulsion, suspension, solution, chewing gum.

In this case, the extract is a liquid dosage form, which is an extract from medicinal raw materials obtained without heating and removing the extractant.

The mechanism of action of the claimed funds is implemented as follows. Free radicals cause irreversible damage to the genetic apparatus, vital proteins and membrane lipids, which is manifested in the formation of large quantities of hydrogen hydroperoxide. Polyphenols stabilize cell membranes, block free radicals of both exogenous and endogenous origin; inhibit the aging process of the skin of cells, cornea, myocardium and other organs.

Due to the capillary-stabilizing properties of the components of the agent associated with the antioxidant effect, the lipooxygenase pathway of arachidonic acid metabolism is blocked, the synthesis of leukotrienes, serotonin and other inflammatory mediators is reduced, and the antulucerogenic effect and radioprotective activity are manifested (after X-ray and gamma irradiation). The cardioprotective properties of the drug are due to an increase in the energy supply of cardiomyocytes due to the antioxidant effect and improved blood circulation. Polyphenols have the property of restoring the function of the p53 gene in cancer cells. It is the mutations of the p53 gene, which normally causes cells that have “rolled” to the cancer path to commit suicide (apoptosis), are responsible for the occurrence of 50-60% of cases of neoplasms. Rehabilitation of the p53 gene helps in the treatment of cancer of the breast, prostate, colon, lung, brain, lymphosarcoma, lymphogranulomatosis and other oncological diseases. After oral administration, the sum of polyphenols and polyacetylene in the indicated ratio is well absorbed and exhibits its immunomodulating and antioxidant effect to the greatest extent.

The study of the immunostatus was performed on volunteer patients before and after treatment. Patients with a secondary immunodeficiency state with an allergic syndrome, confirmed by immunological analyzes, were selected. In addition, patients were assessed for the activity of antioxidant enzymes (in particular, catalase levels specific for high concentrations of hydrogen hydroperoxide and glutathione neoxidase, which breaks down various hydroperoxides, by their conversion to water).

The study of the impact of the claimed funds on the immunostatus was performed on 59 patients (men and women) who had the following diseases:

- hypertension - 14;

- erysipelatous inflammation - 3;

- erosive and ulcerative diseases of the oral mucosa - 7;

- acne - 5;

- psoriasis - 4;

- neurocirculatory dystonia - 8;

- hemorrhagic diathesis - 6;

- bronchial asthma - 12.

A course of treatment with the use of the claimed funds with immunomodulating and antioxidant effects has been applied. The course of treatment was carried out for 3 weeks. At the beginning and at the end of the tests, patients were sampled for analysis.

18 patients received an extract of plant material containing psefellus herb extract on 40% alcohol, including polyphenols in an amount of 8 mg / ml, polyacetylenes in an amount of 0.05 mg / ml.

18 patients received an extract of plant material containing psefellus herb extract on 5-75% glycerin, including polyphenols in an amount of 9 mg / ml, polyacetylenes in an amount of 0.04 mg / ml.

Eight patients received plant extract containing 5% honey and water psefellus herb extract in a ratio of 1: 5, respectively, including polyphenols in an amount of 8 mg / ml, polyacetylenes in an amount of 0.03 mg / ml.

7 patients received plant extract containing 50% honey and water extract of psefellus herb in a ratio of 1: 5, respectively, including polyphenols in an amount of 9 mg / ml, polyacetylenes in an amount of 0.4 mg / ml.

8 patients received plant extract containing 100% honey and water extract of psefellus herb in a ratio of 1: 5, respectively, including polyphenols in an amount of 10 mg / ml, polyacetylenes in an amount of 0.05 mg / ml.

For administration, the agent according to the present invention is preferably diluted in a ratio of 10 drops per 0.5 cup of water for administration for 5 days, 2 times a day, or used in a dosage form suitable for oral administration from the group of capsules, tablets, powders, pills, dragees, granules, sachets, gels, pastes, syrups, emulsions, suspensions, solutions, dental infusion, chewing gum.

As a result of treatment, clinical syndromes of diseases decreased and disappeared, a pronounced anti-inflammatory effect and an increase in nonspecific resistance of the body were observed, the skin condition improved, edema and hyperemia disappeared in those patients in whom they were observed before treatment. In general, the result of the use of the drug was expressed in an increase in the body’s anti-infective potential, a decrease in the process of inflammation and infectious toxic stress with a statistically significant increase in the activity of antioxidant defense enzymes: on average, catalase from 476 to 986 mmol / mg, glutathione peroxidase from 4.33 to 4.87 u / l

The results of the impact of the proposed drug on the phagocytic activity of neutrophils in patients are shown in the table.

Number of observations Phagocytic number Phagocytic activity of neutrophils Ref. level In 3 weeks Ref. level In 3 weeks 59 0.67-0.81 1.07-1.22 25-30 65-78

The number of circulating immune complexes decreased in the vast majority of patients (91.5%), which indicates a favorable course of diseases related to immunity.

The claimed drug in the vast majority of patients provides an increase in the content of T-suppressors with a simultaneous decrease in the number of T-helpers in the blood of patients, which allows you to normalize the immunoregulatory index (IRI). The consequence of this is an increase in the functional activity of almost all parts of the body's immune defense. Clinically, all patients noted an improvement in overall health, the disappearance of increased fatigue.

In experiments on laboratory animals, the stimulating effect of the compound on myeloid activity and the primary humoral response (evaluated by the number of IgM antibody-forming cells) and the depressive effect on the cellular immune response proliferation of spleen cells was revealed.

Thus, as a result of the application of the proposed tool, it was revealed that all the altered patient indices approached the normal range, which is important for a long-term favorable prognosis of the disease and indicates a general increase in the immunoreactivity of the patient’s body. The tool can be used both for parenteral and oral, external and local use (intranasal, conjunctival, vaginal).

When using a drug with immunomodulating and antioxidant effects, the result obtained is associated both with the regulation of subcortical-cortical bioelectric processes, the exchange of neurotransmitters, the normalization of microcirculatory disorders, which contributes to the correction of the function of the endocrine and immune systems, and due to the parallel increase in the activity of monocytic-macrophage cells system.

The inventive tool having immunomodulatory and antioxidant action is an effective restorative agent in the prevention and treatment of diseases accompanied by a decrease in the activity of the immune system, can be successfully used to correct the immune system in patients who are difficult to treat by conventional means.

In this case, there is an increase in the resistance and adaptive capabilities of the body, which underlies the processes of self-healing of impaired homeostasis.

Claims (2)

1. A drug having immunomodulatory and antioxidant action, characterized in that it is an extract of the herb Psefellus, including polyphenols in an amount of 8-10 mg / ml, polyacetylenes in an amount of 0.03-0.05 mg / ml, obtained in the ratio raw materials: extractant 1: 5 for 7 days without access of light, while the extractant is selected from the group: 40% alcohol, 5-75% glycerin, 5-100% honey and water. 2. The medicine according to claim 1 is in the form of a capsule, tablet, powder, pill, dragee, granule, sachet, gel, paste, syrup, emulsion, suspension, solution, chewing gum.