RU2308961C2 - Agent possessing antioxidant, antitumor, anti-inflammatory, antibacterial, hypotensive, immunomodulating and adaptogenic effect - Google Patents

Abstract

FIELD: medicine, chemical-pharmaceutical industry.

SUBSTANCE: agent possessing antioxidant, antitumor, anti-inflammatory, antibacterial, hypotensive, immunomodulating and adaptogenic effect comprises complex of active substances isolated from aqueous extract of peach leaves and involving flavonoids, tannic substances, coumarins, phenylcarboxylic acids, phenolglycosides, saponins, complex of active substances isolated from plant eyebright (Euphrasia) aqueous extract and involving flavonoids, phenolcarboxylic acids, steroid saponins, glycosides, carotinoids wherein the ratio of complexes is 1:1 or 1;2, or 2;1, and also biologically active components chosen from group: glucose, lactose, ascorbic acid, vitamins A and B, vegetable cellulose and accessory substance taken in the definite ratio. Agent is designated for oral using as drops, powders, tablets, lozenges and capsules. Agent doesn't possess toxicity, mutagenic, embryotoxic and teratogenic effects. Invention can be used in treatment and prophylaxis of inflammatory diseases being among them eyes, tumor processes, cardiovascular system diseases, secondary immunodeficient states and as a general tonic agent. Invention expands spectrum of effect the preparation, provides the development of a novel medicinal preparation based on substances of vegetable origin and possessing antioxidant, antitumor, anti-inflammatory, hypotensive, immunomodulating and adaptogenic effect by combination of two aqueous purified concentrated extracts from peach leaves and plant eyebright (Euphrasia).

EFFECT: improved, enhanced and valuable medicinal effects of agent.

3 cl, 5 tbl, 4 ex

Description

The invention relates to the pharmaceutical industry and can be used for the treatment and prevention of inflammatory diseases, including the eyes, tumor processes, diseases of the cardiovascular system, secondary immunodeficiency states and as a restorative agent.

Known antitumor agent for the prevention and postoperative treatment of malignant neoplasms (its variants), consisting of 2 tinctures and decoction, which include angelica root, vira root, ephedra grass, plantain grass, rootworm root, decopus root, chaga, rosemary, hypericum, immortelle sand, calendula, elecampane root, blueberry leaves, knotweed, horsetail, chicory, rose hips, honey bee (RF Patent No. 2027441, А61К 35/78, 1995).

The disadvantage of this drug is its inefficiency in the treatment of tumor patients in the 4th stage of the disease.

The closest analogue to the present invention is an agent with antitumor and immunomodulatory effects ("Oleksin"), which is an aqueous extract of flowers and leaves of common peach, containing substances of a polyphenolic nature of plant origin (flavonoids, tannins, phenolcarboxylic acids, phenol glycosides, coumarins, saponins and others) (RF patent No. 2132197, АКК 35/78, 1999).

The disadvantage of this tool is that when administered orally, exhibiting significant immunomodulating and adaptagenic activity and effectiveness in the treatment of tumor patients in the 4th stage of the disease, there is a lack of anti-inflammatory, antibacterial and hypotensive activity.

The technical result consists in the creation of a new drug with an expanded spectrum of action, which has antioxidant, immunomodulating, antitumor, anti-inflammatory, antibacterial, hypotensive and adaptogenic effects, based on polyphenolic substances of plant origin by combining aqueous purified concentrated extracts from peach leaves and eyebright plants.

The essence of the invention lies in the fact that the proposed tool with antioxidant, antitumor, anti-inflammatory, antibacterial, antihypertensive, immunomodulating and adaptogenic effects, contains a complex of active substances isolated from an aqueous extract of peach leaves, including flavonoids, tannins, coumarins, phenylcarboxylic acids, phenylcarboxylic acids , saponins, a complex of active substances isolated from an aqueous extract of an eyebright plant, including flavonoids, phenolcarboxylic acids, steroidal saponins, glycosides, carotenoids, while the ratio of the complexes is 1: 1 or 1: 2, or 2: 1, as well as biologically active components selected from the group of glucose, lactose, ascorbic acid, vitamins A and E, plant fiber and auxiliary substances in the following ingredients, wt.%

complex of active substances their peach leaves and eyebright plants 10-50 biologically active component 5-65 Excipients rest

The product is intended for oral use in the form of drops, powders, tablets, dragees, capsules.

The product contains excipients selected from the group of starch, calcium stearate, magnesium stearate, menthol, powdered sugar, starch syrup, sugar grains, purified water.

This wide range of substances provides the complex preparation with a pronounced antioxidant, antitumor, anti-inflammatory, antibacterial, antihypertensive, immunomodulating and adaptogenic activity. In this case, the biologically active components of peach leaves and eyebright plants should be taken in an effective ratio of 1: 1.

To obtain a more pronounced immunomodulating, antitumor and adaptogenic activity, biologically active components of peach leaves and plants, eyelids should be taken in an effective ratio of 2: 1.

To obtain a more pronounced antihypertensive, antibacterial and anti-inflammatory activity, the biologically active components of peach leaves and plants, eyelids should be taken in an effective ratio of 1: 2.

The complex preparation is intended for oral use in the form of drops, powder, tablets, dragees, capsules, powders.

Biologically active components can be added to powders, tablets, dragees, capsules.

As biologically active components, the agent may contain, for example, glucose, lactose, ascorbic acid, vitamins A and E, plant fiber.

The use of biologically active components expands the range of therapeutic effects of the drug. For example, ascorbic acid, vitamins A and E enhance the antioxidant effect of polyphenolic substances and at the same time provide the body with vitamins.

Glucose and lactose are an additional source of energy. Plant fiber, for example, MCC, acts as a carrier sorbent, prolonging and enhancing the action of antioxidant substances that are part of extracts from peach leaves and eyebright plants.

The use of excipients (filler) allows you to create various dosage forms: tablets, dragees, capsules, powders. As excipients, components approved by the Russian Ministry of Health for use in the medical industry should be used.

Example 1. Obtaining the drug in the form of drops by combining aqueous purified concentrated extracts from peach leaves and eyebright plants. The resulting preparation includes:

The complex of substances isolated from a plant of eyebright and peach leaves fifty% Biologically active component 5% Filler - purified water rest

In patients suffering from cancer of the II-IV stages with malignant tumors of various localization (concomitant pathology: atherosclerotic lesion of the cerebral vessels with the phenomena of discirculatory encephalopathy, chronic gastritis, atrophic gastritis, chronic pancreatitis), a complex drug used in the form of drops for 1- 2 months, significantly improves the quality of life of cancer patients (Table 1).

Table 1
Assessment of the quality of life of cancer patients taking the complex drug (assessment according to WHO criteria) WHO criteria for assessing the quality of life of patients Distribution of patients according to WHO criteria, pers. before taking the drug after 2 months of admission Normal physical activity and sleep one 9 Physical activity is reduced, sleep is disturbed, he visits a doctor on his own eleven 5 Bed rest 50% of the daytime, sleep disturbance 2 -

The drug, diluted 10 times, causes complete inhibition of the growth of pathogenic microbial cultures. Staphylococcus strains are most sensitive to the drug (Table 2).

table 2
The effect of the complex drug on the growth of pathogenic bacteria Test culture Dilution of the drug 1/10 1/20 1/100 1/200 1/400 Staphylococcus aureus 0-5 colonies Staphylococcus
epidermidis - - - - 0-7 colonies Pseudomonas aeruginosa 3-10 colonies 1/6 Petri dish solid growth solid growth Streptococcus faecalis 1/3 Petri dish solid growth solid growth Klebsiella pneumoniae solid growth solid growth solid growth solid growth Proteus vulgaris 3-10 colonies 21-32 colonies solid growth solid growth Note: .- "- the complete lack of growth in the culture of microorganisms.

Example 2. Obtaining tablets by granulation and pressing of the components contained in the extracts from peach leaves and eyebright plants, and the biologically active component glucose (lactose).

Tablet composition Content of components in one tablet The complex of substances isolated from the plant euphrasia and peach leaves 0.1 g twenty% Biologically active glucose (lactose) 0.3 g 60% Excipients: starch, calcium stearate or magnesium stearate, menthol an amount sufficient to obtain a tablet weighing 0.5 g

Pills of a pleasant taste, are intended for resorption (absorption of the drug occurs in the oral cavity).

When taking tablets in patients with hypertension (GB), a hypotensive effect is detected. Significantly decreased indicators of average blood pressure, pulse blood pressure, heart rate in both morning and evening hours (table 3). The course of treatment with tablets significantly improves the quality of life of patients with GB: such complaints as headache, dizziness, weakness, palpitations, etc. significantly decrease (Table 4).

Table 3
Dynamics of blood pressure and heart rate in patients with hypertension Indicators Before treatment M ± m After treatment, M ± m R GARDEN, mmHg Art. 149.5 ± 7.4 131.0 ± 4.8 <0.001 DBP mmHg Art. 91.0 ± 4.0 84.5 ± 2.3 <0.001 Heart rate bpm 74.2 ± 2.3 66.6 ± 1.7 <0.001

Table 4
The dynamics of the clinical manifestations of hypertension during treatment with pills (score on a 10-point scale) Symptoms Before treatment After treatment R Headache 9.3 ± 1.0 6.1 ± 0.8 <0.001 Dizziness 6.7 ± 0.7 2.7 ± 0.4 <0.001 Sleep disturbance 8.6 ± 1.4 1.7 ± 0.8 <0.001 Heartbeat 6.6 ± 1.4 4.3 ± 1.0 <0.001 Weakness 9.6 ± 1.5 2.4 ± 1.2 <0.001 Unstable mood 8.4 ± 1.5 4.1 ± 0.9 <0.001

Example 3. Obtaining pills by the method of layer-by-layer rolling of the components contained in extracts from peach leaves and eyebright plants, and biologically active components - vitamins A (beta-carotene), E (tocopherol), C (ascorbic acid).

Dragee composition Contents of the components The complex of substances isolated from the plant euphrasia and peach leaves 0.05 g 10% Biologically active component:
Ascorbic Acid (Vitamin C)
Vitamin A (beta-carotene)
Vitamin E (tocopherol) 0.05 g
0.02
0.005
0.001 5% Excipients:
Powdered sugar
Molasses starch
Granulated sugar an amount sufficient to obtain a dragee weighing 0.5 g

Clinical evaluation showed that dragees are an effective tonic in the prevention and treatment of diseases accompanied by a decrease in the activity of the immune system (Table 5).

Table 5
Changes in the phagocytic activity of neutrophils after taking dragees Number of observations Phagocytic number Phagocytic index % phagocytosis % active phagocytes Ref. level Across
2 weeks Ref. level Across
2 weeks Ref. level Across
2 weeks Ref. level In 2 weeks 60 0.77 1.21 1,60 2.04 47.60 58.1 18.95 32.9 ± 0.05 ± 0.09 ± 0.04 ± 0.09 ± 2.43 ± 2.45 ± 1.84 ± 2.73 p <0.00 p <0.00 p <0.00 p <0.00 one one one one

A comprehensive study of biological properties showed that this tool does not have toxicity, mutagenicity, embryotoxicity, teratogenicity, does not exhibit allergenic properties, i.e. It is a harmless product and can be recommended for long daily use.

The tool stimulates all parts of the immune system: increases the phagocytic activity of macrophages and neutrophils, enhances the production of antibodies, increases the number of T-lymphocytes, protects the immune system from the inhibitory effect of immunosuppressors and stress. In animals with secondary immunodeficiency, when administered orally, the agent raises hemagglutinin titers, the number of antibody-forming cells and the phagocytic activity of neutrophils to the control level to normal.

An important property of the drug is its ability, when administered orally, to have an antitumor, anti-inflammatory, antibacterial, hypotensive and adaptogenic effect.

Claims (3)

1. An agent with antioxidant, antitumor, anti-inflammatory, antibacterial, hypotensive, immunomodulating and adaptogenic effects, characterized in that it contains a complex of active substances isolated from an aqueous extract of peach leaves, including flavonoids, tannins, coumarins, phenylcarboxylic acids, phenylcarboxylic acids, phenylcarboxylic acids, saponins, a complex of active substances isolated from an aqueous extract of an eyebright plant, including flavonoids, phenolcarboxylic acids, steroidal saponins, gly ozides, carotenoids, while the ratio of the complexes is 1: 1 or 1: 2, or 2: 1, as well as biologically active components selected from the group of glucose, lactose, ascorbic acid, vitamins A and E, plant fiber and excipients in the following the content of ingredients, wt.%: complex of active substances their peach leaves and eyebright plants 10-50 biologically active component 5-65 Excipients rest 2. The tool according to claim 1, which is intended for oral use in the form of drops, powders, tablets, dragees, capsules. 3. The tool according to claim 1 or 2, which contains auxiliary substances selected from the group: starch, calcium stearate, magnesium stearate, menthol, powdered sugar, starch syrup, sugar grains, purified water.