RU2311916C2 - Agent having antianemic, immunomodulating and adaptogenic actions (variants) - Google Patents

Abstract

FIELD: chemical-and pharmaceutical industry.

SUBSTANCE: claimed agent contains DNA sodium salt isolated from bovine testis and is useful in peroral application in form of powder, tablets, pellets, and capsules for treatment and prophylaxis of anemia, secondary immunodeficit conditions and as bracing agent. Agent may additionally contains biologically active components and filler.

EFFECT: effective and convenient agent having antianemic, immunomodulating and adaptogenic actions.

3 cl, 3 ex, 6 tbl

Description

The invention relates to the pharmaceutical industry and can be used for the treatment and prevention of anemia, secondary immunodeficiency states and as a general strengthening agent.

Known tool - polydane (sodium nucleospermate) - 1.5% solution for injection, (registration number 95/292/8), stimulating leukopoiesis, containing a mixture of sodium salts of polychlorohydrates of DNA derivatives and RNA isolated from sturgeon milk. (Radar, M., 2002, p. 689)

Polydan is an injectable drug that restores white blood counts (leukopenia) reduced as a result of chemotherapy of tumors with cytostatic agents.

The disadvantage of this tool is that the preparation uses insufficiently purified components - fragments of nucleic acids isolated from the tissues of organisms that are evolutionarily far removed from the human class (fish), which are injected. With their introduction, a number of negative aspects are noted: significant pain syndrome, pyrogenic effect; the injection method of administration carries the potential risk of infection, the need for the participation of medical staff and the creation of aseptic conditions for the administration of the drug.

The closest analogue to the proposed invention is a tool with a leukopoietic and immunomodulating property - Derinat. (Radar, M., 2002, p. 282)

Derinat is a sodium salt of DNA with a molecular weight of 270-500 kDa with a small content of impurities of less than 1%; it is also released from sturgeon milk. Derinat also normalizes reduced hematopoiesis, but additionally exhibits an immunomodulatory effect, it is used in the form of a 1.5% solution for intramuscular administration.

The disadvantage of this tool is that with parenteral administration there is a significant pain syndrome, pyrogenic effect, the potential danger of infection, the need for medical staff and the creation of aseptic conditions for the administration of the drug.

The technical result consists in expanding the spectrum of action of the drug, creating a new drug with antianemic, adaptogenic and immunomodulating activity, eliminating the risk of infection and ease of use by the possibility of oral administration, without the participation of medical staff.

The essence of the invention lies in the fact that the tool contains sodium salt of DNA isolated from mammalian tissues - bovine testes, which is intended for oral use in the form of tablets, dragees and capsules for the treatment and prevention of anemia, secondary immunodeficiency states and increased performance.

A group of inventions is proposed, united by a single inventive concept.

An agent having an antianemic, immunomodulating, adaptogenic effect, containing sodium salt of DNA from animal tissues, microcrystalline cellulose and excipients is proposed in the following ratio of ingredients in g per 1 tablet weighing 0.2 g:

sodium salt of DNA 0.05 microcrystalline cellulose 0.149 Excipients rest.

The tool as auxiliary substances contains starch, calcium stearate or magnesium stearate.

An agent having an antianemic, immunomodulating, adaptogenic effect, containing sodium salt of DNA from animal tissues, cyanocobalamin (vitamin B ₁₂ ), folic acid and excipients in the following ratio of ingredients in g per 1 dragee weighing 0.5 g is proposed.

sodium salt of DNA 0,025 cyanocobalamin (vitamin B ₁₂ ) 0.00002 folic acid 0.0001 Excipients rest.

The tool as excipients contains powdered sugar, starch syrup and sugar grains.

It is also proposed a tool with antianemic, immunomodulating, adaptogenic action, containing sodium salt of DNA from tissues of animal origin, glucose and excipients in the following ratio of ingredients in g per 1 capsule:

sodium salt of DNA 0.3 glucose 0.3

The use of biologically active components expands the range of therapeutic effects of the drug. For example, vitamins B ₁₂ and folic acid enhance antianemic properties, glucose enhances adaptogenic activity. Plant fiber, for example, MCC, acts as a carrier sorbent, prolonging and enhancing the action of the agent. The use of various dosage forms (tablets, dragees, capsules, powders, etc.) determine the convenience of the drug.

Example 1. Obtaining tablets.

Tablet composition Content of components in one tablet A component containing sodium salt of DNA 0.05 g 25 biologically active component: microcrystalline cellulose 0.149 g 75 Excipients: starch, calcium stearate or magnesium stearate enough to get a tablet weighing 0.2

Every day for a month, 22 women with anemia and asthenovegetative syndrome received 1 tablet 2 times a day. Other medicines were not prescribed during this period.

The number of red blood cells, white blood cells, and hemoglobin concentration significantly increased and reached the normal level (Tables 1, 2)

Table 1
Changes in hemograms when taking tablets Indicators Baseline After 4 weeks Hemoglobin, g / l 115.3 ± 2.6 124.8 ± 3.0 * Red blood cells, × 10 ¹² / l 3.98 ± 0.1 4.22 ± 0.08 * * - p <0.05 - according to student t-test relative to the initial level.

Table 2 Changes in physiological parameters when taking tablets

Blood pressure, mmHg Heart rate, beats / min Respiratory rate, breathe. movement / min Exodus. 1 month Exodus. 1 month Exodus. 1 month 118.4 ± 3.9 / 70.7 ± 2.4 113.4 ± 2.4 / 69.3 ± 1.4 81.8 ± 1.9 75.7 ± 1.2 * 17.7 ± 0.5 14.2 ± 0.5 ** * - p <0.05; ** - p <0.01 according to student t-test relative to the initial level.

Example 2. Getting a dragee.

Structure Contents of the components Sodium DNA Container 0.025 g 5% Biologically active components:
Cyanocobalamin (Vitamin B ₁₂ )
Folic acid 0.00012 g
0.00002 g
0.0001 0.02% Filler:
Powdered sugar
Molasses starch
Granulated sugar an amount sufficient to obtain a dragee weighing 0.5 g

Every day for a month, 18 women with signs of anemia and asthenovegetative syndrome received 2 tablets 2 times a day. Other medicines were not used during this period.

The test results are presented in table 3, 4.

Table 3
The effect of dragee intake on hemogram values Indicators Baseline After 4 weeks Hemoglobin, g / l 113.3 ± 5.5 122.9 ± 4.29 * Red blood cells, × 10 ¹² / l 3.91 ± 0.17 4.29 ± 0.09 * * - p <0.05 according to student t-test relative to the initial level. Table 4
Changes in the phagocytic activity of neutrophils when taking dragees Indicators Baseline After 1 month The percentage of phagocytosis 38.83 ± 2.43 50.83 ± 3.77 ** Phagocytic index 1.48 ± 0.07 1.59 ± 0.05 Phagocytic number 0.57 ± 0.04 0.83 ± 0.08 ** Abs. the number of captured phagocytosis objects 1786 ± 172 2070 ± 245 ** - p <0.01 according to student t-test relative to the initial level.

Example 3. Obtaining capsules.

Structure The ratio of components in one capsule weighing 0.6 g Sodium DNA Container 0.3 g fifty% Glucose 0.3 g fifty%

Tablets, dragees, powder from capsules significantly increase the performance of animals (Tables 5, 6).

Table 5
The effect of the drug on the strength endurance of mice Forms of the drug Number of animals Retention time on a horizontal bar, sec The control 9 12.22 ± 2.31 Powder 10 33.10 ± 5.82 ** Pills 10 36.50 ± 5.22 *** Jelly beans 9 29.67 ± 6.93 * * - p <0.05; ** - p <0.01; *** - p <0.001 according to student t-test relative to control. Table 6
The effect of the drug on the power stability and muscle endurance of mice Experience Options The mass of the held weights, g Swimming time, sec The control 36.18 ± 3.32 465.67 ± 73.91 (n = 11) (n = 6) Powder 44.50 ± 1.62 * 778.20 ± 158.77 * (n = 12) (n = 5) • - p <0.05 according to student t-test relative to control.

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 harmless 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 antibody production; increases the number of T-lymphocytes; protects the immune system from the inhibitory effects of immunosuppressors and stress; with secondary immunodeficiencies when administered orally, it increases hemagglutinin titers, the number of antibody-forming cells and the phagocytic activity of neutrophils to normal. Derinat, when administered intramuscularly at the same dose, does not restore these parameters to normal levels.

An important property of the drug is its ability to provide an antianemic effect when administered orally. It has been shown in animals that the drug has the ability to increase the reduced number of red blood cells and the concentration of hemoglobin to normal, increases bone marrow cellularity, and levels lymphopenia.

When administered orally, the drug contributes to a significant increase in muscle and strength endurance of animals.

With the participation of a group of volunteers, the immunomodulating, erythropoestimulating and adaptogenic activity of the drug used in the form of tablets and dragees was confirmed. The drug significantly increases mental and physical performance.

Claims (5)

1. The tool has an antianemic, immunomodulating, adaptogenic effect, characterized in that it contains the DIC sodium salt isolated from bovine testes, microcrystalline cellulose and excipients in the following ratio of ingredients in g per 1 tablet weighing 0.2 g: sodium salt of DNA 0.05 microcrystalline cellulose 0.149 Excipients rest 2. The tool according to claim 1, where as auxiliary substances contains starch, calcium stearate or magnesium stearate. 3. A tool with antianemic, immunomodulating, adaptogenic action, characterized in that it contains sodium salt of DNA isolated from bovine testes, cyanocobalamin (vitamin B ₁₂ ), folic acid and excipients in the following ratio of ingredients in g per 1 dragee weighing 0 5 g: sodium salt of DNA 0,025 cyanocobalamin (vitamin B ₁₂ ) 0.00002 folic acid 0.0001 Excipients rest 4. The tool according to claim 3, where as auxiliary substances contains powdered sugar, starch syrup and sugar grains. 5. A tool with antianemic, immunomodulatory, adaptogenic action, characterized in that it contains sodium salt of DNA isolated from bovine testes and glucose in the following ratio of ingredients in g per 1 capsule: sodium salt of DNA 0.3 glucose 0.3