RU2560518C1 - Agent possessing lymphokinetic activity - Google Patents

Abstract

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry, particularly to an agent possessing lymphokinetic activity. The agent possessing lymphokinetic activity contains dihydroquercetin and arabinogalactan in ratio (weight parts) 1:5.

EFFECT: agent described above possesses the synergic lymphokinetic activity.

1 tbl, 4 ex

Description

The invention relates to medicine, specifically to pharmacology, and relates to agents used to treat diseases associated with difficulty in lymphatic drainage.

Known drugs that increase the outflow of lymph: flavonoids - dihydroquercetin, hesperidin + diosmin [1, 2].

Closest to the claimed tool (prototype) is dihydroquercetin [3]. The disadvantage of the prototype is the lack of activity as a lymphokinetic agent.

The purpose of the invention is an increase in lymphokinetic activity.

This goal is achieved by creating a tool containing dihydroquercetin and arabinogalactan in a ratio (parts by weight) of 1: 5.

New in the invention is the additional inclusion of arabinoglactan and the ratio (parts by weight) of dihydroquercetin and arabinogalactan 1: 5.

Dihydroquercetin is a flavonoid with antioxidant, hypolipidemic, hepatoprotective, capillary protective, lymphokinetic and decongestant activity [2].

Arabinogalactan is a polysaccharide with immunomodulating, hepatoprotective and antioxidant activity [4].

The poor solubility of dihydroquercetin in water and the low dissolution rate limits its use in medical practice [5, 6]. In turn, arabinogalactan is able to increase the solubility of drugs (drugs) and their pharmacological activity [7, 8]. The use of a complex of drugs and arabinogalactan has been shown to be effective when used in a ratio (parts by weight) of 1: 5 [9]. In addition, it was shown that when dihydroquercetin is used in a composition with arabinogalactan in a ratio of 1: 5, the ability of dihydroquercetin to enhance microcirculation increases [10].

The use of dihydroquercetin and arabinogalactan-based agents as a lymphokinetic agent is not described.

Previously proposed tool has not been used.

Fundamentally new in the present invention is that the lymphokinetic agent contains dihydroquercetin and arabinogalactan 1: 5.

The technical result of the invention is the expansion of the arsenal of funds with lymphokinetic activity.

The essential features showed new properties in the claimed combination, which are not explicitly derived from the prior art and not obvious to a specialist.

An agent containing dihydroquercetin and arabinogalactan can be used to treat diseases associated with difficulty in lymph outflow.

Thus, this technical solution meets the criteria of the invention of "novelty", "inventive step", "industrially applicable".

New properties of the agent containing dihydroquercetin and arabinogalactan (hereinafter referred to as the agent) were discovered experimentally.

Experiments on the study of the lymphokinetic activity of the drug were carried out on 24 Wistar male rats weighing 250-350 g. Lymphokinetic activity was determined by the rate of lymph outflow (μl / kg · min) released through the puncture of the milky cistern (cistema chyli) in 10 min. An hour before the experiment, dihydroquercetin at a dose of 50 mg / kg, arabinogalactan at a dose of 250 mg / kg and a drug at a dose of 300 mg / kg (dihydroquercetin 50 mg / kg + arabinogalactan 250 mg / kg) were administered intragastrically once as a suspension in purified water. The animals of the control group were injected with an equivalent volume of purified water.

The collected lymph was stabilized with heparin at a final concentration of 50 U / ml [11].

Statistical processing was performed using the software package "Statistica 6.0". The mean value, standard error was calculated, and the Mann-Whitney U test was used to identify intergroup differences.

The results of the study of lymphokinetic activity are presented in examples 1-4 and the table.

Example 1. In control animals, the outflow rate of lymph through a lacteal tank puncture was 72.7 ± 1.3 μl · kg / min (table, Control).

Example 2. In the group of animals treated with dihydroquercetin at a dose of 50 mg / kg, the outflow rate of lymph was 81.0 ± 3.4 μl · kg / min, which significantly exceeded the value of the indicator in control animals by 11% (table, DHA) .

Example 3. In the group of animals treated with arabinogalactan at a dose of 250 mg / kg, the lymph outflow rate was 82.3 ± 5.4 μl · kg / min, which was 13% higher than the value of the control animals (table, AH).

Example 4. In the group of animals treated with the drug at a dose of 300 mg / kg (dihydroquercetin 50 mg / kg + arabinogalactan 250 mg / kg), the lymph outflow rate was 99.8 ± 4.2 μl · kg / min, which significantly exceeded the value the indicator in the control group and in the groups receiving dihydroquercetin and arabinogalactan, by 37, 23 and 21%, respectively (table, Tool).

Table The effect of a single intragastric administration of dihydroquercetin (DHA), arabinogalactan (AH) and funds on the rate of lymph outflow in rats Group (n = 6) The rate of lymph outflow, μl · kg / min The control 72.7 ± 1.3 DHA, 50 mg / kg 81.0 ± 3.4 ⁺ AH, 250 mg / kg 82.3 ± 5.4 Means, 300 mg / kg 99.8 ± 4.2 ⁺ * ^# Note: ⁺ - p <0.05 compared with the control; * - p <0.05 compared with DHA; ^# - p <0.05 compared with hypertension.

Thus, an agent containing dihydroquercetin and arabinogalactan in a ratio of 1: 5 exhibits greater lymphokinetic activity compared to dihydroquercetin and arabinogalactan individually at the doses included in the agent. The present invention extends the arsenal of funds with lymphokinetic activity.

References taken into account

1. Mashkovsky M.D. Medicines - 15th ed., Rev., Rev. and add. - M.: RIA "New Wave": Ed. Umerenkov, 2008 .-- S. 459, 460, 461, 642.

2. Kolkhir V.K., Tyukavkina N.A., Bykov V.A. and others. Dikvertin - a new antioxidant and capillaroprotective agent // Chem.-farm. journal - 1995. - No. 9. - S. 61-64.

3. RF patent No. 2423138. An agent with lymphokinetic activity.

4. Peter d′Adamo. Larch Arabinogalactan is a Novel Immune Modulator // J. Naturopath. Med. - 1996. - No. 3. - P. 32-39.

5. Taxifolin from dahurian larch - application for the approval as novel food // Regulation (EC) no 258/97 of the European parliament and of the council of 27 January 1997 regarding novel foods and novel food ingredients. - 1997. - P. 1-130.

6. Shikov A.N. Nanodispersions of taxifolin: impact of solid-state properties on dissolution behavior // Int. J. Pharm. - 2009. - Vol. 377, Issues 1-2. - P. 148-152.

7. Tolstikova T.G. Arabinogalactan - a plant polysaccharide as a new tool for the clathration of pharmacons // Doklady Akademii Nauk. - 2010. - Volume 433, No. 5. - S. 713-714.

8. Dushkin A.V. Mechanochemical preparation and pharmacological activity of water-soluble intermolecular complexes of arabinogalactan and drugs // Bulletin of the Russian Academy of Sciences. Ser. Chem. - 2008. - No. 6. - S. 1274-1282.

9. RF patent No. 2337710. Water-soluble drug composition and method for its preparation.

10. RF patent No. 2421215. Composition with increased pharmacological activity based on dihydroquercetin and plant polysaccharides (options).

11. Kuznetsov A.V. A new method of collecting lymph from animals // Bull. an experiment. biol. and honey. - 1993. - T. 116, No. 9. - S. 329-331.

Claims (1)

A tool having lymphokinetic activity containing dihydroquercetin, characterized in that it additionally contains arabinogalactan in a ratio (parts by weight) of 1: 5.