Supramolecular complex, possessing anti-inflammatory and angioprotective activity and method of obtaining thereof

FIELD: chemistry.

SUBSTANCE: supramolecular complex, possessing an anti-inflammatory and angioprotective activity, which includes dihydroquercetin, arabinogalactan and water with a specified content of components. The method of obtaining the supramolecular complex includes mixing arabinoglactan with water to complete dissolution, then the addition of dihydroquercetin, heating the solution, mixing, with the following drying of the obtained solution by a method of spraying, under specified conditions.

EFFECT: increase of dihydroquercetin water solubility.

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Group of inventions relates to the pharmaceutical industry, for the production of water-soluble complex with high pharmacological activity, consisting of a poorly soluble in water drug dihydroquercetin and water-soluble complexing agents.

The range of application of dihydroquercetin (DQC) is wide enough, it is used in the manufacture of various products, including in the pharmaceutical industry for the production of dietary SUPPLEMENTS and medicines, as well as in the food industry as an antioxidant. Its disadvantage is the low bioavailability due to poor water solubility. Due to the wide use of the DQC in the food, medical, cosmetic industries, the problem of obtaining water-soluble complex of dihydroquercetin with high pharmacological activity and the development of improved means of obtaining it remains relevant.

It is known that to obtain a water-soluble drugs to poorly soluble in water drug add various water-soluble natural oligo - and polysaccharides, such as dextran, inulin, maltodextrin and cyclodextrin, which form water-soluble complexes with the target drug and, consequently, increase its bioavailability.

From the local water-soluble composition, including soluble antibiotic in the amount of 20-60% and natural polysaccharide selected from the group - dextran, inulin and maltodextrin, taken in a certain ratio. Known composition was prepared by mixing solutions of antibiotics and polysaccharides, followed by drying and allocation of dry adduct in which antibiotics polysaccharides bound non-covalent and non-ionic bonds (US patent 6821959 B1, op. 23.11.2004).

Known water-soluble composition, comprising a low-solubility drug and a cyclodextrin, mainly beta-cyclodextrin. As a poorly soluble drug substance composition contains a non-steroidal anti-inflammatory drug (paracetamol, ibuprofen, Ketoprofen, floranova and mefenamovaya acid and others), steroid, prostaglandin, prostacyclin, a barbiturate, a sulfonamide, a cardiac glycoside. Water-soluble intermolecular complexes of lipophilic organic compounds in solution due to the intercalation of these molecules in the cavity (J. Szejtli, Industrial Applications of cyclodextrins. In Inclusion Compounds, v.3. ed. Atwood J. L., Davies J. E., Mcnicob D. D., Academic Press, N Y., 1984, p.331-390).

The complex on the basis of dihydroquercetin, which is an aqueous solution of dihydroquercetin in molecular encapsulated in the form of water-soluble associate. To obtain this complex is syshestvyut homogenization of dihydroquercetin in the melt surface-active substances, preferably Cremophor RH 40, or in a common solvent is ethanol at a ratio of surfactant to dihydroquercetin 5:1 in the temperature range of 40-70°C, followed by dilution with water and concentration by evaporation of water (patent RU 2406496 C1, op. 20.12.2010). The invention improves the solubility and bioavailability of dihydroquercetin.

The disadvantage of this complex is the low solubility of dihydroquercetin, as well as a long and complicated way of its receipt.

Renowned pharmaceutical composition comprising a poorly soluble drug substance and arabinogalactan (AG), taken in the ratio 1:(5-20) by weight, which is obtained by mechanical treatment of the mixture, preferably in ball mills, in particular planetary (patent RU 2337710 C2, op. 10.11.2008).

However, the method of obtaining water-soluble composition requires the use of shock-abrasive and other intensive mechanical stress, including pressure and shear deformation, which leads to the destruction of the crystal structure of dihydroquercetin.

The most closest to the claimed complex on the basis of dihydroquercetin and method thereof - a prototype is a solid nanocomposite for delivery of biologically active substances, containing 0.1-15% of the active component, in which nanocomposite contains taxifolia is, 40-95% of polymer, in which nanocomposite contains arabinogalactan, or glycols, or polyvinylpyrrolidone, or polyvinly different molecular masses, 0-56% water-soluble component selected from a range of possible fillers: kollidon VA64 (copolymer of vinylpyrrolidone and vinyl acetate), kollidon 90F (high-molecular polyvinylpyrrolidone with M m 1000000-1500000), ludipress (modified lactose), sugar powder, isomaltose, 0-6% or inert hydrophobic polymer in order to achieve a controlled release of medicinal substance, where the hydrophobic component nanocomposite contains compritol 888 ATO (composition of mono-, di - and triglycerides beganovi acid), in an inert - kollidon SR. (a mixture of polymers of polyvinylpyrrolidone and polyvinyl acetate).

The way to get nanocomposite containing Taxifolin and arabinogalactan in a weight ratio of 1:10, includes the following stages: arabinogalactan (10 g) dissolved in 10 ml of water; separately preparing a solution of Taxifolin by dissolving the latter (1 g) in 10 ml of water under stirring and by heating in a temperature-controlled vessel until complete dissolution of Taxifolin; in a vessel with a solution of arabinogalactan with stirring and temperature control add a solution of Taxifolin to obtain a homogeneous medium followed by lyophilization of the product (RPP is NT EN 2351352 C2, op. 10.04.2009).

The disadvantages of the known solid nanocomposite are the complexity of the composition, the use of a large number of imported hard-to-reach components, the high cost of the target product, as well as the duration and intensity of its receipt (the need to use expensive freeze drying).

The task of the group of inventions is the creation of a complex on the basis of dihydroquercetin with increased solubility in water and method of its production.

Effect: increase the water solubility of dihydroquercetin and increase its pharmacological activity, reducing the duration of the method of obtaining complex.

The problem is solved by the claimed composition and the method of its production.

The complex includes dihydroquercetin, arabinogalactan and water, with the following content of components, wt.%:

dihydroquercetin1,0-22,8
arabinogalactan75,2-96,8
water2,0-5,0

The method of producing complex mixes arabinogalactan with water until dissolved, then add dihydroquercetin, the heated solution is to 40-45°C, stirring for 0.5-1 hour, followed by drying the solution obtained by the sputtering technique. For this purpose, in a vessel containing deionized water, dissolved arabinogalactan until dissolved, then the solution is added dihydroquercetin in the ratio of dihydroquercetin: arabinogalactan, equal to 1:(3-100), preferably 1:(50-100) by weight, respectively, the solution is subjected to heating to 40-45°C, stirred for 0.5-1 hour, then the resulting solution was dried by a spray method.

For drying of the complex can be used in the spray dryer with a centrifugal spray (type FEC)with a blade (flat surface) high-speed disk or a spray dryer with the nozzle of the spray (the type SRF), equipped with pneumatic or mechanical (high pressure) nozzle.

Arabinogalactan is a water-soluble polysaccharide with m m 9-18 KD, the main chain of which consists of chains of galactose side chains from chains of arabinose and galactose. This structure promotes the formation of strong intermolecular complexes of drugs, molecules which are likely linked by intermolecular hydrogen bonds in the space formed by the side chains. Given the conformational mobility of the macromolecules of arabinogalactan, this is the space may vary contributing to the formation of intermolecular complexes with a wide range of substances. In addition, the possible formation of complexes of different stoichiometry, when one molecule of arabinogalactan can communicate with several other molecules of organic compounds of medicinal substances, allowing you to change the ratio of these components in a wide range. This are the benefits of arabinogalactan as complexing agents compared with usually used for these purposes by cyclodextrins.

In the same way, perhaps, is the interaction of molecules of dihydroquercetin with complexing agents arabinogalactan. Molecule dihydroquercetin may penetrate between the long polysaccharide chains of arabinogalactan, forming a supramolecular complex, which has a higher solubility in water compared to low dihydroquercetin. As a result, when the preservation of therapeutic action of dihydroquercetin manage dozens of times to increase its solubility and effectiveness.

The defining differences of the proposed complex and method of its production compared to the prototype are:

1. Declare supramolecular complex after drying contains dihydroquercetin and arabinogalactan, taken in the ratio of dihydroquercetin: arabinogalactan is h, equal to 1:(3,3-96,8) by weight, respectively, and water, which improves the solubility of the DQC in water at 11.8-22.5 times and increase its pharmacological activity.

2. The method of producing complex on the basis of dihydroquercetin involves mixing of arabinogalactan with water until dissolved, then add dihydroquercetin in the ratio of dihydroquercetin: arabinogalactan, equal to 1:(3-100), preferably 1:(50-100) by weight, respectively, heating the solution up to 40-45°C, stirring for 0.5 to 1 hour, followed by drying the solution obtained by sputtering technique, which allows to reduce the duration of the method while maintaining the high quality of the target product.

The spray drying process proceeds very quickly (typically 15-30 seconds) and particle composition in the zone of high temperatures have a rich surface. Thanks to instant drying and low temperature sputtered particles of the complex dried product obtained is of good quality, because there is no violation of the natural properties of dihydroquercetin and arabinogalactan, which is of special importance for the pharmaceutical industry.

In addition, since the mixing of the substances is carried out in the liquid phase, preferably in deionized water, then there is a uniform distribution of substances throughout the volume of the solvent,which results in homogeneity of the obtained complexes.

When using drying method spray significantly reduced and fully mechanized technological cycle of production of finished dry complex of dihydroquercetin with arabinogalactan. In this case, the excluded processes of crystallization, planting, filtration, centrifugation, drying, grinding, grinding of the finished product, which significantly reduces energy consumption.

Drying material during the drying process is not in contact with the surfaces of the dryer until then, until it dries. This simplifies the resolution of the problems of corrosion and material selection for the drying chamber. When other methods of drying the wet product is in contact with metal surfaces.

Techno-economic performance of the method of spray drying can be significantly improved due to the intensification of the process of evaporation in the spray dryer. As shown, when the drying of highly dispersed materials can significantly intensify the process, resulting in reduced size and costs of electricity and heat.

The present invention is illustrated by the following examples.

Example 1. Obtaining complexes on the basis of dihydroquercetin

In a vessel containing deionized water, was added arabinogalactan and dihydroquercetin, taken in the mass ratio is s, equal 1:3, 1:5, 1:10, 1:20, 1:30, 1:50 and 1:100 respectively, the solution was subjected to heating to 40-45°C, stirred for 0.5-1 hour and received aqueous solutions of the complexes DQC/AG, which are then subjected to physico-chemical methods of analysis.

As dihydroquercetin used commercial product "Lavitol (dihydroquercetin), batch No. 700V from 23.08.11, TU 9325-001-70692152-07), and arabinogalactan - commercial product "Lavitol-arabinogalactan", lot no. 44 dated 09.11.2011, TU 9325-008-70692152-08). The results of the study of the composition of the obtained complexes, including water, in weight%, before the drying process by sputtering technique, are presented in table 1.

From table 1 it is evident that to obtain a complex of the desired ratio may vary wt.% dihydroquercetin and liquid phase at constant weight.% arabinogalactan.

Example 2. Obtaining a set of dihydroquercetin with arabinogalactan in the ratio 1:3

The complex of dihydroquercetin with arabinogalactan in the ratio of 1:3 by weight, respectively, was prepared as follows. In a vessel containing deionized water displacement 48,0 l, dissolved arabinogalactan powder mass 9,00 kg After complete dissolution contributes to the solution was added a powder of dihydroquercetin mass 3.00 kg, the solution was subjected to heating up to 40°C, paramesh the study was carried out for 1 hour, next, the resulting solution was dried by a spray method.

The dried complex was performed by the method of sputtering in the dryer brands GLP-60 centrifugal spray (type FEC)with a blade (flat surface) high-speed disk.

The time spent drying material in the chamber of the dryer of 1.5-2.0 seconds, the temperature of the inlet air is 180-200°C, outlet temperature of 70-80°C.

The result obtained is a water-soluble complex containing, wt.%:

dihydroquercetin22,8
arabinogalactanto 75.2
water2,0

Example 3. Obtaining a set of dihydroquercetin with arabinogalactan in the ratio of 1:20

The complex of dihydroquercetin with arabinogalactan in the ratio of 1:20 by weight, respectively, was prepared as follows. In a vessel containing deionized water displacement 50,55 l, dissolved arabinogalactan powder mass 9,00 kg After complete dissolution contributes to the solution was added a powder of dihydroquercetin weight 0.45 kg, the solution was subjected to heating to 45°C, stirring was carried out for 0.5 hours, then the resulting solution was dried by a spray method similar Primero.

The result obtained is a water-soluble complex containing, in wt.%:

dihydroquercetin4,4
arabinogalactanbr93.1
water2,5

Example 4. Obtaining a set of dihydroquercetin with arabinogalactan in the ratio of 1:100

The complex of dihydroquercetin with arabinogalactan in the ratio of 1:100 by weight, respectively, was prepared as follows. In a vessel containing deionized water displacement 50,91 l, dissolved arabinogalactan powder mass 9,00 kg After complete dissolution contributes to the solution was added a powder of dihydroquercetin weight 0,09 kg, the solution was subjected to heating to 45°C, stirring was carried out for 0.5 hours, then the resulting solution was dried by a spray method. The result obtained is a water-soluble complex containing, in wt.%:

dihydroquercetin1,0
arabinogalactan96,8
water2,2

In a similar way received the complexes of arabinogalactan is dihydroquercetin in other relationships.

Example 5. The study of the composition of the obtained complexes

Identification and quantitative content of dihydroquercetin in the complex was determined by HPLC using a device MiLiChrome a-02 (CJSC "EcoNova", , Novosibirsk), 290 nm, gradient mode as eluent used a mixture of acetonitrile: water as an internal standard used caffeine as an external standard, a standard sample of dihydroquercetin company "Sigma-Aldrich". Data processing was performed using the software "Multicam".

Chromatogram of a standard sample DQC (a) and complex DQC:AH (1:3) (b) using the internal standard caffeine represented in the drawing. Peak dihydroquercetin included in the composition, on the chromatogram corresponds to the peak standard.

Each received complex in the above ratios were analyzed by chromatographic method under the same conditions.

The AG content in the composition was determined photometrically by the reaction with astronom in an acidic environment. The data on the composition of the obtained water-soluble complexes are shown in table 2.

From table 2 it follows that the formation of the complex by the method of spray drying of new chemical bonds are not formed, the chemical composition is not estudia, is education only intermolecular bonds between the molecule DQC and AG to increase the solubility of the DQC in the water.

Example 6. The study of water solubility of the complexes of dihydroquercetin with arabinogalactan

An experiment was conducted to study the water solubility of the resulting complexes. For this purpose, the samples were dissolved in 100 ml of distilled water at 20°C on a magnetic stirrer (400 rpm). The dissolution was carried out before until you add the sample continued to dissolve. The concentration of the DQC in solution was determined by the photometric method.

From table 3 it can be seen that with the increasing content of AG in the complex solubility DQC increases.

Example 7. Study of anti-inflammatory activity of complexes of dihydroquercetin with arabinogalactan

Anti-inflammatory activity was studied on a model of acute exudative inflammation in mice caused sublunary the introduction of 0.04 ml of 2% formalin solution into the left rear paw. The investigated complexes were injected intragastrically in water for 1 hour before injection of formalin. A group of control animals received equiano the amount of water treated. After 3 h after injection was measured mass of the left and right rear legs and the difference between them is judged in the ragonetti edema.

The obtained data on the impact of a single intragastric administration of the investigated complexes to increase the mass of the left foot towards the right (Δ, %) presented in table 4.

From table 4 it is seen that the complex of dihydroquercetin with arabinogalactan in the ratio(1:3), (1:5) and (1:10) showed greater anti-inflammatory activity than pure dihydroquercetin.

Example 8. The study angioprotective activity of complexes of dihydroquercetin with arabinogalactan

The study angioprotective activity carried out by the reaction to xylene, which was administered to rats in amounts of 0.02 ml intradermally in nepilirovanny abdomen after 10 min after intravenous injection of 2 ml/kg of 1% solution of Evans blue. Criterion vascular permeability was time (s) between the introduction of xylene and the first signs of skin color. The investigated material was administered intragastrically for 7 days in purified water. A group of control animals received equiano the amount of water treated. The recent introduction of the substances was carried out for 1 hour before injection of a solution of Evans blue. Data on the impact of exchange rate intragastric administration of complexes in capillary permeability in rats is shown in table 5.

From table 5 it follows, is then investigated complexes of dihydroquercetin with arabinogalactan have strong angioprotective properties.

The invention allows to increase the solubility of dihydroquercetin in the water up to 11.8-22,5 time, to improve its bioavailability by increasing the absorbability of the complex, resulting in a possibility of reducing the dose of the medication dihydroquercetin while maintaining its pharmacological activity.

The invention also allows to considerably reduce the duration of the method of producing complex while maintaining the high quality of the target product.

1. Supramolecular complex with anti-inflammatory and angioprotective activity, including dihydroquercetin, arabinogalactan and water, with the following content of components, wt.%:

dihydroquercetin1,0-22,8
arabinogalactan75,2-96,8
water2,0-5,0

2. A method of obtaining a supramolecular complex under item 1, comprising mixing arabinogalactan with water until dissolved, then add dihydroquercetin, heating the solution up to 40-45°C, stirring for 0.5 to 1 hour, followed by drying the solution obtained by the sputtering technique.



 

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4 tbl, 6 ex

FIELD: chemistry.

SUBSTANCE: method of obtaining rutin from vegetative mass of buckwheat includes the following stages: dried, crushed buckwheat is subjected to extraction with 70% ethyl alcohol, thickened, filtered, dried, purified from admixtures by means of organic solvents, dissolved, subjected to hot filtration, crystallised, with crushed vegetative buckwheat mass being before extraction subjected to uncoiling, extraction with 70% ethyl alcohol on boiling water bath, filtration and re-extraction with 70% ethyl alcohol, re-filtration, obtained alcohol extracts are concentrated on water bath under vacuum and dried, twice purified from admixtures by means of organic solvents, as organic solvents used are diethyl ester and ethylacetate. After crystallisation, re-crystallisation is carried out with hot 70% ethyl alcohol with hot filtering through paper filter, with further cooling until rutin crystals precipitate, filtration under vacuum and drying in the open air.

EFFECT: application of the claimed method makes it possible to obtain rutin with high degree of purification.

1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: what is presented is using the cannabinoid substance HU-210 as an agent simulating postconditioning. It is shown that a myocardial necrotic zone tends to decrease both absolutely, and as a percentage of an infarction zone to a hypoperfusion zone.

EFFECT: invention may be used to create a new effective agent simulating cardiac postconditioning.

1 tbl

FIELD: organic chemistry, medicine.

SUBSTANCE: invention relates to new compounds of coumarone class, namely, to 6-nitro-2-iminocoumarin 3-carboxylic acid 4-toluidide silver salt of the formula (1): that elicits an antibacterial effect and can be used in medicine. Invention provides preparing a new compound eliciting an antibacterial effect with respect to S. aureus, E. coli, and C. albicans with mononuclear cells values 0.25; 0.5 and 7.8 mcg/ml, respectively, and with acute toxicity value LD50 for these compounds 2 460 ± 230 mg/kg.

EFFECT: valuable properties of compound.

1 cl, 1 tbl, 2 ex

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