Composition for prevention and treatment of asthma and upper airways diseases and method of production thereof

FIELD: medicine; pharmacology.

SUBSTANCE: composition for prevention and treatment of asthma and upper airways diseases is characterised by that it includes incense tree Boswellia serrata dry extract solution with Boswellia acids content in terms of β- Boswellia acid not less than 80%, in wheat germs oil mixed with pharmaceutically acceptable selenium source and encapsulated containing glycerine, gelatin, pharmaceutically acceptable zinc source and chicory dry extract. Composition production implies that pharmaceutically acceptable zinc source, chicory dry extract gelatin, glycerine are sequentially dissolved renovated water. Agitated mixture is used to make capsule thereafter filled with capsulation solution produced by stirring of wheat germs oil and pharmaceutically acceptable selenium source followed by gradual addition of incense tree Boswellia serrata dry extract, with Boswellia acids content in terms of β- Boswellia acid not less than 80% till it is completely dissolved. Produced capsules are kept at temperature 5-10°C and dried out.

EFFECT: produced composition has improved efficiency.

4 cl, 4 ex

 

The invention relates to the field of medicine and food industry.

Diseases of the upper respiratory tract represent a significant group of pathologies, including rhinitis, laryngotracheitis, bronchitis, pneumonia, acute respiratory viral infection - ARI and others

One of the most common currently, diseases of the upper respiratory tract is bronchial asthma (BA) is a chronic inflammatory disease which is a serious health problem all over the world. Asthma is common in all age groups and often has severe fatal course. More than 100 million people suffer from this disease, and their number is constantly increasing.

In the last decades in all developed countries there has been a significant increase in the severity of bronchial asthma, characterized by earlier onset of the disease. According to some reports, the frequency of bronchial asthma is in the structure of infant morbidity in Russia from 0.2-0.5% to 8%.

That is why there are many international programs and consensus to prevent and combat the spread of BA.

Treatment of asthma is a long process. Etiology it is still not completely clear. Therefore, the action of most medications for asthma basically is not designed to eliminate when the ins disease, and on the removal of the attacks and their prevention.

Designed many structures, including on the basis of natural substances.

Known, for example, a dietary Supplement for prevention and maintenance therapy of asthma and inflammatory diseases of the respiratory system based on medicinal plants containing dry extract of licorice root dry aqueous concentrates of Valerian root, herb, sage, herb, hyssop, dry concentrate infusions peppermint, crushed ginger root, zinc sulfate, calcium gluconate, starch, calcium stearate and sugar (EN 2207143).

According to modern concepts bronchial asthma develops as a multifactorial pathology, in which the original role of activation of mediators of inflammatory interleukins (IL-4, -5, and others)that stimulate the growth, differentiation, and mobilization of mast cells, basophils, eosinophils, and b cells as cellular components of the allergic response.

The prior art work, according to which effective means of influencing these factors can be recognized structures on the basis of an extract of Boswellia and isolated from his active compounds.

In particular, double-blind, placebo-controlled trials of German scientists in 40 patients with bronchial asthma were identified improvement show the lei of the disease in 70% of patients who extract Boswellia. The improvement in the control group (placebo) was only 27% (Gupta I, Gupta V, Parihar A, Gupta S, Ludtke R, Safayhi H, Ammon H-P. // Effects of Boswellia serrata gum resin in patients with bronchial asthma: results of a double-blind, placebo-controlled, 6-week clinical study. Eur J Med Res. 1998 Nov 17; 3(11):511-4).

It is known that the Kameda-resin of Boswellia serrata containing Boswellia acid, is used traditionally in India for the treatment of inflammatory diseases. Boswellia acid inhibit the biosynthesis of leukotrienes, elastase in leukocytes and, consequently, the proliferation. In clinical trials, promising results were observed in patients with rheumatoid arthritis, chronic colitis, disease Crohn's and bronchial asthma (Ammon H-P, Boswelliasauren (Inhaltsstoffe des Weihrauchs) als wirksame Prinzipien zur Behandlung chronisch entzundlicher Erkrankungen. [Boswellic acids (components of frankincense) as the active principle in treatment of chronic inflammatory diseases], Wien Med Wochenschr. 2002; 152(15-16): 373-8).

As the closest analogue may be the source describing the use of 11-keto-beta-Boswellia acid for the treatment of inflammatory diseases such as bronchial asthma (DE 10053056). However, this tool is not a tool for effective preventive action and provides no safe level of intake, which is possible when taking dietary supplements.

The objective of the invention is to develop a composition and method of reception, which can the be used more effectively as in the treatment or prevention of asthma, and other inflammatory diseases of the upper respiratory tract.

This problem is solved by the present invention.

As the basis of the composition of the selected solution of dry extract of Boswellia Boswellia serrata (resin of the frankincense tree in wheat germ oil. In addition, to enhance the biological effect of the funds included in the composition of pharmaceutically acceptable source of selenium, preferably in soluble form, pharmaceutically acceptable source of zinc, preferably in the form of zinc lactate, as well as the extract of chicory dry. Composition per capsule (mg/capsule)

The wheat germ oil200,0-300,0
extract Boswellia Boswellia serrata dry,
content boswellic acids in terms of
on β-Boswellia acid at least 80%20,0-40,0
pharmaceutically acceptable source
selenium in terms of selenium0,004-0,006
The composition of the shell
Gelatinthe 17.3-21,1
Glycerin5,7-6,9
Pharmaceutically acceptable source of zinc
in terms of what and zinc 0,5-0,6
Extract of chicory dry2,2-2,6

Boswellia sacred (incense tree) - Boswellia serrata, a family of burzanovic grows on the slopes of the mountains of the Peninsula Somalia in India. Boswellia exhibits a pronounced anti-inflammatory properties, the ability to repair damaged blood vessels, antimicrobial activity.

As noted above, to date, has enough scientific evidence that anti-inflammatory action boswellic acids.

The study of molecular mechanisms of anti-inflammatory action boswellic acids found that their main feature is the ability to inhibit biochemical pathway arachidonic acid metabolism through the inhibition of 5-lipoxygenase and thereby prevent the formation of leukotrienes. Inhibition of leukotriene biosynthesis and release of leukocyte elastase is an important mechanism for preventing the development of proinflammatory and hypersensibility processes in the body (Safayhi ea, 1997). This Boswellia acid does not block the activity of two other enzymes involved in the metabolism of arachidonic acid to 12-lipoxygenase and cyclooxygenase. This circumstance differs a pharmacological effect bow is llii from known non-steroidal anti-inflammatory drugs, blocking ziklooksigenazny way of transformation of arachidonic acid into prostaglandins and thromboxanes is an important substance in the regulation of hemostasis and flow.

Anti-inflammatory activity of Boswellia was confirmed in studies related to the proinflammatory action of tumor necrosis factor (TNF-alpha), (Royea, 2005).

Another aspect of the anti-inflammatory effects of the extract Boswellia linked to inhibition of nitric oxide production from activated LPS macrophages (Pandey ea, 2005).

Revealed the effectiveness of drugs boswellic acids in chronic colitis (Gupta ea, 2001), in patients with chronic arthritis, knee osteoarthritis and inflammatory neuropathology of spinal origin (Kimmatkar ea, 2003; Kulkami ea, 1991; Reichling ea) and, most importantly, in bronchial asthma.

According to the invention can be used dry extract of Boswellia received traditional known methods, for example, "Boswellia of Serata food quality, New Ambadi Estates PVT. LTD, India", the certificate of state registration № U.

Dry extract of Boswellia is a fluffy powder yellowish-grayish color with a characteristic smell, which has low solubility. In this regard, in accordance with the present invention was developed to form oil the aqueous solution of the extract of Boswellia in wheat germ oil.

The wheat germ oil is obtained by using the dual cold pressed from fresh embryos without any auxiliary materials technology, ensuring the complete safety of biologically active substances that are naturally inherent in the grain.

The uniqueness properties of the oil of wheat germ caused by the presence in its structure of at least 3 active complexes

- antioxidants Tocopherols, carotenoids, and vitamin E oil is the champion of all natural compounds (200 to 600 mg%);

- essential polyunsaturated fatty acids (including linoleic, linolenic), and lecithin ratio, for optimal lipid metabolism in humans;

- b vitamins, D, RR; Antonova and folic (2-3 mg%) acid; the amino acid methionine.

It is widely known that wheat germ oil has a General healing effect, normalizes the function of the immune and endocrine systems; it is a stimulant of the reproductive function; increases capacity; improves vitality and resistance to stress. It promotes rapid healing of wounds, burns, ulcers and diseases of the gastrointestinal tract, has anti-sclerotic and cardiotoxicity properties, lowers cholesterol in the blood and liver, regulates hormonal the th balance.

Biological activity α-tocopherol and its analogs based on high efficiency and ability to liquidate peroxyl radicals of lipids by transfer of the hydrogen atom of the hydroxyl group (one-electron transfer to the radical and restore lipids (antiradical potential). Thus vitamin E prevents the oxidation of unsaturated lipids and prevents oxidation of biological membranes.

Unlike other antioxidants vitamin E is fat-soluble (lipophilic) connection and therefore can easily be integrated directly into the structure of low density lipoproteins and cell membranes, and thus effectively prevents the oxidation of lipoproteins and lipid peroxidation of cell membranes.

Unlike α-tocopherol β- and γ-tocopherol oils have a lower antiradical activity, but their antioxidant activity in the absence of regenerating antioxidants significantly higher than that of the α-tocopherol. Therefore, the presence of wheat germ oil (α, -β, -γ-Tocopherols (24%, 10% and 10%, respectively), along with a-tocopherol significantly increases the efficiency of the antioxidant action of the oil in the ratio of membrane lipids in various tissues.

The importance of the third component of the composition of selenium, the AK essential factor in human nutrition was established about half a century ago. This stimulated the emergence of the doctors numerous selenium-containing biologically active additives to food and officinal preparations. In our country the practical use of selenium in medical practice began relatively recently.

Selenium can be incorporated in the form of any pharmaceutically acceptable source, for example, in the form of Selenomethionine, selenocysteine, of sodium Selenite. A particularly preferred use of selexin. Seleken-9-phenyl-symmetric, octahydrophenanthrene - the strongest antioxidant. Selaxin is the only antioxidants is able to heal itself. It is a prolonged form of metabolically active depot selenium.

Antioxidant effect of selenium significantly enhanced in combination with vitamin E.

The inclusion of zinc in the composition is primarily due to its antioxidante properties. Being a part of Zn-dependent superoxide dismutase, he protects endogenous nitric oxide from its radical transformation into toxic peroxynitrite. Antioxidant activity of zinc is multidimensional. When enriching the body with zinc reduced the concentration of peroxide lipids, including atherogenic low-density lipoprotein. It is known that zinc also has a significant impact on gormo the social functions of the body, including the production and action of androgens and extrarenal; production and function of insulin; the condition of the thymus and production of hormones, with which is closely associated with the immune system of the body.

In recent years increased the demand for zinc in connection with dominance in food vysokouglevodnye food, requiring increased production of insulin and a high prevalence of diabetes.

As pharmaceutically acceptable source of zinc can be used, in particular, zinc sulfate, zinc carbonate, zinc oxide, zinc acetate, zinc ascorbate, etc. Preferably in the form of zinc lactate. For example, the source may be a food additive Pyramex (Puramex) ZN (PURAC Biochem .V, the Netherlands).

Chicory is used in folk medicine since ancient times. Improves the function of the spleen, regulates heart rhythm, increases the force of contraction of the cardiac muscles, calming effect on the Central nervous system, improves the flow of bile, removes cholesterol, eliminates nausea, lowers the level of glucose in the blood, diuretic, stimulates the metabolism and has a stimulating effect, has an analgesic property.

Currently use a variety of drugs chicory, including dry extract Extractum siccum radix Cichorium inthybus.

According to the invention is used, in particular, dry ex is ract chicory FEZ 78.22.59.919.11.000850.04.04 from 26.04.04.

The method of obtaining the composition of the supplements for the prevention and treatment of asthma and diseases of the upper respiratory tract according to the invention is that in the treated water are dissolved successively pharmaceutically acceptable source of zinc, dry extract of chicory, gelatin, glycerin, under stirring, the resulting mass to form a shell which is filled with a solution for encapsulation obtained by mixing oils of wheat germ and pharmaceutically acceptable source of selenium, followed by a gradual addition of dry extract of Boswellia Boswellia serrata, with content boswellic acids in terms of β-Boswellia acid at least 80%, up to its complete dissolution, withstand received capsules at a temperature of 5-10°and dried.

If necessary, after stirring withstand the gelatinous mass to obtain the viscosity of the mass 500-600 mm2/s viscosity Determination is carried out in a thermostat using a viscometer at a temperature of 60°C.

The optimal parameters of the drying air capsules: temperature (17-22)°C, humidity (45-60)%, the drying duration 18-24 hours.

The invention is illustrated by the following specific examples.

Example 1

The content of the capsule mg/capsule

The wheat germ oil 269,983

Boswellia serrata (extract-Boswellia dry) total content boswellic acids in terms of β -Boswellia acid at least 80% 30,00

"Seleken" 0,017 (in terms of selenium 0,004)

The composition of the shell (in terms of dry substance)

Gelatin 19,2

Glycerin 6,3

Food additive "Pyramix" 2,12 (in terms of zinc 0,50)

Extract of chicory dry 2,4

The way to obtain

Preparation of a gelatinous mass

In the reactor manually download 26,69 kg purified water. Poured in a container of about 1.0 kg of water, heated to 60°C. Through a hatch parts when operating the mixer load manually 1.05 kg of zinc lactate, close the lid and stirred until complete dissolution of zinc lactate within 10-20 minutes. Then download 1.19 kg of the extract of chicory and stirred until complete dissolution. Then charged to the reactor 14,96 kg of gelatin, 4,49 kg of glycerol. Close the lid and the contents of the reactor maintained at a temperature (40-45)°C for 0.5-1 h to dissolve gelatin with stirring (the mixer rotation speed of 30 rpm), avoiding strong foaming. If gelatin is received in the form of large conglomerates and rapid swelling and dissolving it difficult, you can increase the duration of the heating and stirring for 30 minutes. The optimal freezing temperature and storage gelatinous mass (20-22)°C.

The entrainment of moisture by evaporation 0,26 kg, mechanical losses gelatinous mass of 1.25 kg Get around to 4.98 kg gelatinous mass, which is used as necessary.

Preparation of the solution for encapsulation

Weighed in the balance the wheat germ oil, selexin. Charged to the reactor to 26.9 kg oil wheat germ, of 1.65 g of selexin. Include a mixer and produce stirring for 2-3 hours. While mixing, gradually, portions of load, 3.3 kg of dry extract of Boswellia serrata. After downloading the entire volume of the extract and continue stirring for 2 hours. Then the resulting mass is left to dissolve. Complete dissolution of the extract of Boswellia serrata control visually. After a specified period of time, the weight should not contain lumps extract and white flocculent particles. Then do unloading solution in the collection.

The output stage 99,0%.

Obtaining gelatin capsules.

Soft seamless gelatinous capsules are made on the Capsulator of molten gelatin mass, filled with product.

Output capsules 27,59 kg

The resulting capsule is maintained at 5-10°in the refrigerating chamber and dried at temperatures of 17-22°in a drying Cabinet.

The shelf life of the product is 18 months from date of manufacture.

The resulting composition is a more effective composition. In particular, the prior art it is known that the optimal dosage of the extract of Boswellia exhibiting anti-inflammatory EF is known without the side effects of oral, is 333 mg (Pharmacokinetic study of 11-Keto-Boswellic Acid, Sharmal S.I; Thawani V.2; Hingorani L.3; Shrivastava M.4; Bhate V.R.5; Khiyani R.6, Phytomedicine, Volume 11, Numbers 2-3, 1 March 2004, pp.255-260(6)). While in accordance with the present invention, the dosage can be significantly reduced and is 20-40 mg.

Example 2

Study of asthma pharmacological activity.

The study suggested the drug was carried out on 26 volunteers (21 women and 5 men) with chronic asthma. Patients were divided into 2 groups: control, treated with the extract-Boswellia 300 mg capsules, and experienced, which applied the proposed composition of example 1 to 3 times a day for 6 weeks. Patients treated BAD, coughing and choking stopped. In 2 patients in the experimental group and 5 in the control over some periods of time resumed coughing. The results of subsequent observations showed that the improvement in the experimental group, on average, 25-30% came faster.

Example 3

Research activity in diseases of the upper respiratory tract.

Patient, 8 years, since the age of five unsuccessfully treated for chronic bronchitis. Constantly worried about the cough, periodically choking, which was shot by INTA. Was prescribed courses of antibiotics. After administration of the composition after two weeks showed a significant Ulu is the solution: stopped coughing, stopped asthma. To date, the disease was not observed.

Patient, 23 years. Treated for chronic tonsillitis, vasomotor rhinitis, frequent colds. Complaints about persistent cough, tonsils are enlarged, sometimes shortness of breath, difficulty in nasal breathing, runny nose. Took the composition of example 1 to 3 times a day for months. After 5-6 days, there have been improvement. After treatment disappeared coughing, a significant decrease of the tonsils, free breathing.

Example 4

Another group of healthy volunteers (11 men) during seasonal outbreaks of influenza and acute respiratory viral infections were investigated prophylactic properties of the new compositions. Twice a day was taken composition of example 1. In the tested group was not registered for these diseases.

Thus, the proposed new treatment is effective and can be widely recommended for treatment and prevention purposes.

1. Composition for the prevention and treatment of asthma and diseases of the upper respiratory tract, characterized in that it comprises a solution of dry extract of Boswellia Boswellia serrata, with content boswellic acids in terms of β-Boswellia acid at least 80%, wheat germ oil, enclosed in a mixture with pharmaceutically pickup is acceptable source of selenium in the shell, contains glycerin, gelatin, pharmaceutically acceptable source of zinc and the extract of chicory dry at the following content of components, mg per capsule:

The wheat germ oil200,0-300,0
Extract Boswellia20,0-40,0
Pharmaceutically acceptable source of selenium
in terms of selenium0,004-0,006
Gelatinthe 17.3-21,1
Glycerin5,7-6,9
Pharmaceutically acceptable source of zinc
in terms of zinc0,5-0,6
Extract of chicory dry2,2-2,6

2. The composition according to claim 1, characterized in that as a pharmaceutically acceptable source of selenium contains selexin.

3. The composition according to claim 1 or 2, characterized in that as a pharmaceutically acceptable source of zinc contains zinc lactate.

4. A method of obtaining a composition for the prevention and treatment of asthma and upper respiratory tract diseases according to any one of claims 1 to 3, characterized in that in the treated water are dissolved successively pharmaceutically acceptable source of zinc, dry extract of chicory, gelatin, glycerin, when s is remesiana from the obtained mass is used to form the shell, which fill with a solution for encapsulation obtained by mixing oils of wheat germ and pharmaceutically acceptable source of selenium, followed by a gradual addition of dry extract of Boswellia Boswellia serrata, with content boswellic acids in terms of β-Boswellia acid at least 80%, up to its complete dissolution, withstand received capsules at a temperature of 5-10°and dried.



 

Same patents:

FIELD: chemistry.

SUBSTANCE: described is a new polymorphous crystalline form B (6S, 9R, 10S, 11S, 13 S, 16R, 17R)-9-chlorine-6-fluorine-11-hydroxy-17-methoxycarbonyl-10,13,16-trimethyl-3-oxo-6,7,8,9,10,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenantrene-17-ylic ether-3-methylthiophene-2-carboxylic acid. Also described are methods of obtaining it.

EFFECT: crystalline form with high antipyretic activity and high stability.

5 cl, 5 ex, 7 tbl, 2 dwg

FIELD: chemistry.

SUBSTANCE: described are the bonds of the formula of pharmaceutical acceptable salt. The bonds possess an inhibiting action in the relation to beta-tryptase. Also, described is the method to treat patients suffering or subject to physiological diseases, with which it is necessary to increase the level of the inhibitor of tryptase.

EFFECT: bonds increase the level of the inhibitor of tryptase.

13 cl, 3 ex, 2 dwg

FIELD: chemistry.

SUBSTANCE: invention relates to the compounds of the formula (I) where: X is O; Y represents a bond, CH2, NR35, CH2NH, CH2NHC(O), CH(OH), CH(NHC(O)R33), CH(NHS(O)2R34), CH2O or CH2S; Z is C(O), or if Y is a bond, then Z can also be S(O)2; R1 could be substituted with phenyl; R4 is hydrogen, C1-6-alkyl (substituted possibly by C3-6-pilkoalkyl) or C3-6-cycloalkyl; R2, R3, R5, R6, R7 and R8 are independently hydrogen, C1-6-alkyl or C3-6-cycloalkyl; type independently indicate 0 or 1; R9 could possibly be substituted with an aryl or heterocycle; R10, R32 and R35 are independently hydrogen, C1-6-alkyl or C3-6-cycloalkyl; R33 and R34 are C1-6-alkyl or C3-6-cycloalkyl; where the aforesaid aryl and heterocyclic groups, when possible, can be substitute with: halogen cyanogens, nitro, hydroxyl, oxo, S(O)Kr12, OC(O)NR13R14, NR15R16, NR17C(O)R18, NR19C(O)NR20R21, S(O)2NR22R23, NR24S(O)2R25, C(O)NR26R27, C(O)R28, CO2R29, NR30CO2R31, by C1-6-alkyl (which itself can be monosubstituted with NHC(O)phenyl), C1-6-halogenalkyl, C1-6-alkoxy(C1-6)alkyl, C1-6-alkoxy, C1-6-halogenaloxy, C1-6-alkoxy(C1-6)-alkoxy, C1-6-alkylthio, C2-6-alkenyl, C2-6-alkinil, C3-10-cycloalkyl, methylenedioxy, difluoromethylenedioxy, phenyl, phenyl(C1-4)alkyl, phenoxy, phenylthio, phenyl(C1-4)alkyl, morpholinyl, heteroaryl, heteroaryl(C1-4)alkyl, heteroarylhydroxy of heteroaryl(C1-4)alkoxy, where any of the said phenyl and heteroaryl groups can be substituted by halogen, hydroxyl, nitro, S(O)r(C1-4-alkyl), S(O)2NH2, S(O)2NH(C1-4-alkyl), S(O)2N(C1-.4-alkyl)2, cyanogens, C1-4-alkyl, C1-4-alkoxy, C(O)NH2, C(O)NH(C1-4-alkyl), CO2H, CO2(C1-4-alkyl), NHC(O)( C1-4-alkyl), NHS(O)2(C1-4-alkyl), C(O)( C1-4-alkyl), CF3 or OCF3; k and r independently mean 0, 1 or 2; R13, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23, R24, R26, R27, R29 and R30 independently represent hydrogen, C1-6-alkyl (probably replaced by halogen, hydroxyl or C3-10-cycloalkyl), CH2(C2-6-alkenyl), C3-6-cycloalkyl, phenyl (itself probably replaced by halogen, hydroxyl, nitro, NH2, NH(C1-4-alkyl), NH(C1-4-alkyl)2, S(O)2(C1-4-alkyl), S(O)2NH2, S(O)2NH(C1-4-alkyl), S(O)2N(C1-4-alkyl)2, cyanogen, C1-4-alkyl, C1-4-alkoxy, C(O)NH2, C(O)NH(C1-4-alkyl), C(O)N(C1-4-alkyl)2, CO2H, CO2(C1-4-alkyl), NHC(O)(C1-4-alkyl), NHS(O)2(C1-4-alkyl), C(O)(C1-4-alkyl), CF3 or OCF3) or heterocyclyl (itself probably replaced by halogen, hydroxyl, nitro, NH2, NH(C1-4-alkyl), N(C1-4-alkyl)2, S(O)2)(C1-4-alkyl), S(O)2NH2, S(O)2NH(C1-4-alkyl), S(O)2N(C1-4-alkyl)2, cyanogen, C1-4-alkyl, C1-4-alkoxy, C(O)NH2, C(O)NH(C1-4-alkyl), C(O)N(C1-4-alkyl)2, CO2H5 CO2(C1-4-alkyl), NHC(O)( C1-4-alkyl), NHS(O)2(C1-4-alkyl), C(O)( C1-4-alkyl), CF3 or OCF3); alternatively, NR13R14, NR15R16, NR20R21, NR22R23, NR26R27 can independently form 4-7-member heterocyclic ring, selected from the group, which includes: azetidine (which can be substituted by hydroxyl or C1-4-alkyl), pyrrolidine, piperidine, azepine, 1,4-morpholine or 1,4-piperazine, the latter is probably substituted by C1-4-alkyl on the peripheral nitrogen; R12, R25, R28 and R31 are independently C1-6-alkyl (possibly substituted by halogen, hydroxyl or C3-10-cycloalkyl), CH2(C2-6-alkenyl), phenyl (itself probably replaced by halogen, hydroxyl, nitro, NH2, NH(C1-4- alkyl), N(C1-4-alkyl)2, (and these alkyl groups can connect to form a ring as described hereabove for R13 and R14), S(O)2(C1-4-alkyl), S(O)2NH2, S(O)2NH(C1-4-alkyl), S(O)2N(C1-4-alkyl)2 (and these alkyl groups can connec to form a ring as described hereabove for R13 and R14), cyanogen, C1-4- alkyl, C1-4- alkoxy, C(O)NH2, C(O)NH(C1-4- alkyl), C(O)N(C1-4-alkyl)2 (and these alkyl groups can connect to form a ring as described hereabove for R13 and R14), CO2H, CO2(C1-4-alkyl), NHC(O)(C1-4-alkyl), NHS(O)2(C1-4-alkyl), C(O)(C1-4-alkyl), NHC(O)(C1-4-alkyl), CF3 or OCF3) or heterocyclyl (itself probably replaced by halogen, hydroxyl, nitro, NH2, NH(C1-4-alkyl), N(C1-4-alkyl)2, (and these alkyl groups can connect to form a ring as described hereabove for R13 and R14), S(O)2(C1-4-alkyl), S(O)2NH2, S(O)2NH(C1-4-alkyl), S(O)2N(C1-4-alkyl)2 (and these alkyl groups can connect to form a ring as described hereabove for R13 and R14), cyanogen, C1-4-alkyl, C1-4-alkoxy, C(O)NH2, C(O)NH(C1-4- alkyl), C(O)N(C1-4-alkyl)2 (and these alkyl groups can connect to form a ring as described hereabove for R13 and R14), CO2H, CO2(C1-4-alkyl), NHC(O)(C1-4-alkyl), NHS(O)2(C1-4-alkyl), C(O)(C1-4-alkyl), CF3 or OCF3); or its N-oxide; or its pharmaceutically acceptable salt, solvate or solvate of its salt, which are modulators of activity of chemokines (especially CCR3); also described is the pharmaceutical composition on their basis and the method of treating the chemokines mediated painful condition.

EFFECT: obtaining new compounds possessing useful biological properties.

13 cl, 238 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, specifically to otolaryngology, and can be used for treatment of children acute purulent maxillary sinusitis or maxillary ethmoiditis. For this purpose, maxillary sinus preliminary washed with distilled water is introduced with medicinal product Actoinvite. Thus Actoinvite is diluted with distilled water 1:10, and 1 ml of solution is introduced through Kulikovsky's needle once in two days. Invention provides increased efficiency of disease treatment, prevents conversion of acute process to chronic due to stimulated neutrophil phagocytic activity, accelerated processes of inflammation resolution.

EFFECT: development of effective method of purulent maxillary sinusitis or maxillary ethmoiditis treatment.

2 ex

FIELD: chemistry.

SUBSTANCE: description is given of a derivative of carboxylic acid with general formula , where R1 represents a hydrogen atom, C1-4alkyl, benzyl, E represents C(=O)-, -SO2- or -CH2-;R2 represents a halogen atom, C1-6 alkyl, C1-6 alkoxy, hydroxyl, C1-4 alkyl, substituted -OR8 , R3 represents a halogen atom, C1-6 alkyl, C1-6 alkoxy; R4 represents a hydrogen atom, C1-6alkyl; R5 represents C1-6 alkyl, C1-10 alkoxy, R8 represents C1-4 alkyl, phenyl; represents a benzol ring; G represents (1) C1-6 alkylene; represents dihydrobenzoxazine; m and n represent 0 or an integer from 1 to 4; I represents 0 or an integer from 1 to 8, where, when m is more or equal to 2, R2 is the same or different; when n is more or equal to 2, R3 is the same of different; when i is more or equal to 2, R5 is the same of different, or its pharmaceutical salt. Since the compound with formula (I), is linked to the DP receptor and has antagonistic effect to the DP receptor.

EFFECT: it is useful for preventing and/or curing such diseases as allergic rhinitis, allergic conjunctivitis, bronchial asthma, malt cell disease, migraine, contact dermatitis, stroke, ulcerative colitis, thrombocyte aggregration or sleep disorder.

FIELD: medicine.

SUBSTANCE: invention can be used for treatment of polypous rhinosinusitis. For this purpose medicine preparation "Longidasa" is applied as injections to polyp tissue dosed 3000 UN per procedure. Course of 5-10 procedures is performed every 5 days. Thus total dose makes 15000 to 30000 UN.

EFFECT: this therapy raises efficiency of non-surgical nose polyp treatment, and increases the disease remission period.

2 ex

FIELD: chemistry.

SUBSTANCE: invention relates to the novel piperazine derivatives with the general formula where R1 is benzofuranyl, inolyl or quinolinyl possibly substituted with one or more halogens; trifluoromethyl; -C1-6alkyl, possibly substituted with COOR15; -C1-6alkoxi, possibly substituted with COOR15; C1-6alkenyl; NR15R16; or C1-6alkylthio groups; and where R15 and R16 independently represent hydrogen, C1-6alkyl or C3-8cycloalkyl or can be condensed together with forming the 5-7-membered non-aromatic heterocyclic ring, possibly discontinued by the O or S atoms and possibly substituted with halogen, C1-6alkyl or -C1-6alkylC1-6alkoxi group; Z is the bind or CO; m is 0 or 2; n is 0; r is 0; p is 1; R3 is -(CH2)q-NR11R12, where q is 3; and NR11 R12 is a pirrolidinyl, piperidinyl, azepanyl or azokanyl, possibly substituted with one or more than one C1-6alkyl group; or their pharmaceutically acceptable salts. The pharmaceutical compositions based on the compounds I and their application in production of the pharmaceuticals, are described.

EFFECT: compounds can be used in treatment of neurodegenerative disorders including Alzheimer's disease.

10 cl, 503 ex

FIELD: medicine; pharmacology.

SUBSTANCE: pharmaceutical formulation as solid dosage form for local treatment of mouth and pharynx inflammatory diseases, containing at least one mucus-producing medicinal plant as dry extract and at least one local analgesic taken in specified ratio. Application of pharmaceutical formulation described above for local treatment of painful inflammatory diseases of mouth cavity and pharynx.

EFFECT: composition is effective for local treatment of painful inflammatory diseases of mouth cavity and pharynx.

9 cl, 4 tbl

FIELD: chemistry.

SUBSTANCE: invention pertains to new hetero-aryl derivatives of 8-azabicyclo-[3.2.1]-octan-3-ol with general formula I where R-R4 represent hetero-aryl. The hetero-aryl is in form of a cyclic aromatic group with C5-C6 or a bicyclic group with C9-C10, which contain 1, 2 or 3 hetero atoms, independently O, S or N, or a residue of , R1-H, C1-C6-akyl, R2 and R3 independently CH3, -OCH3, F, Cl, Br, J, R4 - from 1 to 4 substitutes, -H, halogen, C1-C6alkyl, -CF3, -OCF3, -(CH2)n-OR5, -(CH2)n-NR5R6, -(CH2)n-NHSO2R5, -(CH2)n-NH(CH2)2NR5R6, -(CH2)n-NHC(O)NR5R7, -(CH2)n-NH(CH2)2OR5, or 1-piperazinyl; n - 0, 1, 2, 3; R5 and R6 - H, C1C3alkyl, R7-H, C1-C3alkyl, aminoalkyl C1-C3, or to their pharmaceutical salts. The compounds are antagonists of the nociceptin ORL-1 receptor.

EFFECT: obtaining of compounds that are useful in the treatment of cough.

10 cl, 22 ex, 1 tbl

FIELD: medicine.

SUBSTANCE: offered method implying treatment of chronic obstructive lung disease by inhalation of dry powder (versions). Offer is characterized by the fact that powder consists of phormotherol or its salt, solvate or solvate of specified salt, and consisting of single particles pharmaceutically acceptable solvent or carrier in amount 400 to 5000 mcg per 1 mcg of active component, taking into consideration that carrier or solvent have average particle size 40 to 100 mcm.

EFFECT: continuous broncholytic action and good safety profile.

10 cl, 1 tbl, 30 ex

FIELD: medicine; pharmacology.

SUBSTANCE: invention concerns composition for treatment, inhibition and prevention of breast cancer containing: one of the processed products and extracts Morinda Citrifolia, in amount five percent by mass; and methylsulphonylmethane in amount five percent by mass. Also application of processed Morinda Citrifolia in manufacturing of composition for treatment, inhibition and prevention of breast cancer and application of processed Morinda Citrifolia in manufacturing of medicinal composition chemically preventing and inhibiting carcinogenesis at initiative stage of carcinogen chemical blocking, free radicals isolation, lipid peroxides suppression and COX-2 inhibition are discovered.

EFFECT: offered composition has synergetic effect.

18 cl, 5 dwg, 5 ex

FIELD: medicine; pharmacology.

SUBSTANCE: wood of Siberian or Daurian larch is debarked, cleaved and dried at 40-50°C to residual moisture 23-27%. Dried wood is chopped, and soluble substances are extracted with 75-85% ethyl alcohol aqueous solution at temperature 45-50°C in ratio raw material:extracting agent 1:(7-10). Further extracting agent is distilled off, and sawdust is supplied to press for additional alcohol return. Then extract aqueous part is cooled to 20-25°C within 20-30 minutes for isolation of resinous impurity accompanying dihydroquercetin (DHQ). Deresined extract aqueous part is added with methyltertbutyl ether (MTBE) in ratio 1: (0.3-0.45), and DHQ is reextracted within 2-3 hours. Extract ether part is isolated separate from aqueous part through sedimentation within 2-2.5 hours and supplied to MTBE evaporation, while target product is crystallised of hot water. Invention enables to produce DHQ with yield 2.2-2.5% of bone-dry wood mass with grade 90-96%.

EFFECT: simplification of process and production of high-quality product.

4 cl, 2 ex

FIELD: medicine; pharmacology.

SUBSTANCE: method of agaricic acid production of tinder fungus medicinal (Fomitopsis officinalis Will., tree fungus family - Polyporaceae, basidium fungi class - Basidiomycetes), including extraction of milled raw materials with ethanol under specified conditions, extract evaporation to specified value, agaricic acid isolation, purification, recrystallisation under specified conditions.

EFFECT: method described above enables to produce clean agaricic acid without impurities and to raise end-product yield.

5 dwg, 2 ex

FIELD: medicine; gynaecology.

SUBSTANCE: progestin stimulation of abstinent bleeding is carried out due to delivery system including water-insoluble water-swelling cross-linked polymer based on polycarboxilic acid and progestin in amount sufficient for endometrium secretory transformation and to prevent considerable adverse by-effects. Cyclic vaginal introduction of progestin along with water-insoluble water-swelling cross-linked polymer based on polycarboxilic acid providing stimulation of regular abstinent bleeding is performed every day.

EFFECT: provided regular abstinent bleeding only after progestin introduction period without uncertainty and inconvenience of irregular and unpredictable bleeding.

5 cl, 3 dwg, 3 tbl, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to chemical-pharmaceutical industry, namely for production of medical agent for external application used for treatment of burns, trophic ulcers, dry and wet gangrene, including against diabetes, decubitus, purulent infections (carbuncle, multiple infected wounds, post-infectious abscess, post appendicostomy suppuration, incomplete chronic rectal fistula, delayed healing), psoriasis, breast mastitis and fungus disease. Antiseptic, anti-inflammatory analgesic contains natural wax, propolis, vegetable oil and yellow melilot sprout tops with leaves and blossom of humidity no more than 9%, at following component ratio, mass%: yellow melilot 1.5-2.5, propolis 2.5-4.5, beeswax 4.5-7.5, vegetable oil 85.5-91.5. Efficiency of treatment is increased due to accelerated epithelisation of superficial burns at simultaneous increase in expiration date of specified agent.

EFFECT: development of method of production of effective antiseptic, anti-inflammatory analgesic.

5 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry, specifically to agent of immunomodulating activity. Application of water-soluble polysaccharides made of birch leaves, as an agent of immunomodulating activity, stimulating Th1-dependent type of immune response. Water-soluble polysaccharides described above produced of birch leaves are effective immunomodulators and activators of Th1-dependent immune response.

EFFECT: development of effective method of immunomodulator production of birch leaves.

2 tbl, 1 ex

FIELD: medicine.

SUBSTANCE: invention refers to veterinary science. Method includes introduction of preparation containing (in mass. %): abamechtine - 0.2-2.0; benzyl alcohol - 17.0-30.0; ethyl alcohol - 7.0-35.0; propylene glycol - 40.0-56.0; polyvinylpyrrolidone - 0.5-30.0; distilled water - rest. Preparation is injected intramuscularly in single or twice dosing calculated as per 0.1-0.2 mg/kg body weight by "ДВ". Method provides high therapeutic effect at reduced number and laboriousness of veterinary managements.

EFFECT: development of effective method of parasitic disease treatment in veterinary science.

3 cl, 10 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to chemical-pharmaceutical industry, namely production of means used in balneology for treatment and prevention of various diseases. Balneal product consists of natural components: bischofite 2.5-3.5 g, 5-% argentiferous disinfectant solution 41.5-42.5 ml, 1.0-2.0 ml, fir essence 1-2 ml and pre-milled air-dry powder of bolus alba 52-55 g. Offered product is fine-dispersed, homogeneous and elastic substratum with widen range of indications and purposeful differentiated influence on specific types of nosology with high medical effect. Simple production technique can be combined with possibility to pack "Glinofit" in plastic containers of various volumes. It is easy-to-use both in hospital, and at home in the form of applications.

EFFECT: development of effective balneal product.

5 tbl

FIELD: medicine.

SUBSTANCE: invention refers to medicine, specifically to surgery, and concerns acute pancreatitis prevention after direct duodenum surgery. For this purpose, duodenal mucous within intestine operational wound is perioperatiionally applied with 0.5% hydrocortisone ointment. Method provides decrease in intrapancreatic microcirculation disturbances and, as consequence, prevents development of obturative mechanism of acute postoperative pancreatitis.

EFFECT: development of effective method of pancreatitis prevention after direct duodenum surgery.

2 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, specifically to experimental cardiology and endocrinlogy, and concerns correction of hypoestrogen-induced endothelial dysfunction. For this purpose, rat females of Wistar line is daily intraperitoneally introduced with furostanol glycosides of cell culture Dioscorea deltoidea within 6 weeks after ovariectomy in dosage 1 mg/kg once a day. Method provides effective correction of endothelial dysfunction without any by-effects due to estrogen-like activity of furostanol glycosides.

EFFECT: development of effective method of correction of endothelial dysfunction without any by-effects.

1 ex, 2 tbl

FIELD: medicine; pharmacology.

SUBSTANCE: invention concerns composition for treatment, inhibition and prevention of breast cancer containing: one of the processed products and extracts Morinda Citrifolia, in amount five percent by mass; and methylsulphonylmethane in amount five percent by mass. Also application of processed Morinda Citrifolia in manufacturing of composition for treatment, inhibition and prevention of breast cancer and application of processed Morinda Citrifolia in manufacturing of medicinal composition chemically preventing and inhibiting carcinogenesis at initiative stage of carcinogen chemical blocking, free radicals isolation, lipid peroxides suppression and COX-2 inhibition are discovered.

EFFECT: offered composition has synergetic effect.

18 cl, 5 dwg, 5 ex

Up!