Drug preparation for prevention and treatment of hypovitaminosis and normalisation of metabolism in poultry
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to pharmaceutics, and aims at the prevention and treatment of hypovitaminosis and the normalisation of metabolism. The drug preparation contains vitamin A, vitamin D3, vitamin E, vitamin C; a selenium compound is presented by DAFS-25 in the following ratio of the ingredients in 1 l of the solution: vitamin A - 25.0-35.0 ml, vitamin D3 - 0.03-0.05 ml, vitamin E - 55.0-65.0 g, vitamin C - 90.0-110.0 g, DAFS-25 - 0.2-0.4 g, polysorbate-80 - 190.0-210.0 ml, 2-pyrrolidone 39.0-41.0 ml, distilled water - up to one litre.
EFFECT: using the declared invention enables increasing the immune status in poultry, normalising the antioxidant and detoxifying systems, improving the livability, egg production and meat production along with reducing the feed consumption per a unit of product.
3 tbl, 3 ex
The invention relates to the field of pharmaceutics and can be used in poultry production to compensate for the deficiency of vitamins and selenium in animals.
The Ministry of agriculture of the Russian Federation for the period up to 2020 has developed the concept of development of the poultry industry, which provides for increased production of poultry meat and eggs. This concept requires the introduction of innovative technologies of poultry feeding. Meanwhile, the realization of potential productivity of broilers, laying hens and improving the composition of meat and food and hatching quality of eggs is constrained by the use in feed rations, the formulation of which is based on local feed grains having a high content of heavy metals, insufficient quantity of antioxidant substances, most microbial contamination and contamination with mycotoxins. Eating such feed reduces to 15-50% of the secretion of digestive enzymes, causing degenerative changes in the liver and kidneys, has immunodepressive action, leads to the reduction or destruction of antioxidant protection of the organism, increasing its susceptibility to various diseases, decreases productivity, and ecological purity of the obtained products. In addition, the shortage of rations of laying hens vitamins a, D3, E, C and selenium (due to their nesteby the major), which are the most important corrective links optimization of the antioxidant status of the organism and its resistance to diseases, accompanied by a deterioration of hatching quality of eggs and emergence of physiologically immature replacements. This problem is particularly acute because Russia joining the WTO, should, like the EU, to eliminate the use of antibiotics in animal rations.
Thus, the question explore the possibility of improving the incubation qualities and hatchability of eggs of laying hens parent stock, as the most important factor in the reproduction and growth of the industrial population is relevant.
Among the many tools that are diverse in origin, physical-chemical, physiological properties and effects on the body of birds, in particular on the state of metabolism in the body, the immune system and factors of nonspecific resistance, widely used preparations of synthetic amino acids (lysine, methionine, tryptophan), fat-soluble vitamins (carotene. A, D, E, K water soluble vitamins (group B1...B12, C, H, F, U), salts of scarce micronutrients Fe, Cu, Co, Zn, Mn, Se, Mo (see Theory and practice of the use of biologically active substances in animal husbandry, Kirov, October 6-7, 1998: proc. Dokl. scient. proc. Kirov, 1998. - 98 C.).
One is to a large part of these drugs selectively affects certain indicators of immunity.
Known vitamin and mineral supplements for birds of foreign production, such as:
- nutri-selenium (Slovenia) - is a combination of 12 vitamins, 3 essential amino acids and selenium - Internet address: http://zoovet.uaprom.net, 21 APR. 2012;
Rex vital electrolytes (Spain) is a comprehensive formula containing essential vitamins, minerals and amino acids - see, REX VITAL ELECTROLYTES, Handbook of agriculture, national, Internet address: http://sprav.agronationale.ru/drugs/21309.html, 2008.
- movicel (Croatia) is a comprehensive formula containing essential vitamins and minerals - the Internet address: http:// www.hellotrade.com;
- ganeshpuri (Spain) is a complex of 19 vitamins and minerals-the Internet address: http:// www.veterinar.ru, 2002.
The above vitamin-mineral complexes have high efficiency, but have a complex structure and high cost.
Known antioxidant preparation of new generation, namely the preparation Carasel containing beta-carotene, vitamins C, E, DAFS-25 dissolved in vegetable oil (see EN 2342119 C2, 27.12.2008).
Carasel has a positive effect on the regulation of productivity of laying hens, the safety of the young, the daily weight gain of the Chicks on commodity and food quality of the eggs.
However, in the drug no vitamins a and D3. In addition, carasel bad peremeci is moved with the feed, and in the case of uneven mixing risk of selenium poisoning.
Known drug Turbosat Se (France). Turbosat Se - liquid vitamin Supplement with selenium for oral administration. Mixes well with water. All components of the drug are in the form of an aqueous dispersion system. Turbosat Se contains fat-soluble vitamins A, D3E, sodium Selenite and propylene glycol necessary to meet the needs of agricultural animals and birds at the critical periods of productivity. The amount of selenium Turbosat Se the most concentrated product on the Russian market.
Internet address - http://www.vitalagro.ru/product/page7/page98/, 2011
This drug is the closest analogue of the proposed drug.
However, the known drug Turbosat Se no vitamin C, and it contains sodium Selenite has a high toxicity.
The objective of the invention is the development of medicines, ensuring the normal course of metabolic processes in living cells, is involved in a complex enzymatic systems that improve the overall health of the birds and increase productivity.
The problem is solved in that the medicinal product for the prevention and treatment of gipovitaminozov and metabolism is of exectv birds, containing vitamin A, vitamin D3, vitamin E, selenium compound and the target additives according to the invention additionally contains vitamin C, and selenium compounds contains DAFS-25 in the following ratio of ingredients in 1 l of solution:
|Vitamin A||25,0-35,0 ml|
|Vitamin D3||0,03-0,05 ml|
|Vitamin E||55,0-65.0 g|
|Vitamin C||90,0-110,0 g|
|Distilled water||to liters|
Vitamin A participates in redox reactions, the braking activity of the insulin effect on carbohydrate and fat metabolism, activates the metabolism of calcium and magnesium, is included in the composition of the lipid layer of cell membranes and thereby regulates the structure, function and regeneration of epithelial tissues and increases resistance against infection. High doses interfere with what iginio weight and increase metabolism.
Vitamin D3regulates the metabolism of calcium and phosphorus, since absorption from the intestine and to excretion of animals, affecting the formation and development of the skeleton.
Vitamin E regulates the redox processes and influences on carbohydrate and fat metabolism, enhances the activity of vitamins A and D3. Vitamin E acts as an antioxidant, provides the stability and activity of the epithelium of the mucous membranes of the reproductive system, gastrointestinal tract and conjunctiva. With vitamins A, D3and E increase the body's resistance to infectious diseases, improve the General condition of the animals, have a helper activity in rickets and osteomalacia.
Vitamin C is a powerful antioxidant. It plays a role in the regulation of redox processes involved in the synthesis of collagen and procollagen, the metabolism of folic acid and iron, as well as in the synthesis of steroid hormones and catecholamines. Vitamin C also regulates blood clotting, normalizes capillary permeability, necessary for blood formation, anti-inflammatory and antiallergic action. Thus, vitamin C is an important factor in normal growth and improve immune function.
Selenium is involved in the metabolism of proteins and nucleic acids, part of the farm is tov and hormones, involved in immune reactions and regeneration. The lack of selenium in poultry parent stock is sharply reduced the fertility of eggs and increased mortality of embryos in the final stages of development. Selenesetestcase proteins form bone and cartilage that support the skeletal and smooth muscle, control hormonal balance. In DAFS-25 selenium is organic, i.e. a more bioavailable form. In addition, DAFS-25 differs from Selenite and selenate sodium significantly less toxicity and indifference to the components of feed mixtures.
The technical result of the claimed invention is an expansion of the means for the prevention and treatment of gipovitaminozov and normalization of metabolism in birds, i.e. the production of domestic harmless non-toxic vitamin-mineral complex, allowing to compensate for the deficiency of vitamins and selenium in the body of birds, and thus increase its protective function and prevent the development of diseases, developing on their background.
The claimed invention is characterized by the following examples, which, however, do not limit the scope of the claims of the applicant.
Prepare the drug by continuous stirring on a magnetic stirrer estimated number of components when the temperature is ur 50°C. In this first mix 200 ml of Polysorbate-80 0,04 ml of vitamin D (5 million/ml), 30 ml of vitamin a (1.7 million/ml)and 60 g of vitamin E (98%). Then to the resulting solution was added a pre-mixed with 0.3 g DAFS-25 and 40 ml of 2-pyrrolidone. Then to the resulting solution was added an aqueous solution of 100 g of vitamin C, add distilled water to 1 l, and mix.
Received the drug is a balanced combination of essential vitamins and nutrient selenium. Contains : active substances: vitamins a, D3, S, s, s, DAFS-25 and auxiliary ingredients: Polysorbate-80 (tween-80), 2-pyrrolidone and distilled water.
The medicinal product is a clear, opalescense liquid from light yellow to yellow color, mixes well with water.
Derived drug used for the prevention and treatment of gipovitaminozov, normalization of metabolism in birds under stress, reduced productivity: with stunted growth and lack of weight gain; infectious and parasitic diseases; veterinary activities: prophylactic vaccinations and deworming; low egg production and low durability of the eggs.
With the preventive purpose chickens and hens-pullet drug is administered orally in a mixture with water for watering 1 time per month. When the intelligence is AI laying hens prophylactic drug given twice with an interval in 2 weeks. For therapeutic purposes (all age groups) frequency increase to 2-3 times per month.
Dilution of the drug in water conduct explored: first, planting drugs in small amount of water (1:100), and then added to the resulting solution was necessary for feeding the birds plenty of water.
The recommended dose of the drug, taking into account, age and method of administration (ml/100 birds): chickens - 10 ml, young laying hens - 15 ml, laying hens - 20 ml, turkeys - 30 ml
Side effects and complications in the use of the drug in accordance with the above doses are not detected.
The study of chronic toxicity oral drug vitamin with selenium in laboratory animals.
During the study of chronic toxicity vitamin complex a, D3E With selenium spend experience on 24 outbred mice-males with the original weight of 20-25 g
All animals were divided into 4 groups, 6 animals. As in the study of acute toxicity of the drug death of animals was not observed even at the maximum possible doses), we have chosen dose, based on the daily needs of the animals in the vitamins. Previously, the drug was diluted in physiological solution 1:100 to increase the amount of injected substance.
Animals of the 1st experimental group intragastrically through a tube daily what UPE within 1 month were injected vitamin complex at 5 times the dose of daily needs for vitamins.
Animals of the 2nd group was administered intragastrically vitamin complex 10 times the dose of daily needs for vitamins
Animals of the 3rd experimental group were intragastrically injected the drug in a dose of 15 times the daily requirement of vitamins.
Animals of the 4th group - control under the same conditions and feeding was administered an equal volume of saline.
During the whole experience were monitoring the condition and behavior of animals, growth of body mass, regularly conducted research to assess the functional state of the liver (gexanova test), kidney (clinical assessment), studied the effect of the drug on hematological indices. Statistical data processing was performed by the Student-Fisher.
The results showed that during the experience of external signs of intoxication in animals was not observed. All animals of both trial and control groups were active, hair shiny, sleek. Reaction to external stimuli saved.
Signs of toxicity and mortality were observed, which gives grounds to speak about the absence of drug in the dose effect of cumulation for toxic sign.
The drug has a positive effect on the increase in live weight, a trend evidenced by the results of the s weighing animals (table 1).
|The influence of vitamin complex on the weight gain of mice after oral administration in one month (n=6).|
|Time weighting||Body weight of mice, g|
|group 1||group 2||group 3||control|
|2 weeks||26,98±1,01||27,6±0,61||of 27.85±1,44||25,01±1,64|
At the end of the experiment was the slaughter of animals, which were taking a blood biochemical and hematological studies, and took the bodies to the morphological study.
To assess the functional state of the liver was determined by the concentration of total protein and its fractions, glucose and cholesterol in blood serum of mice, enzyme range included determination of activity indicator enzymes ACT (aspartate aminotransferase) and ALT (alanine aminotransferase).
About the state of functional activity of the kidneys was assessed by the concentration of creatinine and urea in blood serum of animals. Biochemical studies were performed using kits Hospitex diagnostics biochemical analyzer Myndrey. Analysis of biochemical parameters of blood of animals of different groups with a long introduction vitamin complex did not reveal statistically significant differences from those of the parameters in animals of the control group (table 2). These data indirectly indicate the absence of disturbances in the functional state of the kidneys and liver.
|The indicators of the functional status of the kidneys and liver of mice with the introduction of a complex of vitamins (n=6, P>0,05)|
|№ p/p||Indicators||Ed. MEAs.||group 1||group 2||group 3||group 4|
|8||ALT||U/l||112,75±to 6.43||126,16±8,84||123,8±9,12||of 118.8±9,41|
The influence of vitamin complex in peripheral blood was assessed by morphological composition of cells and hemoglobin, the apparatus Neeta Screen. As shown by the results of what you study, chronic administration of the drug did not cause significant differences in hematological parameters in comparison with control (table 3).
|Hematological parameters of mice after intramuscular injection of b complex vitamins (n=6, P>0,05)|
|Index||Ed. MEAs.||group 1||group 2||group 3||group 4|
|leukocytes WBC||×109/L||6,4||2,28||5,9||2,40||6,6||1,87||6,6||the 1.44|
|the absolute content of LYM lymphocytes||×109/L||the 4.7||2,49||4||1,50||4,5||0,98||3,1||1,11|
|the absolute content of a mixture of monocytes, basophils and eosinophils MID||×109/L||1,1||0,15||1,2||0,83||1,2||0,14||2,3||0,33|
|the absolute content of granulocytes GRA||×109/L||0,6||0,21||0,7||0,61||0,9||0,12||1,2||0,26|
|the relative content of lymphocytes||%||72,5||5,23||68,4||5,41||68||4,86||46,3||3,76|
|the relative content of the mixture of monocytes, basophils and eosinophils MID||%||17,4||3,45||20||1,28||18,4||2,8||34,4||1,13|
|the relative content of granulocytes GRA||%||the 10.1||1,31||the 11.6||2,82||13,6||1,98||19,3||is 3.08|
|hemoglobin G||g/L||139||13,04||140||14,03||142||8,98||116||of 6.78|
|the average amount of hemoglobin in a red sit||Pg||15,5||1,10||15,4||1,14||14,5||1,68||13||0,98|
|the average volume of red blood cells MCV||Fl||51,8||2,49||50,4||4,82||47,3||3,01||42,6||2,45|
|the width of the distribution. erythrocyte volume RDW-CV||%||18,7||3,76||17,1||3,18||18||to 1.86||14,8||0,10|
|relates. the width of the distribution. erythrocyte volume RDW-SD||F1||48,3||6,40||to 43.1||to 4.41||42,7||4,3||31,5||7,70|
|the hematocrit HCT||%||46,5||5,80||45,9||6,02||46,5||5,08||38,1||1,09|
|the average amount of platelets MPV||F1||5,5||0,15||5,5||0,10||5,3||0,1||5,1||0,40|
|otnoshenia width of the distribution. platelet volume PDW||F1||5,1||0,61||5,6||0,68||5,9||0,12||6,1||0,59|
|the ratio of large platelets|
If pathological examination of the internal organs of mice receiving the claimed medicinal product, there was no evidence of any pathological changes.
Claimed the drug was tested on 2 groups replacements birds cross "Rhodonite-2". Group in the amount of 200 heads were formed on the principle of analogues. Conditions the birds were the same. Both groups received a single diet, the composition of which corresponds to the recommendations of breeding.
Histological studies have shown that chickens treated with this vitamin-mineral complex from the first day, the volume of lymph follicle exceeded that of the control hens 2.5-3.5 times, which indicates the improvement of the immune status of birds, about the activation of immunological centers limpetlike, but also promotes the growth of resistance to various vozbuditeljasyvorotku diseases.
The analysis of the bodies of birds, we have also studied on the selenium content of eggs from laying hens, systematically treated with the drug in the dose. The test results showed that the content of selenium in the liver, muscle, and eggs of birds of the experimental group in 2-2,5 times the amount of selenium in the liver, muscle, and eggs from birds fed the standard premixes foreign production with the use of sodium Selenite.
According to the results of the research showed that the feeding of the proposed drug for the females of the experimental group had a positive effect on egg production and longer peak productivity. Thus, the intensity of oviposition 75 and 95% of the control hens showed, on average, 2 days earlier than hens of the experimental group. The intensity of oviposition at the level of 94-99% of laying hens of the experimental group were held on average for 6 days longer than the hens in the control group. For the entire period, the average egg production of hens in the experience was 89,54% against 84,89% in the control.
The use of the claimed medicinal products had a positive impact on safety. In the control group mortality was a 10.74 and experienced - 6,28%. All this is best reflected in the productivity of chickens. During the research period, the gross collection of eggs in the experimental group was 9.28 are%, and egg production on 8,18 more in comparison with control. The Indus is soo egg, considering live weight, daily feed intake and the level of egg-laying hens of the experimental group on 7,34% was superior to the control. Increased and feed conversion in chickens during the productive period. So, to education 10 eggs bird control group was spent on 5,38% feed more than experienced.
Evaluation of hatching quality of eggs of laying hens, which were added to the declared drug, and without him was performed in 26, 44 and 56 weeks of age. Both morphological and biochemical parameters contributing to the satisfaction of the embryo and to improve the hatchability of eggs, chickens from the experimental group was superior to the chickens of the control group.
Improved and the quality of the eggs from the experimental group. Their eggs are characterized by a significantly greater mass and density. In the yolk, as protein part of the eggs experienced chickens, there is increased content of protein, fat, carbohydrates at a constant level of ash. In addition, the yolk significantly more were deposited carotenoids, vitamins a, C and selenium.
We compared the groups with increasing age, the release of eggs suitable for incubation, but in laying hens fed a feed with the addition of the requested drug, this index in all age periods 0.9-4% more.
Chickens from the experimental group was significantly superior to chickens of the control group on fertilized the spine and hatchability of eggs.
According to the results of biological monitoring conducted during incubation, embryonic development of eggs from hens of the experimental group were more intensively than from chickens of the control group. Total waste of incubation, namely: the level of blood cells in the yolk, the number of eggs with frozen embryos, the number of sadahiko in chickens from the experimental group, on average, 5% lower than females in the control group, which contributed to the increase in output of youngsters.
The mass of the organs involved in the body's immune defense (fabriciana bag, spleen), in chickens from the experimental group is higher than in the control 1.5 and 2 times, respectively.
It was also established that the use of the claimed medicinal product helps improve physical activity and nutritional value of liver, increases its content of vitamins and mineral substances, reduces the accumulation of xenobiotics.
Poultry products after the use of the claimed medicinal product can be used without restrictions.
The above experimental data, it can be concluded that the obtained harmless non-toxic vitamin-mineral complex, allowing to compensate for the deficiency of vitamins and selenium in the body of birds, and thus increase its protective functions, which, in turn, can effectively prevent and treat youwithin the PS birds under stress, by reducing productivity, infectious and parasitic diseases, veterinary activities, and low egg production and low durability of the eggs
In the claimed invention taken into account mutual influence of micronutrients, strengthened their antioxidant activity, which allowed us to obtain the drug improved the quality and expand the range of domestic vitamin-mineral preparations for birds, i.e. to solve the problem.
Medicinal product for the prevention and treatment of gipovitaminozov and normalization of metabolism in birds, containing vitamin a, vitamin D3, vitamin E, selenium compound and the target additives, characterized in that it additionally contains vitamin C, and selenium compounds contains DAFS-25 in the following ratio of ingredients in 1 l of solution:
|Vitamin a||25,0-35,0 ml|
|Vitamin D3||0,03-0,05 ml|
|Vitamin E||55,0-65.0 g|
|Vitamin C||90,0-110,0 g|
|Distilled water||to liters|
SUBSTANCE: invention refers to medicine, namely to cardiology, and may be used for treating and preventing arterial hypertension with metabolic syndrome. That is ensured by adding the food ration with the functional foodstuff 'Samarskiy Zdorovyak' No 61 in a min daily dose of 33.3 g per one intake - with breakfast or lunch or dinner with underlying drug-induced therapy.
EFFECT: enabled treatment and prevention of arterial hypertension with metabolic syndrome
FIELD: medicine, pharmaceutics.
SUBSTANCE: present invention refers to medicine. A pharmaceutical formulation for the treating diseases associated with endothelial dysfunction contains an active ingredient presented by a methyl pyridine derivative - 1.0-6.0 wt %; purine - 10.0-80.0 wt % and additive agents - the rest. The active substance is presented by compounds of a group: 3 -(N,N-dimethyl carbamoyloxy)-2-ethyl-6-methylpyridinium succinate, 3-methylpyridinium succinate, 2-ethyl-6-methyl-3-hydroxypyridinium hydrochloride, 6-trichloromethyl-2-chloropyridine (nitrapyrin), 2-ethyl-6-methyl-3-hydroxypyridine succinate. Purine is presented by inosine, adenosine, hypoxanthine. The pharmaceutical formulation may be presented in the form of injections, lyophilisate, solid capsules, tablets and suppositories.
EFFECT: formulation according to the invention provides creating the stable drug dosage form which considerably exceeds the existing analogues in pharmacodynamics activity on the endothelial dysfunction and toxicological properties.
4 cl, 4 tbl, 9 ex
SUBSTANCE: present compounds can be used, for example, in treating diseases of the central nervous system, peripheral nervous system, cardiovascular system, pulmonary system, gastrointestinal system and the endocrine system.
EFFECT: described compounds are useful in treating a range of diseases or conditions in which interaction with the histamine H3 receptor is beneficial.
9 cl, 216 ex
SUBSTANCE: invention relates to novel phenylaminopyrimidine compounds of formula I, which are JAK kinase inhibitors. In particular, these compounds selectively act on JAK2 kinase. The compounds can be used to treat diseases such as immunological and inflammatory diseases; hyperproliferative diseases, myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases. In the compound of formula I , Q and Z are independently selected from N and CR1; R1 is independently selected from hydrogen, halogen, R2, OR2, OH, R4, OR4, CN, CF3, (CH2)nN(R2)2, where n equals 1,2 or 3, NO2, R2R4, NR2SO2R3, COR4, NR2COR3, CO2H, CO2R2, NR2COR4, R2CN, R2OH, R2OR3 and OR5R4; or two substitutes R1 together with carbon atoms with which they are bonded form an unsaturated 5- or 6-member heterocyclic ring containing 1-4 N atoms; R2 is C1-4alkyl; R4 is R2, C2-4alkenyl or phenyl; R4 is NH2, NHR2, N(R1)2, substituted or unsubstituted morpholine, CH2morpholine, substituted or unsubstituted thiomorpholine, substituted or unsubstituted thiomorpholino-1-oxide, substituted or unsubstituted thiomorpholino-1,1-dioxide, substituted or unsubstituted piperazinyl, substituted or unsubstituted piperidinyl, substituted or unsubstituted pyridinyl, substituted or unsubstituted pyrrolidinyl, substituted or unsubstituted pyrrolyl, substituted or unsubstituted oxazolyl, substituted or unsubstituted imidazolyl, substituted or tetrahydrofuranyl unsubstituted and substituted or unsubstituted tetrahydropyranyl; R5 is C2-4alkylene; R6-R9 are independently selected from H, RXCN, halogen, substituted or unsubstituted C1-4alkyl, OR1, CO2R1, N(R1)2, NO2 and CON(R1)2, wherein at least one of R6-R9 is RXCN; the rest of the values of the radicals are given in the claim.
EFFECT: high efficiency of treatment.
29 cl, 7 dwg, 2 tbl, 93 ex
SUBSTANCE: invention relates to compounds of general formula (1) or salts thereof, where in formula (1) R1 is a lower C1-C6alkyl group, a lower C3-C6cycloalkyl group, a phenyl group, a heterocyclic group, which relates to a residue formed by removing a hydrogen atom from a saturated or unsaturated monocyclic heterocyclic ring containing one, two or three heteroatoms in the ring, selected from a nitrogen atom, an oxygen atom and a sulphur atom, or a phenyl(C1-C6alkyl) group; in cases when R1 is a lower C1-C6alkyl group, that lower C1-C6alkyl group can have, as substitute(s), one, two or three groups selected from a halogen atom, a heterocyclic group which relates to a residue formed by removing a hydrogen atom from a saturated monocyclic heterocyclic ring containing one or two heteroatoms in the ring, selected from a nitrogen atom and an oxygen atom, a carboxyl group, a lower C1-C6alkoxycarbonyl group, a lower C1-C6alkylamino group, a lower C1-C6alkylamino group, substituted with a lower C1-C6alkylamino group, a lower C1-C6alkylamino group, substituted with a phenyl group; in cases when R1 is a phenyl group, a heterocyclic group which relates to a residue formed by removing a hydrogen atom from a saturated or unsaturated monocyclic heterocyclic ring containing one, two or three heteroatoms in the ring, selected from a nitrogen atom, an oxygen atom or a sulphur atom, or a phenyl(C1-C6alkyl) group, that phenyl, heterocyclic or phenyl(C1-C6alkyl) group can contain, as substitute(s), one, two or three groups selected from a halogen atom, a lower C1-C6alkyl group, a hydroxyl group or a lower C1-C6alkoxy group; R2 is a hydrogen atom or a lower C1-C6alkyl group; R3 is a hydrogen atom or a lower C1-C6alkyl group; R4 and R5 can be identical or different and are a hydrogen atom or a lower C1-C6alkyl group; R6 is a hydrogen atom or a lower C1-C6alkyl group; R7 is a phenyl group or a heterocyclic group which relates to a residue formed by removing a hydrogen atom from a saturated monocyclic heterocyclic ring containing one heteroatom in the ring, selected from an oxygen atom and a sulphur atom; in cases where R7 is a phenyl group or a heterocyclic group which relates to a residue formed by removing a hydrogen atom from a saturated monocyclic heterocyclic ring containing one heteroatom in the ring, selected from an oxygen atom and a sulphur atom, that phenyl or heterocyclic group can contain, as substitute(s), one or two groups selected from a halogen atom, a lower C1-C6alkyl group, a hydroxyl group, a lower C1-C6alkoxy group and a nitro group; W is an oxygen atom or NR8; R8 is a hydrogen atom or a lower C1-C6alkyl group; X is an oxygen atom or a sulphur atom; Y is a lower C1-C6alkylene group; Z is an oxygen atom, a sulphur atom, NR9 or OCO; R9 is a hydrogen atom or a lower C1-C6alkyl group. The invention also relates to a pharmaceutical composition based on said compounds, having GR binding activity.
EFFECT: obtaining novel compounds and a pharmaceutical composition based on said compounds, which can be used in medicine as glucocorticoid receptor modulators.
10 cl, 1 tbl, 3 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to naphthalene carboxamide derivatives of general formula I which possess the properties of protein kinase or histone deacetylase inhibitors. The compounds can find application for preparing a drug for treating inflammatory diseases, autoimmune diseases, oncological disease, diseases of the nervous system and neurodegenerative diseases, allergies, asthma, cardiovascular diseases and metabolic diseases or disease related to hormonal diseases. In general formula I: , Z represents CH or N; each of the groups R1, R2 and R3 represents hydrogen, halogen, alkyl, alkoxy or trifluoromethyl; R4 represents or X represents a benzene ring or a pyridine ring; R5 represents one or more substitutes specified in a group consisting of hydrogen, halogen, alkyl, alkoxy or trifluoromethyl. The invention also refers to a method for preparing the above compounds, a pharmaceutical preparation and using them.
EFFECT: preparing the compounds which possess the properties of protein kinase or histone deacetylase inhibitors.
13 cl, 10 tbl, 6 dwg
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention also relates to pharmaceutical compositions. Compounds of the formula given below are used for treatment of diabetes mellitus of type 1 or type 2, hyperglycemia, diabetic complications, insulin-resistance, metabolic syndrome, hyperinsulinemia, hypertension, obesity, edema, dislipidemia, chronic heart failure, atherosclerosis or related diseases, and can be introduced simultaneously or successively with at least one additional therapeutic agent, selected from group consisting of anti-diabetes agent, agent, which reduces content of lipids/modulates lipids, agent for treatment of diabetic complications, anti-obesity agent, hypotensive agent, anti-hyperuricemia agent and agent for treatment of chronic heart failure, atherosclerosis or related diseases.
EFFECT: claimed are compounds which possess inhibiting action on sodium-dependent co-carrier of glucose SGLT.
8 cl, 50 ex, 1 tbl, 15 dwg
SUBSTANCE: invention refers to medicine, namely paediatric resuscitation, and may be used for treating depressed cases in newborns with a surgical pathology. That is ensured by intravenous administration of 20% neat human serum albumin 3-5 ml/kg (no more than 1 g/kg) a day for 10 minutes. Observing persistent arterial hypertension requires an additional intravenous infusion of normal saline 3 ml/kg for 15 minutes, while in the presence of recurrent persistent arterial hypertension, 6% hydroxyethyl starch 3 ml/kg for 30 minutes is administered intravenously.
EFFECT: method enables a higher effect of the performed anti-shock therapy combined with reduced postoperative complications ensured by the prevented liquid outflow from the blood flow that might happen due to high oncotic and osmotic pressure of the concentrated solution of human albumin with contracting the infusion therapy extent.
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to new compounds of the following general formula [1a], wherein R1 represents (1) a hydrogen atom, (2) C1-C6alkyl group, (3) C2-C6alkenyl group, (4) C2-C6alkynyl group, (5) C1-C6alkoxygroup, (6) hydroxyC1-C6alkyl group, (7) C1-C6alkoxy(C1-C6)alkyl group, (8) -CONR11R12, wherein R11 and R12 are identical or different, and each represents a hydrogen atom or C1-C6alkyl group, (9) phenyl group or (10) a five-member heteroaryl group which contains at least one heteroatom specified in a group consisting of a nitrogen atom and oxygen atom, and which may be substituted by C1-C6alkyl group; R2 represents (1) a halogen atom, (2) C1-C6alkyl group, (3) hydroxy group or (4) C1-C6alkoxy group; p is equal to 0, 1, 2 or 3; X represents a carbon atom or nitrogen atom; m1 is equal to 0, 1 or 2; m2 is equal to 0 or 1; the spiro ring AB may be substituted by 1-5 identical or different, specified in a group consisting of (1) hydroxy group, (2) C1-C6alkyl group, (3) C1-C6alkoxygroup and (4) oxo group; n1 is equal to 0, 1, 2, 3 or 4; n2 is equal to 1, 2, 3 or 4; n3 is equal to 0, 1 or 2, provided n2+n3 is equal to 2, 3 or 4; and a bond presented by the symbol means a single bond or a double bond, provided the three adjoining carbon atoms forms no allene bond presented by formula: C=C=C, or a pharmaceutically acceptable salt thereof.
EFFECT: invention refers to a pharmaceutical composition possessing GPR40 agonist activity, to a GPR40 agonist drugs; to a hypoglycemic agent stimulating insulin secretion on the basis of the above compounds.
45 cl, 42 tbl, 120 ex
SUBSTANCE: invention refers to medicine, namely to using the preparation Infliximab as an agent regulating erythrocytes metabolism in the patients with inflammatory intestinal diseases.
EFFECT: invention provides normalising the cell metabolic processes.
1 tbl, 3 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to pharmaceutical industry, namely to a preparation for prevention and treatment of osteoporosis and bone fractures. A method for prevention and treatment of osteoporosis and bone fractures involving the administration of male bee brood, D-group vitamin or vitamins, and/or active metabolites thereof, a calcium compound taken in certain proportions. The preparation for prevention and treatment of osteoporosis and bone fractures consisting of male bee brood, D-group vitamin or vitamins, and/or active metabolites thereof, a calcium compound taken in certain proportions.
EFFECT: preparation and method for treatment enable enhancing the mechanism of uniform recovery of mineral bone density and bone tissue retention ensured by maintaining the androgen level.
3 cl, 1 tbl, 21 dwg, 2 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to pharmaceutical industry, namely to an agent for treating atypical osteoporosis with normal or increased bone mineralisation with cavitary lesions in trabecular bones in overweight and metabolic syndrome. The method of treating atypical osteoporosis with normal or increased bone mineralisation with cavitary lesions in trabecular bones in overweight and metabolic syndrome involving administering male bee brood, D-group vitamin or vitamins, and/or active metabolites thereof. A preparation of treating atypical osteoporosis with normal or increased bone mineralisation with cavitary lesions in trabecular bones in overweight and metabolic syndrome, containing male bee brood, D-group vitamin or vitamins, and/or active metabolites thereof taken in certain proportions.
EFFECT: preparation and method of treating promote body calcium distribution: reducing mineralisation of the soft tissue, vessels and other organs, as well as cavity filling in the trabecular bone.
3 cl, 8 dwg, 4 ex
SUBSTANCE: invention refers to medicine, specifically dermatology, and may be used for treating the patients with psoriatic erythroderma. For this purpose, detoxification hormone therapy combined with external ointment therapy is preceded by prescribing Galavit in a therapeutic dose of 100 mg intramuscularly every day within the course of 10 procedures.
EFFECT: method provides higher clinical effectiveness ensured by a shorter length of therapy, no side effects and prolonged remission.
2 ex, 1 tbl
SUBSTANCE: invention relates to medicine, namely to gynecology, endocrinology and can be used for correction of vaginal dysbiosis in case of metabolic syndrome. For this purpose complex impact on the organism by correction of body weight by means of no-pharmaceutical and pharmaceutical preparations is performed. Hypocaloric diet with reduced caloric content of 500-600 kcall/day, with reduced content of fats in food up to 20-30% and hypolipidemic direction is administered. Increased physical activity and xenical preparation are also administered for 6 months. Correction of metabolic disorders is carried out by means of preparations possessing antioxidant and membrane-stabilising action daily for 3 months. Recovery of vaginal microflora is performed by means of preliminary sanitation of vaginal biotope with antibacterial preparations for 7 days and immunocorrection for 10 days with further administration of eubiotic preparations for 5-7 days. Correction of vaginal dysbiosis is carried out until amount of opportunistic bacteria decreases and/or content of normal microflora is recovered.
EFFECT: method ensures increased efficiency of correction of dysbiotic vaginal disturbances in case of metabolic syndrome.
1 ex, 1 tbl, 3 dwg
SUBSTANCE: invention relates to medicine, namely to orthopedics and restorative medicine, and can be used for increasing mineral density of bone tissue. For this purpose human body is subjected to impact of uniformly accelerated physical loading created by movement of simulator vibration platform in three mutually perpendicular planes with increase of intensity of physical loading and mode. Alendronic acid in dose 70 mg 1 time per week, calcium preparations in dose 1000 mg per day, vitamin D in dose 800 IU per day, as well as functional foodstuff "Samarskiy zdorovyak" No 83 in volume 90 g per day are additionally introduced. Treatment course constitutes 24 weeks.
EFFECT: method ensures increase of mineral density of bone tissue by 4,33%, as well as increase of duration of therapeutic effect action due to stimulation of processes of bone tissue formation, normalisation of gastrointestinal tract functions and metabolism at the background of antiresorptive therapy.
4 cl, 1 tbl
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to pharmaceutical industry, namely to a method for providing cold and influenza virus resistance. The method for providing cold and influenza virus resistance involves the stage whereat a composition containing cholecalciferol and tea extract taken in certain proportions is introduced into an individual. The method for providing cold and influenza virus resistance involves: the stage whereat a composition containing cholecalciferol, tea extract and a probiotic taken in certain proportions is introduced into an individual. The method for providing cold and influenza virus resistance involves: the stage whereat a composition containing cholecalciferol, vitamin D2 and tea extract taken in certain proportions is introduced into an individual.
EFFECT: methods effectively improves cold and influenza virus body resistance, and ensures favourable effects of fit of energy, stress relief and mood improvement in the individual.
20 cl, 37 ex
SUBSTANCE: group of inventions refers to medicine, namely pulmonology, and may be used for treating and preventing a respiratory infection. That is ensured by administering a composition containing: cholecalciferol 450 to 500000 IU per a dose of the composition, and at least one excipient. The excipient is specified in a group consisting of tea extract, vitamin A, probiotics, vitamin C, Andrographis extract, 1-tryptophan, Allium sativum, Eleutherococcus senticosus, Rhodiola rosea, coenzyme Q10, acai, blueberry, cranberry, grapes, guarana, mangosteen, great morinda, pomegranate, sea buckthorn, barbarum berries, Barbados cherry, cere, bilberry, black raspberry, black chokeberry, black currant, Myrciaria dubia, sour cherry, Theobroma grandiflorum, durian, elder-berry, guava, Emblica officinalis, kiwi, red bilberry, litchi, bullace grape, papaya, pomelo, amelanchier, tamarind, sweet cherry, ichang bitter orange and their combinations. A composition is also presented.
EFFECT: group of inventions provides treatment, as well as prevention and relief of respiratory symptoms ensured by combined application of cholecalciferol and said excipients.
19 cl, 37 ex
SUBSTANCE: invention refers to medicine, namely obstetrics and gynaecology, and may be used for treating benign hyperplastic processes of the female reproductive system. That is ensured by the introduction of gonadotropin-releasing hormone agonist for 6 months once monthly in a combination with the oral administration of the preparation for hormonal replacement therapy. It is preceded by specifying the initial metabolic, vegetative and gynaecologic status of the patient which along with an age group provides a basis to assess an adequacy of initiating hormonal add-back therapy. If the patient belongs to the age group of under 40 years of age, and in case of observing additional burdening of the metabolic and vegetative status, the introduction of gonadotropin-releasing hormone agonist with no hormonal add-back therapy prescribed. For the purpose of preventing potential negative symptoms, it is combined with underlying prescription of a complex of phytoestrogens and vitamins with required intake of calcium and vitamin D3. Each injection of gonadotropin-releasing hormone agonist, starting with the second one, is followed by clinical assessment of hypestrogenism symptoms and blood chemistry analysis, and if observing hypestrogenism symptoms, additional hormonal add-back therapy is prescribed. If the patient appears to belong to the age of 40 years old and more, and in case of observing the presence of burdened metabolic and vegetative status regardless of the age group, 2 years after the first injection of gonadotropin-releasing hormone agonist, hormonal add-back therapy is started. When selecting the preparation included in the hormonal add-back therapy regimen: there are differentiated: if the patient belongs to a younger group under 35 years of age, a therapeutic add-back preparation is presented by a combine oral contraceptive containing ethinyl estradiol 30 mg and dienogest 2 mg in each tablet. The oral contraceptive is prescribed 1 tablet a day in the continuous regimen which is recommended to be used after termination of the therapeutic course with gonadotropin-releasing hormone agonist if pregnancy prevention is required. If the patient belongs to the age group of 35 years and older, a therapeutic hormonal add-back preparation is presented by a preparation for hormonal replacement therapy containing micronised 17-p estradiol 1 mg and dydrogesterone 5 mg or a preparation containing drospirenone 2 mg instead of dydrogesterone in each tablet 1 tablet a day in the continuous regimen. An initial or underlying tendency to increase of blood pressure, a combined preparation for hormonal replacement therapy containing drospirenone is prescribed. The therapeutic course is followed by recommended administration of the preparation of hormonal replacement therapy if the patient belongs to the age group of 50 years and older in the continuous regimen.
EFFECT: method enables providing an evident therapeutic effect that is manifested in stable elimination of estrogenic deficiency symptoms accompanying gonadotropin-releasing hormone agonist therapy with preserved clinical effectiveness and improved patient's quality of life.
SUBSTANCE: toxic action of cadmium is experimentally simulated by the daily subcutaneous introduction of a cadmium sulphate solution 0.3 mg/kg on a metal basis wherein a unit of the solution 1 ml is equal to cadmium 0.3 mg. A preventive agent is presented by Aquadetrim introduced in animals once a day daily through a probe into a stomach in dose 25000 IU/kg 1 hour before the subcutaneous introduction of the sulphate solution.
EFFECT: effective reduction of toxic action of cadmium on the body that has been shown by the functional renal state.
2 dwg, 5 tbl, 1 ex
SUBSTANCE: toxic action of cadmium is experimentally simulated by the daily subcutaneous introduction of a cadmium sulphate solution 0.3 mg/kg on a metal basis wherein a unit of the solution 1 ml is equal to cadmium 0.3 mg. A preventive agent is presented by Aquadetrim 25000 IU/kg and 10% calcium chloride 1.5 ml/ kg of body weight. Said preparations are introduced simultaneously daily through a probe in a stomach once a day for 30 days. For the following 30 days, said preparations are introduced daily 1 hour before the subcutaneous injection of cadmium sulphate.
EFFECT: effective reduction of toxic action of cadmium on the body, particularly nephropathic action ensured by changed calcium hemostasis.
2 dwg, 5 tbl, 1 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to pharmaceutical industry, namely to an immunomodulator. An immunomodulator for the immunocorrection accompanying the integrated treatment of chronic non-specific pulmonary diseases, chronic obstructive pulmonary disease, bronchial obstruction syndrome, chronic bronchial pneumonia, pulmonary fibrosis, tracheobronchitis, chronic laryngitis, pulmonary, tracheal and pharyngeal cancer; the immunomodulator is prepared by mixing a water infusion of rose bay leaves and a water infusion of yellow melilot taken in equal proportions, with a cattle lung and larynx powder, settling the prepared mixture, keeping on a boiling water bath, cooling; further, the mixture is filtered; the prepared solution is added with cattle blood serum containing leukaemia oncovirus antibodies, hemlock infusion, ascorbic and sorbic acids until all the ingredients fully dissolved; the prepared solution is placed in the water bath, cooled, filtered, sterilised under certain conditions.
EFFECT: above preparation provides higher effectiveness and reduces the length of treating the above diseases, and ensures the higher immunobiological properties of the human body.