Use of uglanex as lipid, carbohydrate and protein normalising drug

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely therapy and endocrinology, and may be applicable as a lipid, carbohydrate and protein normalising drug in treating type II diabetes mellitus, atherosclerosis and metabolic syndrome. That is ensured by adding the integrating therapy with the drug Uglanex.

EFFECT: invention provides effective treatment of said pathological conditions ensured by reducing a cholesterol level, an atherogenicity index, blood sugar, insulin resistance and albuminuria.

3 tbl

 

The invention relates to medicine and can be used as a new tool for the normalization of lipid metabolism in the treatment of diabetes type II, atherosclerosis, and metabolic syndrome.

In patients with diabetes and metabolic syndrome status of lipid metabolism is one of the most important risk factors for cardiovascular complications and criteria for the identification of the metabolic syndrome. Diabetes is a consequence of the relative or absolute deficiency of insulin. In accordance with the who classification distinguishes between two forms of the disease: insulin (diabetes mellitus type I) and insulin (diabetes type II). Diabetes type I is characterized by an absolute deficiency of education of insulin and requires hormone replacement therapy insulin therapy. Diabetes type II (non-insulin-dependent diabetes) is a metabolic disease characterized by chronic hyperglycemia that develops in the result of a breach of insulin secretion or mechanisms of its interaction with tissue. Patients with diabetes mellitus type II require the appointment of oral antidiabetic drugs. Metabolic syndrome (MS), the prevalence of which according to the results of a large prospective study ARIC reaches 24% in the of enshin and 23% in men, is extremely important medico-social problem. All components of the metabolic syndrome, such as hypertension, abdominal obesity, hypertriglyceridemia and insulin resistance are factors of cardiovascular risk. It is shown that the metabolic syndrome has a negative impact not only on the course of cardiovascular disease, but also on renal function. The risk of developing chronic kidney disease (CKD) increases with the number of components of the metabolic syndrome. Furthermore, the characteristics of lipid metabolism in the presence of metabolic syndrome can be a cause of a violation of the functional state of the kidneys in these patients. Filtered in the glomeruli lipoproteins lead to damage to the endothelium of the capillaries of the glomeruli and the deposition of lipids in mesangial cells, which stimulates the development of sclerosis interstice. Therefore, the current use of drugs that affect the blood lipid profile.

Known means of plant origin, which can be used as a means for correction of disorders of carbohydrate metabolism for the prevention and treatment of diabetes mellitus type II. The tool is ecdysteroidogenesis substance isolated from the aerial parts of plants behold the POOHS crowned Serratula coronata L. (Asteraceae), representing a mixture of 20-gitoxigenin not less than 75% and 25S-inokosterone not less than 10%. The proposed remedy for the treatment of insulin-independent diabetes (type II diabetes) is characterized not only glucose-lowering effect and hypolipidemic activity (Patent No. 2337698, publ. 10.11.2008).

It is known the use of clinoptilolite zeolite Chivyrkuyskogo field as a means for the treatment of diabetes. The tool has a hypocholesterolemic effect and stimulates the regeneration of the endocrine part of the pancreas. Additionally, the tool enhances the regenerative processes in the kidney, liver, intestine, due to the binding and excretion of low molecular weight toxic substances such as urea, uric acid, creatinine, etc. reduces their toxic effect on the body, partially offset renal failure; stimulates reparative regeneration in the blood-forming organs (Patent 2329813, publ. 27.07.2008).

Known plant fees for the prevention and treatment of diabetes. The proposed options. The first version of the collection of medicinal plants for treatment of diabetes contain the herb Galega drug, sheet bilberry, an herb nettle, horsetail grass, herb, leaf fruit beans, fennel fruit is byknowing, a sheet of bearberry leaf, rosehips, a sheet of white birch, seeds, flax seed, walnut leaves. The second option collection for diabetes treatment contains the herb Galega drug, sheet bilberry, an herb nettle, horsetail grass, herb, leaf fruit beans, fennel, a sheet of bearberry leaf, rosehips, a sheet of white birch, seeds, flax seed, walnut leaves and Manchurian aralia. A third option collection for diabetes treatment contains the herb Galega drug, sheet bilberry, an herb nettle, horsetail grass, herb, leaf fruit beans, fennel, a sheet of bearberry leaf, rosehips, a sheet of white birch, seeds, flax seed, walnut leaves, Siberian ginseng root. Options for the collection of medicinal plants help to improve therapeutic efficacy, they can be used as an independent and additional tool, along with other methods of treatment (Patent No. 2331431, publ. 20.08.2008).

It is known for the treatment of diabetes mellitus type II. To do this, along with the conventional drugs used for the treatment of type 2 diabetes, impose additional funds contain an extract of birch bark. The method allows the led is ü the effectiveness of treatment due to hypoglycemic, antioxidant and hypolipidemic properties of biologically active substances, included bark extract (Patent No. 2304976, publ. 27.08.2007).

Task - expanding Arsenal of plant origin, normalizing exchanges in the treatment of diabetes type II, atherosclerosis and metabolic syndrome, which are not toxic and do not cause side effects.

The technical result from the use of the medicinal drug of plant origin is the normalization of the status of lipid, carbohydrate and protein exchanges in adjuvant therapy in the treatment of diabetes type II, atherosclerosis and metabolic syndrome, it causes no side effects and is non-toxic.

The technical result is achieved by using drugs Yuglanex in complex therapy as a means of normalizing lipid, carbohydrate and protein exchange in the treatment of diabetes type II, atherosclerosis, and metabolic syndrome

There was an open randomized comparative prospective 12-week study of the efficacy of therapy Yuglanex, which included 100 patients with diabetes, atherosclerosis and metabolic syndrome, confirmed in outpatient and/or inpatient survey. Patients were randomly assigned at the Nations "1-2" into 2 groups: the main group (50 people) received in addition to basic therapy (drugs to control blood pressure and treatment of coronary heart disease and, if necessary, the glucose-lowering means) - Uglichskaya group (50 people) received only basic therapy. Yuglanex administered at a dose of 5 ml (1 teaspoon)dissolved in 1/2 Cup boiling water, 3 times a day after meals. Characteristics of groups of patients participating in the study are shown in table 1.

Table 1.
the main groupthe control group
The number of patients5050
Age57,17+1,5660,4+2,58
Male/female17/3323/27
Diabetes mellitus, type II, m/W4/54/5
Metabolic syndrome, m/W6/147/14
Obesity12/2413/23
The body mass index, kg/m230,28±4,0631,76±4,42
7,03±1,036,25±0,89
Glycosylated hemoglobin, HbAlc5,79±1,135,26±0,89
Arterial hypertension3839
GARDEN, mm Hg141,3±11,03142,5±15,9
DBP, mm Hg84,25±5,3987,7±to 9.57
Ischemic heart disease2020
Stable angina8/49/3
Disorders of heart rhythm4/13/2
Postinfarct cardiosclerosis2/12/1
Diabetic microangiopathy99
Diabetic peripheral neuropathy5

We also studied the effect of combined treatment with Yuglanex on the state of lipid metabolism diabetes mellitus, atherosclerosis and metabolic syndrome. In patients with diabetes and metabolic syndrome status of lipid metabolism is one of the most important modifiable risk factors for cardiovascular complications and criteria for the identification of the metabolic syndrome. Furthermore, the characteristics of lipid metabolism in the presence of MS can cause violations of the functional state of the kidneys in these patients. Filtered in the glomeruli lipoproteins lead to damage to the endothelium of the capillaries of the glomeruli and the deposition of lipids in mesangial cells.

In the main group of patients who Yuglanex, the positive effect of the drug on almost all indicators of lipid profile: total cholesterol (TC), cholesterol lipids high (Gslwp), very low (JSONP) and low density (Hsnp), triglycerides (TG), atherogenic index (IA). In the main group of patients showed a significant decrease of the content of OH on 10,19% of baseline (p<0.05), and in the control group by 0.85% (p>0,05) (difference between groups significant, p=0,019). Also noted a significant decrease in the content Hlnp on 18,04% (p<0.05) in the primary group and 1.99% (p>0.05) in the control g is the SCP, the difference between groups is statistically significant (p=0.003). The TG content was not significantly changed in both the main and control group.

The atherogenic index (IA) significantly decreased on 16,62% in the main group of patients, whereas in the control group remained almost unchanged (Δ,% 0,75).

Thus, in the study group showed a significant beneficial effect of the drug Yuglanex on the lipid profile of surveyed patients with diabetes type II, atherosclerosis and metabolic syndrome.

We also studied the effect of treatment with Yuglanex on the indices of glycemia on an empty stomach, the level of glycated hemoglobin in patients with diabetes mellitus, atherosclerosis and metabolic syndrome.

Characteristic of diabetes mellitus and metabolic syndrome disorders of carbohydrate metabolism also leads to increased risk of mortality from cardiovascular disease. Even in patients without diabetes, suffering from morbid obesity and impaired glucose tolerance, the probability of myocardial infarction and cerebral stroke 1.9-2.1 times higher, and the mortality rate is two times higher than in patients without metabolic disorders.

We also studied the effect of Yuglanex on HbAlc, fasting glucose in patients with diabetes mellitus, atherosclerosis and metabolic syndrome. Fasting glucose decreased by 4.93% in the main group and in the control of InEU group increased by 10.23% (p> 0,05).

We also studied the effect of treatment with Yuglanex on the severity of albuminuria (AU) in patients with diabetes mellitus, atherosclerosis and metabolic syndrome.

The relationship between microalbuminuria (MAU) and obesity are shown in the GUBBIO study: with increasing body mass index (BMI) at 4 kg/m2potential increased excretion of albumin in urine was increased to 1.83 times men Yves 1.33 times for women.

The presence of MAU says about significant renal dysfunction in patients with diabetes mellitus and MS and is associated with adverse cardiovascular prognosis in these patients. Dynamics of the level of albuminuria in patients with diabetes mellitus, atherosclerosis and metabolic syndrome are shown in table 2

Table 2
Indexthe main groupthe control group
sourceafter 12 weeksΔ,%psourceafter 12 weeksΔ,%p
SU mg/l 390±33,41297,79±26,81*#-23,64<0,05335,35±21,21334,4±21,36-0,4>0,05
Note. The significance of differences with the figures before treatment: * p<0,05. The significance of differences between groups # the - p<0,05

The positive effect of Yuglanex on the severity of albuminuria. Patients of the main group on the background of reception of a preparation AU decreased by 23,64% (p<0.05), whereas in the control group, the severity of AU practically did not change (Δ,% -0,4 p>0,05). The difference between groups is statistically significant (p=0.001).

Thus, the positive effect of the drug Yuglanex on the functional state of the kidneys, which may be mediated by a high content of antioxidants in the product.

We also studied the effect of therapy with Yuglanex on insulin resistance in patients with diabetes mellitus, atherosclerosis and metabolic syndrome.

Insulin resistance, which determines the development of DM and MS, is now seen as the primary etiological factor in the development of heart failure neishemicescoy Genesis. It is shown that in the pathogenesis of the development insulinorezistentne cardiomyopathy is" is a violation of the energetic metabolism of the myocardium, mediated by the formation of the syndrome lipotoxicity, sympathetic dysregulation, oxidative and inflammation, as manifested by the prevalence of the processes b-oxidation of fatty acids and harsh suppression of glucose oxidation in the myocardium and metabolic in it. Therefore, the use of drugs with a high content of antioxidants prospectively in patients in this category.

The results obtained on the effect of the drug Yuglanex on the level of insulin (IRI) and insulin resistance index (NOMA) is presented in table 3.

Table 3
Indexthe main groupthe control group
sourceafter 12 weeksΔ,%psourceafter 12 weeksΔ,%p
IRI16,25+1,6213,02+0,88-19,88>0,0510,7±0,7611,09±0,75 of 3.64>0,05
Index NOMEAndroid 4.04+0,552,87+0,19*-28,96#0,053,27+0,332,85+0,29by 12,8>0,05
Note: p - * the significance of differences between the source and destination parameters, the significance of differences between groups # the - p<0,05

Showed a significant reduction in severity of insulin resistance in the main group of patients (in patients receiving UGLINESS) - Δ, % - of 28.96 (p<0,05). In the control group reliable change index NOMA is not received.

Thus, the obtained results indicate the possibility of correction of the severity of insulin resistance in patients with diabetes and metabolic syndrome using Yuglanex.

We also studied the effect of therapy with Yuglanex on the activity of alanine and aspartic aminotransferases serum of patients with diabetes, atherosclerosis and metabolic syndrome.

The security problem of treatment is the most important aspect of applying any medication. Of particular importance she gets when introduced into clinical practice the drug is destined is asenovo for different age and extent affects the health of groups of patients. The positive effect of many drugs affecting lipid metabolism due to inhibition of synthesis in hepatocytes of cholesterol (LDL), which may be accompanied by lowering the cholesterol content in the membrane of hepatocytes and decrease their microviscosity, increased permeability of the plasma membrane of cells. This forms the cytolysis syndrome - after in the extracellular environment and the blood content of cytosol, in particular alanine aminotransferase and aspartate aminotransferase.

In this regard, the transaminases are indicator enzymes and the content of alanine (ALT) and aspartic (ACT) aminotransferase most widely used markers destruction of the parenchyma of the liver and hepatocellular necrosis.

In our study, both in main and in the control group did not identify adverse events and clinically significant increases in transaminases.

Thus, the claimed invention to the use of the drug Yuglanex in complex therapy normalizes lipid, carbohydrate and protein exchange in the treatment of diabetes type II, atherosclerosis and metabolic syndrome, it causes no side effects and is non-toxic.

The use of the drug Yuglanex in complex therapy as a means of normalizing lipid, carbohydrate and protein exchange in the treatment with Chernogo type II diabetes, atherosclerosis and metabolic syndrome.



 

Same patents:

FIELD: food industry.

SUBSTANCE: invention relates to alimentation field. The infant food set for prevention of children adiposity contains at least three separate nutritional compositions where each of them represents a separate meal for 6-36 months old children. The nutritional compositions include macronutrients content whereof gradually changes in an essentially rectilinear way from the composition containing nearly 40-50% of fat energy and nearly 40-49% of carbohydrate energy for 6 months old babies to the composition containing 30-35% of fat energy and nearly 50-55% of carbohydrate energy for 36 months old children. Additionally one proposes a method for reduction of 6-36 months old children adiposity risk and a dietary regime for such children; these method and dietary regime envisage usage of the said infant food set.

EFFECT: invention allows to prevent adiposity with children during their subsequent life.

22 cl, 6 dwg, 19(32) tbl, 5 ex

FIELD: chemistry.

SUBSTANCE: invention describes novel compounds of general formula where Ar is part of quinoline or isoquinoline, which is substituted or unsubstituted; B is -O-; R1 is hydrogen or S(O)2R4; R2 is S(O)2R4, C(O)OR5 or C(O)(CH2)n-C(O)OR6; R3 is halogen; R4 is an aryl which is unsubstituted or optionally has up to five identical or different substitutes selected from a group consisting of halogen, alkyl, fluoroalkyl, hydroxyl, alkoxy, trifluoromethoxy, cyano, amide, CH3CONH-, acyl and carboxyl; R5 is phenyl; R6 is hydrogen; n is an integer from 1 to 3; and a pharmaceutically acceptable salt or solvate. Also described is a method of producing compounds of formula (I) and pharmaceutical compositions containing said compounds, and also a method of treating metabolic disorders associated with resistance to insulin and hyperglycaemia and use of compounds of formula (I) to prepare a medicinal agent for treating metabolic disorders.

EFFECT: novel compounds which are suitable for treating metabolic disorders associated with resistance to insulin or hyperglycaemia are obtained and described.

28 cl, 54 ex, 4 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, namely peptides which can find application for metabolic syndrome correction.

EFFECT: what is presented is an agent for metabolic syndrome correction representing the tripeptide L-lysyl-L- glutamyl -L-tryptophane.

3 dwg, 3 tbl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, veterinary science, herbal medicine, food and pharmaceutical industry, and may be used in preparing herbal drugs, namely herbal extracts and microelements. The agent contains dry extracts of goat's-rue, Garsinia, linseeds, young shoots of bilberry, bean shell, Gymnema Sylvestre, hill-growing saltwort, rhizomes of a wheat grass and microelements - chromium picolinate, magnesium oxide and vanadium sulphate.

EFFECT: agent provides tissue and cell metabolic change expressed in lower blood glucose level.

7 tbl, 2 dwg

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely therapy and endocrinology, and concerns correction of lipoperoxidation accompanying hypolipidemic therapy of the patients with metabolic syndrome. That is ensured by the combined introduction of statins and coenzyme Q10 scheduled as follows: atorvastatin 20 mg a day in the evening, cudesan equivalent to the content of coenzyme Q10 30 mg a day in the morning daily for 8 weeks with a pause of 8 weeks and renewed introduction; the therapeutic course is 1 year.

EFFECT: such regiment and empirically prescribed drug doses provide intensified antioxidant protection and reduced free-radical lipid oxidation that in turn enables the prolonged introduction of statines that ensures a maximum hypolipidemic effect with no side effects of these preparations.

4 tbl, 2 ex

FIELD: medicine.

SUBSTANCE: group of inventions refers to versions of applying an antisecretory protein which corresponds the amino acid sequence SEQ ID NO:6, its homologue, and/or a fragment containing the amino acid sequence SEQ ID NO:4 showing equivalent activity, and/or its pharmaceutically active salt for preparing a pharmaceutical composition and/or nutritional care for treatment and/or prevention a dysfunction, e.g. a pathological function, lipid raft, receptor and/or small pit hypo- or hyperfunction. The lipid raft, receptor and/or small pit dysfunction can be induced by or cause a number of the other conditions, such as vascular and pulmonary dysfunctions and/or endocrine disorders, e.g. diabetes and related disorders.

EFFECT: group of inventions enables controlling intracellular transport and cell product release, as well as normalising tissue component distribution in various diseases.

13 cl, 12 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula I , and pharmaceutically acceptable salts thereof, where L denotes O, S, or CH2; Y denotes N or CH; Z denotes CR3; G denotes CH; R1 denotes a heteroaryl ring of formula , where D1 denotes S, O; D2 denotes N or CR12; D3 denotes CR12; R2 denotes (C6-C10)-aryl; 5-9-member mono- or bicyclic heteroaryl with 1 or 2 heteroatoms independently selected from N or S; a saturated or partially saturated (C3-C7)-cycloalkyl; or a saturated 5-6-member heteocyclyl with 1 heteroatom selected from N, where said aryl, heteroaryl, cycloalkyl and heterocyclyl are optionally substituted with one or two groups independently selected from (C1-C6)-alkyl, F, Cl, Br, CF3, CN, NO2, OR6, C(-O)R6, C(=O)OR6, C(=O)NR6R7, saturated 6-member heterocyclyl with 2 heteroatoms independently selected from N or O, and S(O)2R6, and where said alkyl is optionally substituted with one -OR8 group; R3 denotes H; (C1-C6)-alkyl; (C2-C6)-alkenyl; Cl; Br; OR6; SR6; phenyl; or a 6-member heteroaryl with 1 heteroatom selected from N, where said alkyl and alkenyl are optionally substituted with one group selected from C(=O)OR8, -OR8, -NR8R9; or a saturated 6-member heterocyclyl with 1 heteroatom selected from N or O.

EFFECT: disclosed compounds are used in treating and preventing diseases mediated by insufficient level of glucokinase activity, such as sugar diabetes.

16 cl, 479 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to novel 6-substituted isoquinolone derivatives of formula

or , or stereoisomeric forms and/or pharmaceutically acceptable salts thereof, where R2 denotes H or (C1-C6)alkyl; R3, R4 and R5 denote H; R6 and R6' independently denote H, (C1-C8)alkyl, (C1-C6)alkylene-R', (C1-C6)alkylene-C(O)O-(C1-C6)alkyl, C(O)-(C1-C6)alkylene-R', or R6 and R6', together with a N atom with which they are bonded form a (C5-C6)heterocyclyl group in which one or more carbon atoms can be substituted with 1, 2 or 3 nitrogen atoms, 1 or 2 oxygen atoms or a combination of different heteroatoms; R7 denotes H, halogen, (C1-C6)alkyl; R8 denotes H; n equals 1; m equals 1, 2, 3, 4 or 5, and L denotes O or O-(C1-C6)alkylene; where, R' denotes (C3-C8)cycloalkyl, (C5-C10)heterocyclyl, (C6-C10)aryl; where in residues R6 and R6' alkyl or alkylene can optionally be substituted one or more times with COOH groups; and where in residues R6 and R6' (C6-C10)aryl and (C5-C10)heterocyclyl are unsubstituted or substituted one or more times with suitable groups independently selected from a group comprising CONH2 and (C1-C6)alkyl; where if m equals 3, R6 cannot denote H; where if m equals 3 and R6 denotes (C1-C8)alkyl, then the alkyl is substituted once or more times, preferably one to three times, with a COOH group. The invention also relates to use of the compound of formula (I) and a medicinal agent based on the disclosed compounds.

EFFECT: novel isoquinolone derivatives which inhibit Rho-kinase and/or Rho-kinase mediated phosphorylation of the myosin light-chain phosphate.

31 cl, 6 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutics. A pharmaceutical granule is spherical or spheroidal and has volume density 0.6-1.3 g/ml and disintegration 0.5-5 minutes. Active pharmaceutical ingredients are preparations of Traditional Chinese Medicine, herbal preparations or their extracts with a nucleus made of an extract of Traditional Chinese Medicine or herbal preparations, and a pharmaceutically acceptable carrier. The content of the pharmaceutically acceptable carrier with respect to total granule weight makes 10-60 wt %. The granule diameter can be equal to 700-1500 mcm. The granule nucleus diameter can be equal to 200-750 mcm. The granule can be also coated with a layer of 2-5 wt % with respect of total granule weight. A method for making the granules consists in introducing initial granules into a layer of a fluidised material as an excipient; the active pharmaceutical ingredients are prepared in the form of a suspension or a solution of the viscosity controlled within 6.0-9.8 MPa·s with using a viscosity-control agent; then they are sprayed over a surface of the initial granule for making a finished granule.

EFFECT: granules possess fast disintegration, contain a small amount of the carrier and contain a low single dose.

12 cl, 5 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new compounds of general formula 1, or their pharmaceutically acceptable salts showing the properties of incretin secretagogues, preferentially the properties of a bile acid receptor TGR5 agonist. The compounds are applicable for treating metabolic diseases associated with glucose metabolism, such as diabetes, obesity, metabolic syndrome, etc. In formula 1 R1, R2 and R3 independently represent a cyclic system substitute specified in: hydrogen, C1-C3alkyl, halogen, a trifluoromethyl group, C1-C3alkoxy, a cyano group, a trifluoromethoxy group; an amino group substituted by C1-C3alkyl; or two radicals R3, found at carbon neighbours in a benzene ring, together with the benzene ring bound therewith form 3,4-methylene dioxyphenyl; R4 represents hydrogen, C1-C5alkyl, a carboxyl group, C1-C3alkoxycarbonyl or an amide group CONHR5; R5 is an optionally substituted by C1-C3alkyl, C5-C6cycloalkyl optionally substituted by phenyl, benzyl, pyridyl; X and Y represent two hydrogen atoms or an oxygen atom, provided Y=O, then X=2H, provided Y=2H, then X=O or X=Y=2H; the sign (N) shows the possibility of bioisosteric substitution of the benzene ring by the pyridine, pyrimidine, pyridazine, triazine or pyrazine ones.

EFFECT: preparing the pharmaceutical composition and the combined drugs with the use of the compounds of formula 1 or the based pharmaceutical composition and a protein kinase DPP-IV inhibitor specified in Vildagliptin or Sitagliptin, and/or an endogenous bile acid or mied bile acid secretagogues.

53 cl, 7 dwg, 8 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, namely peptides which can find application for metabolic syndrome correction.

EFFECT: what is presented is an agent for metabolic syndrome correction representing the tripeptide L-lysyl-L- glutamyl -L-tryptophane.

3 dwg, 3 tbl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to pharmaceutical field and deals with perorally bioavailable pharmaceutical composition, which contains (a) CETP inhibiting compound, which has formula , or its pharmaceutically acceptable salt: (b) concentration-increasing polymer and (c) optionally one or more surface active substances. Invention also relates to application of said composition for production of medication, which increases level of HDL-cholesterol in patient.

EFFECT: invention provides compositions, which increase level of HDL-cholesterol and characterised by improved bioavailability in introduction to patient.

20 cl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of formula I, as well as to their physiologically acceptable salts wherein: X means NH; R1 means (C1-C6)-alkyl; R2 means OH; R2' means H; R5' means (C1-C6)-alkylene-O-S(O)2-R6; R3, R3', R4, R4' and R5 independently mean H, OH, (C1-C6)-alkylene-O-S(O)p-R6, O-(CH2)m-phenyl; at least one of the radicals R3, R3', R4, R4' and R5 has the value -O-(CH2)m-phenyl; R6 means OH; m=1; p=2.

EFFECT: compounds can find application in medicine, eg as lipid-lowering agents.

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to new benzimidazole derivatives of general formula (I) or to its pharmacologically acceptable salts wherein R1 represents a C6-aryl group which can be substituted by 1-3 groups optionally specified in a group of substitutes (a), or a heterocyclic group which represents pyridyl, dihydrobenzofuranyl, 1,3-benzodioxolyl, tetrahydropyranyl, tetrahydrofuranyl which can be substituted by 1-3 groups optionally specified in a group of substitutes (a), R2 represents a C1-C6 alkyl group, R3 represents a C6-aryl group which can be substituted by 1-2 groups optionally specified in a group of substitutes (a), Q represents a group represented by formula =CH-, or a nitrogen atom and a group of substitutes (a) represents a group consisting of a halogen atom, a C1-C6 alkyl group, a C1-C6 halogenated alkyl group, a carboxyl group, a C2-C7 alkylcarbonyl group, a C2-C7 alkoxycarbonyl group, a C1-C6 alkoxy group, a C1-C6 halogenated alkoxy group, an amino group, a 4-morpholinyl group and a di-C1-C6 alkyl)amino group. Also, the invention refers to a pharmaceutical composition based on a compound of formula (I), to a PPARγ activator/modulator based on the compound of formula (I), to using the compound of formula (I), to a method of reducing blood glucose, to a method of activating PPARγ, a method of treating and/or preventing said pathological conditions.

EFFECT: there are produced new benzimidazole derivatives showing PPARγ modulatory activity.

41 cl, 2 dwg, 6 tbl, 76 ex

FIELD: medicine.

SUBSTANCE: invention relates to medicine, namely to pediatrics, and can be used for selection of drug therapy of atherogenic dyslipidemia in children and teenagers with abdominal-visceral obesity. For this purpose index of body weight (IBW) is determined. By results of blood serum lipidogram calculation of atherogenity index (AI) is performed. If IBW is higher than 90-th percentile set for said age group, and AI level is from 2 to 4 including anthropometric parameter - sagittal diameter of abdomen (SDA) is additionally measured. If SDA index equals or is higher than 24.0 cm, state is estimated as requiring drug therapy with chophytol.

EFFECT: method ensures increase of drug therapy efficiency and reduction of risk of early development of atherosclerosis in said group of patients due to possibility of fast and objective determination of degree of expression of risk of early atherosclerosis development, individualisation of indications for drug therapy and its early administration.

1 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a compound of formula (II)

or to its pharmaceutically acceptable salt wherein the ring A represents a group presented by formula 2 R1 represents hydrogen or C1-6alkyl; R2 represents -SR5, halogen, halogenated C1-6alkyl, etc., R3 represents a group presented by formula: -CH=CH-C(RaRb)-Rc-Rd, or a group presented by formula: -(CReRf)m-C(RaRb)-Rc-Rd wherein radicals and symbols have the values presented in the patent claim, R4 represents -OR6, -CONR7R8, -NR9CONR7R8, -(CR10R11)POH, -(CR10R11)pOCONR7R8, -NR9COR12, -(CR10R11)pNR9COR12, -C(=O)NR9OR12, -CONR9CONR7R8, -CN, halogen or NR9(C=O)OR12; R5 represents C1-6alkyl; R6 represents -CONR7R8; each of R7 and R8 independently represents hydrogen or etc., R10 and R11 independently represents hydrogen; R12 represents C1-6alkyl; each of m and p independently represents an integer 1 to 3. This compound is applicable as a type 1 11β-hydroxysteroiddehydrogenase inhibitor.

EFFECT: invention also refers to single compounds, pharmaceutical compositions on the basis of the declared compounds, to a method for preventing and treating diabetes and the use of the compound of formula (II).

21 cl, 289 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new piperazine amide derivatives of formula wherein X represents N or CH; Y represents N or CH; R1 represents lower alkyl, phenyl, phenyl-lower alkyl wherein phenyl can be optionally substituted by 1-2 substitutes independently specified in a group consisting of halogen, lower alkyl; R2 represents lower alkyl, phenyl, naphthyl or heteroaryl specified in dimethylisoxazolyl, quinolinyl, thiophenyl or pyridinyl wherein phenyl or heteroaryl are optionally substituted by 1 substitute optionally specified in a group consisting of halogen, lower alkoxy group, fluor-lower alkyl, lower alkoxy-carbonyl and phenyl; R3 represents phenyl, pyridinyl or pyrazinyl wherein phenyl, pyridinyl or pyrazinyl are substituted by 1-2 substituted optionally specified in a group consisting of halogen, lower alkyl and fluor-lower alkyl; R4, R5, R6, R7, R8, R9, R10 and R11 independently represent hydrogen, as well as to their physiologically acceptable salts. These compounds are bound with LXR alpha and LXR beta, and are applicable as therapeutic agents for treatment and/or prevention of high lipid levels, high cholesterol levels, low HDL cholesterol, high LDL cholesterol, atherosclerotic diseases, diabetes, non insulin dependent diabetes mellitus, metabolic syndrome, dislipidemia, sepsis, inflammatory diseases, infectious diseases, skin diseases, colitis, pancreatitis, cholestasis, liver fibrosis, psoriasis, Alzheimer's disease, etc.

EFFECT: preparing new piperazine amide derivatives.

15 cl, 88 ex

FIELD: medicine.

SUBSTANCE: what is offered is a solid dosage pharmaceutical composition containing a combination of acetylsalicylic acid and ethylmethyl hydroxypyridine malate and ethylmethyl hydroxypyridine succinate possessing antiaggregant, lipid-regulating and gastroprotective activities. What is shown is substantial prolongation of shelf life of the solid dosage form.

EFFECT: pharmacological and pharmacokinetic findings of the new composition make perspective in manufacturing of the solid dosage drugs for preventing and treating obesity, pathological conditions of the cardiovascular system, preventing ischemic disorders with manifested atherosclerosis, old infarction, ischemic stroke; peripheral artery disease.

10 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: layered pharmaceutical compositins for introduction of two or more pharmaceutically active ingredients involves two layers and an intermediate layer located between the first and second pharmaceutical layers. The first and second pharmaceutical layers contain pharmaceutically active ingredients specified in a group of Bupropion, Naltrexone and Zonisamide. The intermediate layer contains at least one monosaccharide sugar, disaccharide sugar or starch. The intermediate layer is formed for fast dissolution in vivo with the first and second pharmaceutical layers remaining intact, but physically separated. The layered composition is used for effective weight loss, loss of appetite and treatment of the obesity-related conditions.

EFFECT: layered pharmaceutical composition under the invention provides maintained predicted dissolution profile of various medical agents.

20 cl, 7 dwg, 3 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: this invention relates to a compound ether of docosahexanoic acid and an alcohol, its production method and a pharmaceutical composition applied as a medication for prevention and treatment of cardiovascular diseases. The said alcohol is selected from pentanol with formula: and inositol with formula . The compound ether production method consists in transetherification of docosahexanoic acid ethyl ether with one of the said alcohols.

EFFECT: development of a pharmaceutical composition applied as a medication for production for cardiovascular diseases treatment and prevention.

10 cl, 5 tbl, 1 dwg, 5 ex

FIELD: medicine.

SUBSTANCE: invention relates to veterinary science. The calves are treated with an alcoholate of the ground herbal mixture and blossom clusters of purple Echinacea, coltsfoot, herb of harmala shrub and roots of common licorice taken in equal proportions. The preparation is sprayed in the form of 3.5-5.0% aqueous solution at 1.5-2.5 ml/m3 for 40-60 minutes by three three-day courses every 48 hours.

EFFECT: method ensures higher prevention effectiveness.

4 tbl, 4 ex

Up!