Agent and method of treating diabetes mellitus
SUBSTANCE: agent for treating diabetes mellitus involving dry aqueous extract of Geranium Dieisianium Knuth and dry aqueous extract of Uncaria tomentosa (Willd) D.C. bark enclosed into gelatine capsules. A method of treating diabetes mellitus provides prescribing the above agent in a daily dose of 180-360 mg after a meal. The above agent enables treating diabetes mellitus effectively by reducing dosages of blood glucose lowering drugs.
EFFECT: agent causes the positive effect on carbohydrate metabolism and possesses non-specific immunomodulatory action.
2 cl, 5 tbl
The invention relates to medicine, namely to therapy and pharmacology, and relates to means for the treatment of diabetes.
Diabetes mellitus is a chronic disease with syndrome chemical hyperglycemia that develops as a result of the impact of genetic and echogenic factors. The prevalence of this disease among the population in some countries is six per cent or more. To date, the globe diabetes affects more than 60 million people.
Treatment of diabetes integrated, depends on the type, stage of the process and develops, as a rule, from insulin therapy, dietary interventions, oral sulfonamides (euglucon, glutaryl, gliclazide) and Begunov (glucophage, adebit).
However, oral antihyperglycemic drugs absolutely contraindicated in ketoacidosis, lactation, diabetic nephropathy. They cause lactic acidosis, exacerbate the underlying disease, and also contribute to the aggravation of diabetic neuropathy.
These shortcomings deprived of phytotherapeutic drugs used in diabetes as a primary or adjunctive treatment.
Hypoglycemic effects have blueberries, chamomile, bergenia crassifolia, juniper berries, burdock root, etc.
Known drug for treatment�finally diabetes Arfazetin containing blueberry leaves (0.2 g); bean leaf (0.2 g); zamanihu high (0.15 g); horsetail grass (0.1 g); chamomile flowers (0.1 g) . However, the hypoglycemic activity of this drug is small. In addition, the drug is poorly combined with insulin therapy, with sulfa and biguanide drugs.
The closest analogue is a device incorporating a Peruvian plant of pasuchaca Geranium Dieisianium Knuth in the form of dry extract in gelatin capsules by 0.1-0.5 or in the form of broth at a ratio of components, wt.%, 1,0-5,0 extract pasuchaca to 100,0 water. Effectively means as monotherapy, as well as in the complex treatment of diabetes mellitus . However, this tool does not have a positive influence on the immune status of patients with diabetes mellitus. Targeted effects on the immune system that suppress the autoimmune reaction against the beta cells, can slow down or even stop the course of insulin-dependent diabetes mellitus. Theoretically, this treatment should help patients with genetically determined insulin dependent diabetes mellitus (spontaneous autoimmune reaction against beta cells), and patients with insulin dependent diabetes mellitus viral or toxic etiology (with induced autoimmune reaction).
The disadvantages of the closest analogue� can be eliminated by assigning phyto, affecting the immunological status on carbohydrate and energy metabolism in patients with diabetes mellitus. This drug, developed by the authors of the invention contains an extract of the Geranium plants dielsianum Knuth (90 mg), famous people of Peru as a “Pasuchaca”, and the bark extract of the plant Uncaria tomentosa (Willd) D.C. (90 mg), famous people of Peru as “Cat's claw”. Plant extracts in a weight ratio of 1:1, enclosed in a capsule made of gelatin and are intended for oral use: 1-2 capsules per day depending on destination specialist (dosage 180-360 mg/day).
As a medicinal raw material is used the bark of the Liana Uncaria tomentosa (Willd) D.C., Geranium dielsianum Knuth used the whole plant. Procurement of plant raw material is produced in distinct areoles Peru, which in this case is the foothills perowsky of the Andes, and in a certain seasonal period is the first month of summer, when concetrate biologically active substances in plants is in the maximum amounts.
The composition of Geranium dielsianum Knuth are: flavonoids, saponins, glycosides, anthraquinones, tannins, fats, wax, resin. The composition of Uncaria tomentosa (Willd) D.C. includes alkaloids: isopteropodine, ringfile, pteropodine, mitraphylline, semitrailer, isorhynchophylline. Polyphenols: triterpenes, plant sterols. Glycosides: glycyrrhizin, glycyrrhizinate acid. Flavone�ID: protoanemonin. Dry extract of Geranium dielsianum Knuth is an amorphous brown powder with a characteristic odor and a bitter astringent taste. Hygroscopic, slightly clump.
Obtaining a dry extract comprises the following steps: washing and grinding of raw material, water extraction of raw materials, filtration, drying by spraying with the use of enveloping substances that preserve the quality of the extract. Dry extract of Uncaria tomentosa (Willd) D.C. is an amorphous powder from gray to pale pink color with the same parameters and extraction technology.
To reveal the essence and relevance of our proposal below presents the results of experimental and clinical research in diabetes mellitus.
1. The experimental study.
1.1. The study of the toxicity of the claimed funds in the acute and chronic experiment.
In the first series of experiments determined the toxic dose of the drug after oral and intraperitoneal administration. The drug was administered in a wide dose range of 0.5-50 g/kg In doses of 0.5-20 g/kg no deaths were observed. With the introduction of a dose of 30 g/kg was observed for the death of 10% of the animals. Only with the introduction of a dose of 50 g/kg was observed 100% mortality of animals.
Thus, the LD50was 35 g/kg.
Assessment of behavioral responses during the entire period of observation showed the presence of the mill�artney motor activity, excitability and reactivity in the normal range. Estimated reflexes unchanged. Only with the introduction of the drug to toxic doses exceeding the LD50was observed excitation, increased motor activity, restlessness, shortness of breath. In a subsequent phase of the excitation is replaced by depression.
In the study of chronic toxicity of the drug was administered to the animals for 21 days with subsequent pathological study of the internal organs (the color of the hematoxylin-Sosin and Sudan-III). When inspecting the bodies normal blood supply. Hemorrhages in organs is not revealed. Liver weights in the normal range. Signs of intoxification liver, i.e., atrophy, vacuolization of cells, polymorphism, piknoz not found.
Blood counts - without pathological changes.
Thus, the data presented indicate non-toxicity of the claimed means in the conditions of acute and chronic experiment.
1.2. The study claimed the funds on the model of alloxan diabetes.
Antidiabetic activity of the claimed funds were studied on the model of alloxan diabetes on 100 male rats weighing 200±10 g.
The alloxan model of diabetes was established by well-known methods by injection of alloxan in a dose of 50 mg per 1 kg weight of the animal, four times every 7 days. To prevent the compensation�ornago reaction from surviving beta cells of the pancreas was injected with allocean dose of 50 mg/kg in 2 months after the start of the experiment, three times with an interval in 2 weeks. The day was injected, allowed to drink animals only, a 5% glucose solution. Resistant diabetes mellitus was noted 4 months after the start of the experiment, as evidenced by high levels of sugar in the blood 9,81±0.8 mmol/l, with a background level of sugar in the blood of 5.7±0.5 mmol/l. By this time the animals have seen the lack of appetite, weight loss, profuse hair loss, aggressiveness.
After receipt of the counter model of diabetes, the animals were divided into 2 groups: 1 group was administered the claimed vehicle, group 2 was the control.
About antidiabetic activity was judged by the level of glucose in the blood and urine of the health of animals and their survival.
The results are presented in table.1, 2, 3.
Thus, as can be seen from the presented data (tables 1-3), declared it exhibits a pronounced gipolipidemicescoy activity on the model of alloxan diabetes.
Impact on immunological status and carbohydrate-energy metabolism of patients with diabetes mellitus is exemplified in clinical trials.
Simple open outpatient, randomized, placebo-controlled trial was attended by 5 people in the test group (4 people with 2 diabetes type 1 diabetes and people with diabetes type 1); 4 pax�century in the placebo group (1 person with type 1 diabetes and 3 people with type 2 diabetes mellitus).
Were evaluated the following performance indicators: fasting glycemia, immunoglobulins G, A, M, E, the indices of body mass index (BMI) and fat tissue in the body special weights company Tanita Corp., additionally, in some patients we evaluated the levels of glycated hemoglobin (HbA1c), C-peptide, proinsulin, immunoreactive insulin.
The benchmarks were: daily glucosuria, levels of total cholesterol, blood pressure, pulse, vibration sensitivity in the lower extremities, the dose gipoglikemisiruushih funds, the dose of medication prescribed complications and/or comorbidities.
All indicators were assessed on the day of appointment of the drug or placebo and after 90-100 days after continuous administration of the drug or placebo 1 capsule after meals with liquid 2 times a day.
Characteristics comparison of tested and control groups on the first day of the beginning of the test and after the test, taking into account factors that could influence the test results presented in table 4.
Dynamic modification of performance criteria during the test is shown in table 5 in the mean of the values.
1. In the test group decreased fasting glycemia and glycated hemoglobin levels, with the exception of the groups� patient P-th, terminated contrary to the order receiving sulfanilamide during the test. This is the only patient in the group that showed an increase in fasting glycemia and glycated hemoglobin. The significance of this increase is reflected in the average figures due to a small sample size, when excluding from the sample the given patient in the rest of the group showed reduction in fasting glycemia and glycated hemoglobin. In the control group was noted implausible increases in the levels of fasting glycemia and glycated hemoglobin levels. If in the test group decreased dosages saharosnijayuschih drugs, in the control group, the dose thereof has been increased. In both groups increased the average daily consumption of carbohydrates (HEH) that the annual rhythm power due to the large consumption of refined carbohydrates in late the autumn months and winter months compared to summer and early autumn.
2. At the same time there were positive changes in lipid metabolism of the tested group compared with the control, manifested in a slight decrease in the level of total cholesterol in the test group, while in the control group cholesterol was increased. In the test group decreased body mass index, while in the control group ind�COP body weight slightly, but there was more. When using zhiroanalizatory marked relative reduction in the mass of adipose tissue in patients of the test group while the marked increase in the mass of adipose tissue in the control group. More significant increase of average daily caloric intake among those in the test group relative to the control.
3. It should be noted the existing trend in the test group to higher levels of IgG and a clear tendency to lower levels of IgE, which is especially apparent in the patient To me, who initially had dramatically increased (more than 5 times from the norm) IgE. In this patient occurred the most significant reduction in IgE after taking the drug. Significant effect on the levels and IgM is not marked.
Described in p. 1 and p. 2 the results can be explained by the relative increase in the hormone b-cell levels of C-peptide, and hence endogenous insulin, while the relative decrease of the increase of proinsulin to load the sample HE that was noted in 3 patients of the test group. It was not a part of this test, so other subjects patients hormone levels were not determined.
Significant changes in the levels of blood pressure, pulse, vibration sensitivity in the lower extremities was noted.
When asking patients about the presence of napurano�completely drug or side effects data has been received.
Thus, a combination drug has a positive effect on carbohydrate metabolism in patients with diabetes, allowing significantly reduce the dosage of hypoglycemic agents, to reduce the average levels of glycemia in the absence of reducing the average daily consumption of carbohydrates in the diet. Product improves fat metabolism, reducing cholesterol levels in the blood, indices of body weight and fat tissue in the body in the absence of reducing daily caloric intake. The drug has a nonspecific imunomoduliruyuschee action, consisting in the possibility to reduce the initially elevated levels of IgE and increase in the normal range IgG levels.
Sources of information
1. Efimov A. S. Clinical endocrinology. M.: Medicine, 1991.
2. Patent RU 2139718, 20.10.1999.
1. The agent for treating diabetes, comprising a dry aqueous extract of Geranium Dieisianium Knuth, characterized in that it further comprises a dry aqueous extract of the bark of Uncaria tomentosa (Willd) D.C., enclosed in a gelatin capsule at a weight ratio of 1:1.
2. A method of treating diabetes d�of abeta, providing for the appointment of a means according to claim 1 at a daily dose of 180-360 mg after meals.
FIELD: medicine, pharmaceutics.
SUBSTANCE: object of the invention is a method and a pharmaceutical composition in the form of a water-alcohol solution of ethanol 30-60° and water 40-70%, wherein at least one hypoglycaemic active substance is stably and completely dissolved, to be used by administering through the oral mucosa as a therapeutic agent in accurate treatment of postprandial hyperglycemia accompanying type II diabetes mellitus in a human or animal; wherein the water-alcohol solution in the composition has a volume of less than 2 ml, wherein an amount of 250mg or less of the above active substance is stably and completely dissolved, while the hypoglycaemic active substance is specified in lipophilic or amphiphilic active substances, such as gliclazide, glinides, incretins and glyphins. The invention also refers to a method for preparing this dosage form.
EFFECT: preparing the therapeutic agent for treating postprandial hyperglycemia accompanying type II diabetes mellitus.
9 cl, 20 ex
SUBSTANCE: invention refers to gene engineering, more specifically to producing the peptide GLP-1, modified by an oligosaccharide chain, and can be used in medicine for treating or preventing diseases associated with GLP-1. In the peptide GLP-1 with SEQ ID NO: 2 or SEQ ID NO: 3 two amino acid peptides are substituted by an amino acid modified by a complex bi-antennal oligosaccharide chain, and wherein each of the centres is specified in a group consisting of positions 18, 22, 26, 30, 34 and 36 in the peptide GLP-1 with SEQ ID NO: 2 or SEQ ID NO: 3. The above modified peptide GLP-1 can involve the deletion, substitution or attachment of 1-5 amino acids, except for the amino acids modified by the oligosaccharide chain.
EFFECT: invention enables producing the peptide GLP-1 modified by the oligosaccharide chain, which shows the stronger activity of blood glucose suppression and twice increased half lifetime as compared to GLP-1 with SEQ ID NO: 3.
24 cl, 5 dwg, 6 tbl, 16 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to peptide analogues of oxyintomoduline (OXM, glucagon-37), which can be modified for providing the stability of cleavage and inactivation with dipeptidyl peptidase IV (DPP-IV) for increasing a half-life time in vivo of the peptide analogue alongside with enabling the peptide analogue acting as a double agonist GLP-1/glucagon receptor (GCGR).
EFFECT: peptide analogues are applicable for treating metabolic disorders, such as diabetes and obesity.
16 cl, 16 dwg, 11 tbl, 12 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to compounds of formula , wherein A represents CRaRb or -CH2-CH2-; R1 represents hydrogen or alkyl; R2 represents hydrogen or alkyl; R3 represents alkyl, cycloalkyl, cycloalkylalkyl, aryl, substituted aryl, 1H-pyrazolyl or substituted 1H-pyrazolyl, wherein substituted aryl represents aryl substituted by 1-3 substitutes independently specified in alkyl, halogen and halogenalkyl, and wherein substituted 1H-pyrazolyl represents 1H-pyrazolyl substituted by 1-3 substitutes independently specified in alkyl and aryl; Ra represents hydrogen or methyl; Rb represents hydrogen or methyl; or Ra and Rb together with a carbon atom, to which they are attached, form cyclopropyl, cyclobutyl or cyclopentyl; provided Ra and Rb both represent hydrogen, or both represent methyl simultaneously, R3 represents (1-methylcyclopropyl)methyl, which possess the inhibitory action on 11b-HSD1.
EFFECT: preparing the compounds, which possess the inhibitory action on 11b-HSD1.
15 cl, 1 tbl, 32 ex
SUBSTANCE: invention refers to a method of treating a condition or a disease, wherein the insulin administration is considered to be effective; the method involves administering effective doses of an insulin derivative representing insulin NεB29-(Nα-(HOOC(CH2)14CO)-y-L-GIu) des(B30) into a patient in need thereof, wherein the above insulin derivative has a prolonged time-action profile, and the above doses are to be administered every 24 to 336 hours.
EFFECT: treating by administering the above insulin through extended intervals of time and simplifying the therapeutic regimens for patient's comfort.
11 cl, 4 ex, 5 tbl, 3 dwg
FIELD: medicine, pharmaceutics.
SUBSTANCE: group of inventions refers to pharmaceutics, namely to an aqueous pharmaceutical composition containing insulin, an insulin analogue or an insulin derivative and methionine; as well as to a method for preparing and using it for treating diabetes mellitus, and to a therapeutic agent for treating diabetes mellitus.
EFFECT: group of inventions provide stability of the above proteins in solution.
29 cl, 10 ex, 6 dwg
SUBSTANCE: invention relates to biotechnology, specifically to a GLP-1 peptide having an attached oligosaccharide chain, and can be used in medicine. Said GLP-1 peptide, having GLP-1 activity, has (a1) one amino acid further attached to the C end (position 37), wherein said attached amino acid is replaced with an amino acid with an attached oligosaccharide chain; or (a2) one or two amino acids, replaced with an amino acid with an attached oligosaccharide chain, where the replacement site is selected from positions 18, 20, 22, 30 and 36, and can further include 1 to 5 amino acid deletions, replacements or inserts, where said oligosaccharide chain contains five or more sugars and is represented by Formula 1. The invention also relates to a pharmaceutical composition and a method of treating or preventing diseases which can be treated or prevented by administering GLP-1, for example diabetes, which comprises use of said GLP-1 peptide having an attached oligosaccharide chain.
EFFECT: invention enables to obtain a GLP-1 peptide having an attached oligosaccharide chain, having improved stability and higher activity in controlling blood sugar level compared to GLP-1.
14 cl, 22 dwg, 10 tbl, 49 ex
SUBSTANCE: invention refers to new anhydrous crystalline forms of saxagliptin hydrochloride of formula presented below There are described methods for producing the crystalline forms of saxagliptin hydrochloride.
EFFECT: crystalline forms of saxagliptin inhibit dipeptidylpeptidase-4.
13 cl, 4 tbl, 11 dwg, 5 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to compounds of formula , where R1 represents hydroxyadamantyl, methoxycarbonyladamantyl, carboxyadamantyl, aminocarbonyladamantyl or aminocarbonylbicyclo[2.2.2]octanyl and where A represents CR5R6; or phenyl, chlorobenzyl, benzyl, chlorophenylethyl, phenylethyl, difluorobenzyl, dichlorophenyl, trifluoromethylphenyl or difluorophenylethyl and where A represents CR5R6; R2 and R3 together with nitrogen atom N* and carbon atom C*, which they are bount to, form group or ; R4 represents hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkoxyalkyl, arylalkyl, arylalkoxygroup, arylalkoxyalkyl, hydroxyalkyl, aryl, heteroarylalkyl, heteroaryloxyalkyl, substituted aryl, substituted heteroarylalkyl or substituted heteroaryloxyalkyl, where substituted aryl, substituted heteroarylalkyl and substituted heteroaryloxyalkyl are substituted with 1-3 substituents, independently selected from alkyl, cycloalkyl, cyanogroup, halogen, halogenalkyl, hydroxygroup and alkoxygroup; R5 represents hydrogen; R6represents hydrogen; as well as to their pharmaceutically acceptable salts and esters, which can be used as 11b-HSD1 inhibitors.
EFFECT: obtaining compounds which can be used as 11b-HSD1 inhibitors.
9 cl, 1 tbl, 103 ex
SUBSTANCE: invention relates to heterocyclic compound of formula or to its pharmaceutically acceptable salt, where Alk represents linear C1-6 alkylene group, branched C1-6 alkylene group or C1-6 alkylene group, which has ring structure, where part of carbon atoms, constituting ring structure can be optionally substituted with oxygen atom, in ring X, X1 represents N or CRX1, X2 represents N or CRX2, X3 represents CRX3, X4 represents N or CRX4, where RX1, RX2, RX3 and RX4 each independently represents hydrogen atom; linear or branched C1-6alkyl group; linear or branched C1-6alcoxygroup; or halogen atom, in ring Y, Y1 represents CRY1, Y2 represents N or CRY2, Y3 represents N or CRY3, Y4 represents N or CRY4, RY1, RY2, RY3 and RY4 each independently represents hydrogen atom; linear or branched C1-6alkyl group, which can be substituted with halogen atom(s); C3-7alkyl group, which has ring structure; linear or branched C1-6alkoxygroup; halogen atom or cyanogroup, in ring Z, RZ represents linear or branched C1-6alkyl group, which can be substituted with halogen atom(s), or C3-7alkyl group, which has ring structure, which can be substituted with halogen atom(s). Invention also relates to particular compounds, DGAT1 inhibitor based on formula (I) compound, application of formula (I) compound, method of prevention or treatment of diseases, mediated by DGAT1 inhibition.
EFFECT: obtained are novel compounds, possessing useful biological activity.
19 cl, 19 tbl, 149 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to chemical-pharmaceutical industry and represents composition for oral cavity care, containing: a) at least one compound of formula M1-A-M2-B-M3, where: M1 and M3 represent Ti or titanium (Ti) oxide; A and B represent C2-C6 dibasic acid; and b) at least one orally acceptable solvent; where composition contains less than 5% of water.
EFFECT: invention provides creation of composition for treatment of teeth hypersensitivity, which effectively seals open dentin canals.
7 cl, 8 tbl, 12 dwg, 1 ex
SUBSTANCE: method comprises dissolving the mixture of birch bark triterpenoids in tetrahydrofuran to obtain the solution with a concentration of 5-10 g/l. Oleic acid is dissolved in an amount of 5-10% by weight of the birch bark triterpenoids. The sterilising filtration of the mixture is carried out. 25-fold excess of 0.01 M tris buffer is added, pH 9.0±0.2, when stirring. Sonication is carried out for 5-10 min. The organic solvent is removed using ultrafiltration on hollow membranes with exclusion threshold of 300 kDa at a rate of 1.0-1.2 L/min at a pressure of 0.6-0.8 atm. Cryoprotectant is added from the group of substances: mannitol, maltose, trehalose, mannose, sorbite, sucrose. The resulting concentrated mixture is frozen.
EFFECT: invention enhances the immunogenic activity of viral vaccines and provides their stability while storage.
2 cl, 2 dwg, 6 tbl, 7 ex
SUBSTANCE: group of inventions refers to an anti-ageing product. Moringa sp. whole seed extract for an anti-ageing effect containing oil and polyphenols representing an extract prepared of a moderately polar solvent. Using Moringa sp. whole seed extract as an active anti-ageing ingredient. Using Moringa sp. whole seed extract for enhancing and recovering a skin barrier function. A cosmetic and/or dermatologic anti-ageing composition. A cosmetic method for the anti-ageing effect in the individuals with mature skin, involving using topical or oral administration of Moringa sp. whole seed extract. A method for preparing Moringa sp. whole seed extract.
EFFECT: extract is effective for the anti-ageing effect.
12 cl, 1 tbl, 5 ex, 1 dwg
FIELD: food industry.
SUBSTANCE: method for production of Siberian cedar seeds liqueur (with hepatoprotective, antioxidant, antihypoxic, hypolipidemic effect) by way of maceration with ethyl alcohol usage; whole Siberian cedar seeds are loaded into the reactor, poured with 70% ethyl alcohol water solution; extraction is performed under preset conditions. The medicinal preparation with hepatoprotective, antioxidant, antihypoxic, hypolipidemic effect contains Siberian cedar seeds liqueur. Usage of the medicinal preparation as a hepatoprotective remedy.
EFFECT: liqueur has pronounced hepatoprotective, antioxidant, antihypoxic and hypolipidemic effect.
6 cl, 3 dwg, 8 tbl
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to cosmetology and dermatology and represents a skin care composition applicable for local skin application, wherein the above composition contains salicylic acid or its salt in a combination with glycyrrhizic acid, or its salt or its derivative, cetylhydroxyproline palmitamide, lactic acid or its salt, bisabolol and niacinamide.
EFFECT: invention provides extending the range of effective skin care agents.
41 cl, 11 ex, 11 tbl
FIELD: medicine, pharmaceutics.
SUBSTANCE: group of inventions concerns oral care compositions effective for treating dental hypersensitivity, and a method of treating using them. The composition contains a compound of formula I: M1-A-M2-B-M1 ; wherein M1 and M3 represent potassium (K); M2 represents Ti or titanium (Ti) oxide; A and B independently represent C2-C6 dibasic acid; and at least one orally acceptable solvent. The oral care composition has pH falling within the range of 2.0 to 7.0. There are also presented a version of the composition, which contains at least one additional desensitising agent, and a method of treating sensitive teeth with the use of this composition.
EFFECT: using the group of inventions provides the effective dental desensitisation by creating a protective barrier on the tooth surface and/or sealing the effective dental tubules effectively.
11 cl, 8 tbl, 12 dwg
SUBSTANCE: invention relates to the field of organic chemistry, namely to novel pyridine derivatives of the general formula
and to their pharmaceutically acceptable salts, where R1 stands for (C1-6) alkyloxy, CN or halogen, R2 stands for a hydrogen atom, R3 stands for a hydrogen atom or (C1-6) alkyl, R4, R5, R6, R7 are similar or different and stand for a hydrogen atom or halogen. The invention also relates to the cosmetic application of the formula (I) compound.
EFFECT: novel pyridine derivatives, useful in the treatment of diseases associated with a receptor of androgens, are obtained.
9 cl, 1 tbl, 16 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to health-promoting compositions and methods for preparing them. A method for preparing the composition of non-living lactic acid bacilli, possessing an ability of specific binding to Streptococcus mutans, involves the following stages: heating a cell suspension of lactic acid bacillus or a mixture of lactic acid bacilli possessing an ability of specific binding to Streptococcus mutans from an initial temperature of less than 40°C to a pasteurisation temperature of 75 to 85°C with a temperature variation within the range of 0.5 to 2°C/min, keeping the heated suspension at a pasteurisation temperature of 20 to 40 minutes and cooling the suspension to a final temperature of less than 40°C within the range of 0.5 to 2°C/min. The specific binding the cell suspension of the lactic acid bacillus or the mixture of lactic acid bacilli to Streptococcus mutans is stable to heat treatment and/or resistant to proteases and/or calcium-dependent and/or is observed within the range of pH values falling within the range of 4.5 and 8.5, and/or in the saliva environment.
EFFECT: invention enables producing the agent preventing or delaying the caries lesion formation.
9 cl, 4 ex
SUBSTANCE: 0.5% dihydroquercetin is instilled into the rectum of a patient with temporary colostomy until he/she starts feeling intestinal inflation. The procedure is performed twice a day, daily up until the restorative surgery.
EFFECT: method reduces a rate and a degree of colitis manifestations by the local antioxidant, anti-inflammatory effect, unfolding the excluded colon.
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to cosmetic industry and represents a cosmetic product which has the following composition in each specific case calculated using the total composition: at least 0.1 wt % of at least one hydrophilic softening product, 2 to 40 wt % of at least one surfactant specified in a group of fatty alcohol ethoxylates, fatty alcohol ether sulphates and salts of sulphated and/or sulphonated fatty acids, 30 to 90 wt % of water, 1 to 30 wt % of one or more abrasives with the total ingredients making 10%; the product contains at least 0.1 wt % of at least one hydrophilic softening product with a hydrophilic-lipophilic balance ≥8 and flour thermally treated by saturated vapour; the flour is natural flour of shell or kernels characterized by a light absorption at wave length 660 nm of less than 1 prepared by reacting the flour 1 g with a solution prepared of water 10 ml and 0.1% aqueous methylene blue 1 ml.
EFFECT: invention provides the lower effect on viscosity, possesses the high cleaning action and high tolerability.
16 cl, 5 ex, 3 tbl
FIELD: medicine, oncology, amino acids.
SUBSTANCE: invention relates, in particular, to the development of an antitumor preparation based on natural substances. Invention relates to an amino acid preparation comprising at least one modified essential amino acid obtained by treatment of amino acid by ultraviolet radiation (UV) at wavelength 250-350 nm for 12-80 h at temperature 15-30oC or with ozone at temperature 15-25oC. The modified amino acid has no toxicity for health cells. Also, invention relates to a method for preparing such preparation. Invention provides the development of an antitumor preparation based on modified amino acids and expanded assortment of antitumor preparations being without cytotoxicity for normal cells.
EFFECT: valuable medicinal antitumor properties of preparation.
8 cl, 4 tbl, 2 dwg, 4 ex