The non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates (A61K47/48)

Nanoparticles carrying chemotherapeutic anti-cancer therapeutic agent // 2616494
FIELD: pharmaceuticals.SUBSTANCE: present invention relates to pharmaceutics, namely to method of treating hepatocellular carcinoma. Method of treating involves administering of nanoparticles to patient containing at least one chemotherapeutic anti-cancer agent representing doxorubicin, at least one poly(C1-C12alkylcyanoacrylate) and at least one cyclodextrin. Nanoparticles are administered by intravenous or intra-arterial infusion for at least 2 hours.EFFECT: invention implementation allows to significantly reduce toxicological adverse effects of doxorubicin nanoparticles and to increase ratio of “benefit/risc”.9 cl, 7 ex, 14 tbl
Complexes based on micro-bubbles and methods of application // 2613321
FIELD: medicine.SUBSTANCE: group of inventions relates to medicine and concerns complex based on micro-bubbles for therapeutic agent delivery to target tissue containing micro-bubble with outer shell containing mixture of native and denatured albumin and hollow core, encapsulating gas perfluorocarbon; therapeutic agent; bifunctional linker. Group of inventions also concerns method of delivering above complex based on micro-bubbles to target tissue.EFFECT: group of inventions provides increased binding of therapeutic agents with micro-bubbles to minimize non-targeted delivery of said agent.17 cl, 4 ex, 10 dwg, 3 tbl
Acne treating method and composition against acne // 2613107
FIELD: cosmetology.SUBSTANCE: invention relates to cosmetology and dermatology and represents composition against acne, containing, at least, one active ingredient, selected from group, including compounds of formula I and formula II based on coumarin and, at least, one pharmaceutically acceptable filler, where amount of said vegetal component ranges from 0.001 to 25% of total weight of composition.EFFECT: invention provides extended range of products applicable for treating acne, high inhibiting activity relative to Propionibacterium acne.13 cl, 1 tbl, 1 ex
Pharmaceutical ketorolac-based composition in form of nasal spray and method for preparation thereof // 2611659
FIELD: pharmaceutics.SUBSTANCE: invention relates to pharmaceutical industry and represents a pharmaceutical composition in form of nasal spray, having analgesic and anti-inflammatory activity, characterized by the fact that it comprises tromethamine ketorolac as an active substance and additives: phenoxyethanol as a antimicrobial preserving agent and antiseptic, poloxamer 407 as a humidifier, disodium edetate as a chelating agent, sodium hydroxide and potassium dihydrogen phosphate as a buffer mixture and a pH regulator and water for injections, wherein ingredients of composition are taken in certain ratio, wt%.EFFECT: invention ensures increased storage life after primary opening up to 20 days, in conditions of a refrigerating chamber, and at room temperature, wider range of nasal sprays, having analgesic and anti-inflammatory activity, as well as storage life of 2 years.2 cl, 7 tbl
Cream for myofascial massage // 2610855
FIELD: pharmaceutics.SUBSTANCE: invention refers to pharmaceutical industry and medicine and represents Myofascial massage cream for treating and preventing of locomotor apparatus diseases, containing “Kapsikam”, indometacin, Dimexidum, “Khondroksid” and Vaseline in weight ratio: 0.1:1:0.1:1:1–6.EFFECT: invention provides pronounced analgesic and preheating effects, enhances blood circulation, reduces swelling and degenerative changes in tissues and joints, improving their mobility.1 cl

Variant forms of urate oxidase and use thereof // 2610680
FIELD: biochemistry.SUBSTANCE: present invention relates to biochemistry, in particular to a conjugate of urate oxidase (uricase), intended for decreasing uric acid levels a subject. Said conjugate comprises isolated shortened mammal uricase, having amino acid sequence SEQ ID NO:11, which is shortened from amine end by 6 amino acids and additionally contains amino acid replacements S46T, D7T, R291K and T301S, and polyethylene glycol. Present invention discloses a pharmaceutical composition for reducing uric acid levels in a subject, as well as a method of decreasing uric acid levels in a subject using said conjugate of uricase and polyethylene glycol.EFFECT: present invention widens the range of products for controlling excess concentration of uric acid (hyperuricemia) in an individual when treating such diseases as gout, gout nodule, renal failure and others.45 cl, 8 dwg, 7 tbl, 8 ex

Antibodies to folic acid receptor 1, their immunoconjugates and application // 2610663
FIELD: biotechnology.SUBSTANCE: invention relates to biotechnology and immunology. Humanized antibody and its antigen-binding fragment are disclosed, specifically binding to human folic acid receptor 1 (FOLR1) and characterized by amino acid sequences of sections determining complementarity with antigen (CDR). Method of producing humanized antibodies under invention; immunoconjugates with cytotoxic agent; pharmaceutical composition; diagnostic composition; kits; methods of inhibiting tumor growth and method of treating cancer are also disclosed. Isolated polynucleotides coding variable domains of disclosed antibodies; vectors containing them and host cells are also disclosed.EFFECT: antibody under invention is humanized form of mouse antibody Mov19 and it can find further application in therapy of diseases characterized by high expression of FOLR1.69 cl, 19 dwg, 4 tbl, 19 ex

New conjugates binding compound - active compound (adc) and use thereof // 2610336
FIELD: medicine.SUBSTANCE: present invention relates to novel conjugates of binding compound – active compound of (ADC) N,N-alkylauristatins targeted against target C4.4a, active metabolites of said ADC conjugates, method of obtaining said ADC conjugates, use of said ADC conjugates for treating and/or preventing diseases, as well as use of these ADC conjugates to produce medicinal agents for treating and/or preventing diseases, more specifically hyperproliferative and/or angiogenic diseases, such as, for example, cancer.EFFECT: such drug treatment can be used in form of single agent therapy or, in another version, in combination with other drugs or additional other therapeutic measures.52 cl, 6 tbl, 128 ex

Respiratory syncytial virus antigenic compositions and methods // 2609661
FIELD: biotechnology.SUBSTANCE: present invention relates to biotechnology. Disclosed are immunogenic compositions in form of a multilayer film, containing B-cell (antibody) epitope of RSV-G169-191 and additionally T-cell epitope of RSV-M281-95 proteins of respiratory syncytial virus (RSV), wherein epitope of RSV-G is located in outer layer of film. Said film comprises two or more layers of polyelectrolytes, where adjacent layers contain oppositely charged polyelectrolytes, containing polycationic substance or polyanionic substance, having molecular weight greater than 1,000, and at least 5 charges per molecule. In addition, described is a method for immunisation against RSV.EFFECT: compositions according to present invention provide increased B-cell response against RSV and can be used in preventing RSV infection.17 cl, 21 dwg, 5 tbl, 19 ex

Prodrugs of active substances with heterocyclic linkers // 2608305
FIELD: pharmaceutics.SUBSTANCE: invention relates to prodrugs of opioid active substance, which provide controlled release of active substance by enzymatic decomposition with further intramolecular cyclization. Invention also relates to compositions, containing prodrugs, and methods for using them.EFFECT: composition can optionally include trypsin inhibitor, which interacts with enzyme, which is mediator in release of active substance from prodrugs in order to attenuate enzymatic splitting of prodrug.16 cl, 17 dwg, 15 tbl, 49 ex
Amphiphilic polymer-metal complexes and synthesis method thereof // 2608304
FIELD: chemistry.SUBSTANCE: invention relates to organic high-molecular compounds, and specifically to novel amphiphilic polymer complexes, a method for production thereof, to a carrier and a composition for delivery of biologically active substances, as well as use of complexes as activators of oxo-biodegradation of carbochain polymers. Polymer complex contains a hydrophilic fragment of an amphiphilic polymer, which is bonded to transition metal ions. Amphiphilic polymer is a homopolymer or random copolymer of general formula H-[-M-]-S-R, wherein [-M-] is a hydrophilic fragment consisting of identical or several different irregularly ordered monomers, selected from a group comprising N-vinylpyrrolidone, N-isopropylacrylamide, N-(2-hydroxypropyl)methacrylamide, ethyleneamine, 2-allyloxybenzaldehyde, acrylamide, N-dialkylacrylamide, maleic anhydride, acrylic, methacrylic, maleic, fumaric, cinnamic acid and esters of said acids; R is a hydrophilic fragment of general structure –(-C8-19alkyl)-CH2-X, where X independently represents H, OH, NH2 or NH3Cl. In amphiphilic polymer at least 1 mol% of monomers are monomers, containing a carboxyl group. Number average molecular weight of amphiphilic polymer ranges from 1 to 30 kDa. Method of producing polymer complexes involves combined incubation of aqueous solution of amphiphilic polymer with aqueous or organic solution of a transition metal salt. Carrier for delivery of biologically active substances is micelles, consisting of said complexes. Composition for delivery of biologically active substances contains at least one biologically active substance and said carrier.EFFECT: invention enables to obtain polymer complexes with high output and high degree of purity, and also to obtain a carrier ensuring high water compatibility of poorly soluble and insoluble biologically active substances.11 cl, 3 dwg, 2 tbl, 9 ex

Liquid dosage form of fenspiride and production method thereof // 2607965
FIELD: pharmaceutics.SUBSTANCE: invention relates to pharmaceutical industry and represents liquid dosage form of fenspiride hydrochloride in form of syrup, including fenspiride hydrochloride, methyl parahydroxybenzoate, propyl parahydroxybenzoate, potassium sorbate, sodium citrate, citric acid monohydrate, sodium saccharinate, noncrystallizing liquid sorbitol, glycerin, honey flavoring agent, fruit flavoring agent, dye E110 and purified water, wherein ingredients of the dosage form are taken in certain proportions, g/100 ml.EFFECT: invention provides extending range of medications, which are liquid dosage forms of fenspiride hydrochloride, stable and long-term storable without use of sucrose.2 cl, 14 dwg, 9 tbl
Enhanced immune response in bovine species // 2606855
FIELD: pharmaceutics.SUBSTANCE: invention relates to pharmaceutics and concerns an immunomodulator composition for treating bovine respiratory disease in cattle caused by Mannheimia haemolytica, which comprises a cationic liposome delivery vehicle and nucleic acid molecule, where nucleic acid molecule is a bacterially-derived non-coding DNA plasmid vector, produced in E.coli, containing 4242 base-pairs without a gene insert.EFFECT: invention provides a eliciting systemic, non-specific and antigen-specific immune responses in animals for protection against infectious respiratory disease.11 cl, 6 ex, 6 tbl, 27 dwg
ethod of producing modified alginate microspheres // 2606843
FIELD: biotechnology.SUBSTANCE: invention relates to investigation of biomaterials and tissue engineering, namely, to a method of producing modified alginate microspheres, involving liver decellularization, its mechanical slicing and further mechanical milling to produce microparticles of decellularized liver, that is fixed by covalent binding on preliminary prepared alginate microspheres, modified using modifying agents, such as hydroxysuccinimide (NHS) and hydrochloride N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (EDC). Invention provides high density of microparticles of decellularized hepatic tissue on the surface of modified alginate microcarriers and a strong covalent bond between them.EFFECT: proposed modified alginate microspheres can act as biodegradable container for biologically active substances and/or cells, as well as to protect the cells, encapsulated inside alginate microcarriers from act of recipient's immune system when implanted.7 cl, 3 dwg

Composition for treating diabetes, containing long-acting insulin conjugate and long-acting insulinotropic peptide conjugate // 2606840
FIELD: pharmaceutics.SUBSTANCE: invention relates to pharmaceutical industry and concerns composition for preventing or treating diabetes, as well as method of treating diabetes. Long-acting insulin conjugate and long-acting insulinotropic peptide conjugate are obtained by binding insulin or insulinotropic peptide with region of immunoglobulin Fc via non-peptide linker to improve duration of effect and stability in vivo. Accompanying administration of long-acting conjugate of insulin and long-acting insulinotropic peptide conjugate inhibits increase of body weight, caused by insulin treatment, vomiting and nausea, caused by insulinotropic peptide treatment, and reduces required dose of insulin.EFFECT: invention consists in fact that composition contains long-acting insulin conjugate and long-acting insulinotropic peptide conjugate.20 cl, 3 dwg, 4 ex

ultimer non-peptide polymer-insulin and method for its production // 2606262
FIELD: biotechnology.SUBSTANCE: invention relates to biotechnology, specifically to complex of hexamer non-peptide polymer conjugate and insulin with ions of trivalent cobalt, and can be used in medicine. Invention enables to obtain stable hexamer form of insulin, associated with non-peptide polymer with increased life time and preserving function of glucose level control in blood.EFFECT: obtained complex can be used in pharmaceutical composition for treating diabetes.15 cl, 4 dwg, 2 tbl, 7 ex

System of intraventricular drug delivery to improve outcome after brain damage, violating cerebral blood circulation // 2606169
FIELD: medicine.SUBSTANCE: group of inventions relates to medicine, namely to neurology, neurosurgery and pharmacology, and can be used for therapeutic treatment of delayed state complication, wherein blood gets into subarachnoid space. Application of microdispersed composition is proposed for preparing drug for treating such conditions. Composition contains powder suspension of microparticles, containing therapeutic amount of agent, selected from group consisting of calcium channel antagonist, endothelin antagonist (ET) and antagonist of channels with transitory receptor potential (TRP), impregnated in matrix or on matrix of biopolymer, and pharmaceutical carrier, which gives viscosity to composition. Microparticles have uniform distribution of size of microparticles. Average particle size is 66 μm. Each microparticle contain at least 40 wt% of therapeutic agent. Method of treatment is also disclosed, which involves use of said microdispersed composition. Sterile set comprises microdisperse composition and syringes with suspension and pharmaceutically acceptable carrier. Method for obtaining microdispersed composition involves use of said set.EFFECT: use of inventions provides gradual release of therapeutic agent for long period of time and introduction into brain ventricle so, that therapeutic composition contacts and flows, at least one cerebral artery in subarachnoid space, not entering system of blood flow in amount, which causes undesirable side effects.23 cl, 21 dwg, 6 tbl, 1 ex
ultivalent composition based on pneumococcal polysaccharide-protein conjugates // 2606152
FIELD: medicine.SUBSTANCE: group of inventions relates to medicine, specifically to immunology, and can be used for preparing an immunogenic composition. Multivalent immunogenic composition contains 13 different polysaccharide-protein conjugates with a physiologically acceptable medium. Each of polysaccharide-protein conjugates contains capsular polysaccharide from separate serotype Streptococcus pneumoniae, conjugated with carrier protein CRM197. Capsular polysaccharides are obtained from 12 serotypes, selected from a group consisting of 1, 3, 4, 5, 6A, 6B, 7F, 9V, 14, 18C, 19A, 19F and 23F, and serotype 2 or 9N. Group of inventions also relates to a pharmaceutical composition for inducing immune response to capsular polysaccharide conjugates Streptococcus pneumoniae.EFFECT: use of one type of carrier protein conjugated with encapsulated polysaccharides in a multivalent vaccine enables to avoid possible immune interference.7 cl, 3 ex

Polyvalent composition containing pneumococcal polysaccharide-protein conjugates // 2605834
FIELD: medicine.SUBSTANCE: group of inventions relates to medicine, specifically to immunology, and can be used for preparing immunogenic composition. Multivalent immunogenic composition contains 15 various polysaccharide-protein conjugates, as well as physiologically acceptable base. Each of polysaccharide-protein conjugates contains capsular polysaccharide, obtained from different serotypes of Streptococcus pneumoniae, conjugated with protein CRM197, wherein capsular polysaccharides are obtained from serotypes 1, 2, 3, 4, 5, 6A, 6B, 7F, 9N, 9V, 14, 18C, 19A, 19F and 23F. Group of inventions also relates to pharmaceutical composition made in form of single dose of 0.5 ml, containing: 2 mcg of each saccharide, except 6B, which is in amount of 4 mcg; approximately 34 mcg of carrier-protein CRM197; adjuvant based on 0.125 mg of elementary aluminium (0.5 mg of aluminium phosphate) and buffer based on sodium chloride and sodium succinate as filler. Immunogenic composition made in form of vaccine, containing aluminium adjuvant, allows to increase range of application on pneumococcal diseases.EFFECT: use of one type of carrier-protein conjugated with encapsulated polysaccharides in multivalent vaccine, allows avoiding possible immune interference.7 cl, 4 ex, 15 dwg, 3 tbl

Growth hormones with prolonged efficacy in vivo // 2605627
FIELD: biotechnology.SUBSTANCE: invention relates to biotechnology. Conjugate of growth hormone (GH) is disclosed, containing GH with single mutation of Cys addition, selected from A98C, N99C, L101C and V102C, and albumin-binding radical, attached through hydrophilic spacer to sulphur atom of this single Cys. Conjugate of growth hormone with specific alternative hydrophilic spacers for attachment of albumin-binding radical is also disclosed.EFFECT: this invention can be used in production of growth hormone conjugates with increased stability and longer half-life in vivo.14 cl, 2 dwg, 6 tbl, 51 ex

Rectal polycomplex gel for treatment of ulcerative colitis, crohn's disease, fistulas and complications caused by these diseases // 2605615
FIELD: pharmaceutics.SUBSTANCE: invention relates to pharmaceutical industry and represents rectal polycomplex gel for treatment of ulcerative colitis, Crohn's disease, fistulas and complications, caused by these diseases characterized by that it contains metronidazole, timogen, carbopol, propylene glycol, disodium EDTA, propyl parahydroxybenzoate, methyl parahydroxybenzoate, sodium hydroxide and water, wherein ingredients of gel are taken in certain proportions, g/150 g.EFFECT: invention provides higher clinical effectiveness in treatment of non-infectious inflammatory diseases of intestinal-digestive tract, reduced length of treatment.1 cl, 3 ex, 3 tbl
Agent for reduction of glutamate-induced apoptosis and inhibition of nmda-receptor, possessing immunomodulatory action, for treating nervous system disorders, effects of craniocereberal injury and ischemic and hemorrhagic stroke // 2605339
FIELD: medicine; pharmaceuticals.SUBSTANCE: invention relates to medicine and pharmaceutical industry and represents therapeutic agent, based on amantadine sulphate, for reduction of glutamate-induced apoptosis and inhibition of NMDA-receptors for treating nervous system disorders, effects of craniocereberal injury and ischemic and hemorrhagic stroke, characterized by that it contains therapeutically effective amount of amantadine sulphate and cytidine 5'-diphosphocholine as active substance, as well as at least one auxiliary substance, selected from group consisting of stabilizers, prolongators, buffering additive solvents, fillers, preserving agents, ingredients are taken in certain ratio, wt%.EFFECT: invention provides extending of range of products for reduction of glutamate-induced apoptosis and inhibition of NMDA-receptors for treating disorders of nervous system, effects of craniocereberal injury and ischemic and hemorrhagic stroke, increase of clinical effectiveness, stability at room temperature, long storage life, at least 3 years.4 cl, 3 ex, 3 tbl

Nasal antimicrobial agent // 2605313
FIELD: pharmaceutics.SUBSTANCE: invention refers to pharmaceutical industry and represents a nasal antimicrobial therapeutic agent containing active and auxiliary materials differing by the fact, that ciprofloxacin hydrochloride antibiotic is selected as active material, and as auxiliary materials are selected - propylene glycol, macrogol glyceryl hydroxystearate, benzalkonium hydrochloride, purified water, wherein the ingredients in the preparation are taken in certain proportions, wt%.EFFECT: invention provides expansion of the range of nasal application antibacterial agents for treating rhinitis, rhinopharyngitis and sinusitis.3 cl

odified binding proteins, inhibiting interaction of vegf-a receptor // 2605309
FIELD: biotechnology.SUBSTANCE: invention relates to biotechnology. Present invention relates to binding proteins, specific to VEGF-A, in particular to recombinant binding proteins, containing polyethyleneglycol fragment and binding domain, which inhibit binding of VEGF-Axxx with VEGFR-2. Examples of such recombinant binding proteins are proteins, which contain anchored binding domain, repeated with desired specificity, and polyethyleneglycol fragment.EFFECT: binding proteins are effective in treating cancer and other pathological states, for example eye diseases, such as age related macular degeneration.18 cl, 8 dwg, 5 ex

Combination of components for improvement of physical parameters in individuals involved in heavy physical activity // 2605280
FIELD: pharmaceutics.SUBSTANCE: invention refers to pharmaceutical industry and represents a composition for maintaining and/or restoring body during and/or after heavy physical activity, containing L-taurine, L-leucine, L-isoleucine, L-valine, extract of green tea leaves, yohimbine hydrochloride, spiny eleutherococcus rhizomes and roots extract, rhaponticum carthamoides rhizomes and roots extract, rhaponticum rhodiola rosea rhizomes and roots extract, bitter orange peel extract, riboflavin sodium phosphate, choline alfoscerate, calcium pantothenate, pyridoxine hydrochloride, folic acid, cyanocobalamin, biotin, nicotinamide, L-carnitine, beta-alanine, potassium orotate, methyluracil, inosine, caffeine, extract of leaves, blossom clusters and blooming sally rhizomes, creatine monohydrate, L-tyrosine, ascorbic acid, magnesium in the form of a bis-glycinate, copper in the form of a bis-glycinate, zinc in the form of a bis-glycinate, L-glutamine, thiamine hydrochloride, cholecalciferol 5000 ME, calcium malate, sodium dihydrogen phosphate, alpha-tocopherol acetate, L-selenomethionine, olive leaf extract, extract of peppermint leaves, leaf extract of goose-tongue, extract of common valerian roots and rhizomes, retinol palmitate and water, the ingredients of the composition are in certain ratio in milligrams.EFFECT: invention provides higher capacity of the body to withstand intensive physical activity, achievement of endurance and faster recovery of the body after the volume of training and heavy physical operation, adequate power supply during the whole period of intensive physical activity, accelerated recovery of the body after its completion, not resulting in depletion of nutrients in the central nervous system and skeletal muscles.10 cl, 3 tbl, 7 ex

Chemical synthesis and anticancer and antimetastatic effects of dual functional conjugate // 2604718
FIELD: chemistry.SUBSTANCE: invention relates to dual functional conjugate of formula i, where docetaxel is linked with muramyl dipeptide derivative, which enables to achieve anticancer and antimetastatic effect. Method of producing conjugate is carried out by combination of solid-phase and liquid-phase synthesis.EFFECT: invention also discloses a pharmaceutical composition and use of conjugate for producing anti-tumour drugs.21 cl, 29 dwg, 13 tbl, 51 ex

Glucagon superfamily peptides exhibiting nuclear hormone receptor activity // 2604067
FIELD: pharmaceutics.SUBSTANCE: invention relates to novel conjugates of glucagon superfamily peptides, which are conjugated with the ligand that is capable of acting at a nuclear hormone receptor of type I.EFFECT: present invention also refers to pharmaceutical compositions containing said conjugates, and methods of treating a disease, for example, a metabolic disorder, diabetes or obesity.15 cl, 19 dwg, 15 tbl, 31 ex
Composition containing amyloidal peptide aβ-1-6 attached to virus-like particle and adjuvant // 2603486
FIELD: medicine.SUBSTANCE: group of inventions refers to pharmaceutics and medicine and concerns a composition for treating and/or preventing dementia, Alzheimer's disease, dementia associated with Alzheimer's disease, or related with the above said diseases conditions, containing 450 mcg of a structure containing peptide Aβ1-6 consisting of a structure of a virus-like particle (VLP) chemically attached to the peptide Aβ1-6 through a divalent linker succinimidyl-6-(b-maleimide propionamido)hexanoate, where the VLP consists of capsid RNA proteins of bacteriophage Qβ and where peptide Aβ1-6 is combined on C-end with the spacer sequence of GGC and with 450 mcg of pharmaceutically acceptable adjuvant, which is a salt of aluminium. In another version the invention is a vaccine, a combination, an application of the composition and a kit.EFFECT: group of inventions provides at weaker immune reactions decreasing of the rate of microbleedings and treatment at early stages of a disease.12 cl, 2 tbl, 4 ex

Conjugation of staphylococcus aureus type 5 and type 8 capsular polysaccharides // 2603267
FIELD: biochemistry.SUBSTANCE: present invention relates to biochemistry, particularly to a method of producing a conjugate of S.aureus type 5 or type 8 capsular polysaccharide and a carrier protein. Method involves a step for depolymerisation of capsular polysaccharide by acid hydrolysis to obtain polysaccharide fragment, step for oxidising fragment for introduction of an aldehyde group into at least one saccharide residue in fragment to produce an oxidised saccharide residue and a step of binding oxidised saccharide residue with carrier protein through an aldehyde group. At oxidation step two vicinal hydroxyl groups of polysaccharide are converted to aldehyde. Present invention provides a conjugate of S.aurens type 5 or type 8 capsular polysaccharide and carrier protein, obtained using said method, and an immunogenic composition including said conjugate.EFFECT: present invention improves immunological properties of obtained conjugate.13 cl, 18 dwg, 8 tbl, 1 ex

Peptide drugs with high effectiveness against insulin resistance // 2602801
FIELD: chemistry.SUBSTANCE: invention relates to peptides (glucagon and/or GLP-1 and analogues thereof), covalently bound with surface-active glycosides, intended for treating or preventing disorders associated with insulin resistance.EFFECT: modification of peptides promotes longer action and/or increased bioavailability of peptides.17 cl, 1 tbl, 3 dwg, 8 ex

Combined preparation for treating fungus diseases of nails // 2601896
FIELD: pharmaceutics.SUBSTANCE: invention refers to pharmaceutical industry and represents a combined preparation for treating for the fungus diseases of nails containing terbinafine and/or its physiologically acceptable salt, econazole and/or its physiologically acceptable salt, as well as hydroxypropyl cellulose, methacrylic acids and ethyl acrylate copolymer, propylene glycol and ethyl alcohol, at that the ingredients of the preparation are taken in certain proportions, w/w %.EFFECT: invention provides a high therapeutic activity, absence of irritant action and toxicity, stability during storage, it provides optimum drying time, high adhesion to the nail, formation of a layer, which is not removed from the nail surface upon contact with water.1 cl, 1 tbl

Amatoxin-conjugates with improved linkers // 2601411
FIELD: medicine.SUBSTANCE: invention relates to tumour therapy. In one aspect, the present invention relates to conjugates of an amatoxin and a target-binding moiety, for example, an antibody, connected by a linker comprising a urea moiety, which are useful in the treatment of cancer. In a further aspect the invention relates to pharmaceutical compositions comprising such conjugates, and a method for synthesizing said conjugates.EFFECT: conjugates that are stable in plasma, so that harmful side effects to non-target cells are minimized.14 cl, 9 dwg, 6 ex

New oligonucleotides conjugates and use thereof // 2599449
FIELD: biochemistry.SUBSTANCE: described is group of inventions involving structure therapeutic agent delivery oligonucleotide polymer nano particle oligonucleotide delivery, containing above therapeutic agent-polymer, conjugate anti-sense oligonucleotide (ASO)-polymer for delivery of anti-sense oligonucleotide polymer, nano particle for delivery of anti-sense oligonucleotide containing above conjugate ASO-polymer and method of conjugate ASO-polymer producing.EFFECT: invention extends range of products, ensuring delivery of oligo-RNA in organism.27 cl, 21 dwg, 12 ex
Composition for healing oral cavity tissue // 2599026
FIELD: pharmaceutics.SUBSTANCE: invention relates to pharmaceutical industry, medicine and dentistry and presents a composition for healing oral cavity tissue, containing astaxanthin, vitamin E, coenzyme Q, propylene glycol, methyl ether of 4-hydroxybenzoic acid, propyl ether of 4-hydroxybenzoic acid, carbopol, triethanolamine and purified water, wherein components are taken in a certain ratio, wt%.EFFECT: invention provides more effective orthopaedic treatment of patients using removable dentures, as well as patients with inflammatory periodontal diseases, does not cause allergic reactions and side effects.1 cl, 3 ex

Composition based on nanoparticles with improved penetration through mucous membranes // 2598627
FIELD: pharmaceutics.SUBSTANCE: group of inventions refers to pharmaceutical industry, namely to hypotonic composition for fast and uniform distribution of therapeutic, prophylactic, diagnostic or nutriceutical mucosal surface agent containing particles, penetrating through mucus, which contain therapeutic, prophylactic, diagnostic or nutriceutic agent and polyalkylene oxide coating, improves penetration through mucus, which improves diffusion of particles through mucus, where the coating has coefficient of density [G]/[G*]>3 , where l is density polyethylene glycol, which characterises the number of molecules of polyethylene glycol at 100 nm2 surface particles while G* is complete coating the surface of particles of which characterises the theoretical number of free molecules of polyethylene glycol, required for full coverage of 100 nm2 surface particles, as well as to a method of introducing one or more therapeutic, prophylactic and/or diagnostic agents to a human or animal with the help of said compositions.EFFECT: group of inventions ensures manufacturing of particles, penetrating through mucus, completely protected against adsorption of mucus.21 cl, 23 dwg, 8 tbl, 10 ex

Inhibitor of liquid in cavities of body accumulation // 2597795
FIELD: pharmaceutics.SUBSTANCE: invention refers to pharmaceutics and concerns drug for inhibiting accumulation of liquid into mammals body cavity, having accumulation of liquid in cavity of body, caused by cancer, as active substance containing covalent conjugate of interferon-beta with polyethylene glycol.EFFECT: invention provides effective treatment and removal of liquid from body cavity by systemic administration as well as by local administration.9 cl, 6 dwg, 6 ex

ethod for creating personalized gene-activated implant for bone tissue regeneration // 2597786
FIELD: medicine.SUBSTANCE: present group of inventions relates to medicine. Invention discloses a personalized gene-activated implant for bone defect replacement in a mammal and method for production thereof, involving computed tomography of the bone grafting area, simulating the bone defect, 3D printing the form of a biocompatible carrier and combination of the biocompatible carrier with nucleic acids. Disclosed is a method for treating bone defects or bone tissue atrophy in a mammal, comprising implantation of a personalized gene-activated implant in bone tissue.EFFECT: presented group of inventions provides the effective means and methods for bone defect replacement in a mammal with the help of 3D-reconstruction.4 cl, 7 dwg, 2 ex

Composition of lipid vesicles and methods of application // 2595872
FIELD: medicine.SUBSTANCE: group of inventions relates to multilayer lipid vescible for delivery of therapeutic, prophylactic or diagnostic agent having a covalent crosslinks between lipid bilayers, wherein at least two lipid bilayers in multilayer lipid vesicle are covalently crosslinked to each other, as well as methods for production thereof, to methods of delivery of therapeutic, prophylactic or diagnostic agent and to pharmaceutical compositions containing such multilayer lipid vesicle.EFFECT: higher efficiency of encapsulation and stability of multilayer lipid vesicles.93 cl, 29 dwg, 3 tbl, 2 ex

Pi3-kinase inhibitors and use thereof // 2595718
FIELD: pharmaceutics.SUBSTANCE: invention relates to compounds which are irreversible PI3-kinase inhibitors, and conjugates containing one or more PI3-kinases, containing cysteine residue, which is covalently and irreversibly boned with PI3-kinase inhibitor. Invention also discloses pharmaceutical compositions containing said compounds.EFFECT: compounds are intended for treating disorders and diseases associated with PI3-kinase.19 cl, 16 dwg, 26 tbl, 52 ex

Conjugates of blood coagulation proteins // 2595442
FIELD: chemistry.SUBSTANCE: group of inventions relates to materials and methods of conjugation polysialic acid (PSA) containing active amino oxy group, with oxidized carbohydrate fragments of protein coagulation, including contact oxidised carbohydrate fragment with an activated PSA in conditions which enable to conjugation. Conjugation is carried out by incubation in buffer containing oxidant, selected from group consisting of sodium periodate (NaIO4), lead tetra acetate (Pb (OAc)4) and potassium perruthenate (KRuO4).EFFECT: obtained using said method conjugates have high activity.16 cl, 8 dwg, 3 tbl, 28 ex
ethod of maturated liver residual cavity treating after echinococcectomy // 2593785
FIELD: medicine. SUBSTANCE: invention refers to medicine and aims at treating maturated liver residual cavity after echinococcectomy. Residual liver cavity is treated with "Bemetrim" preparation consisting of (g/100 ml): pepsin powder 4.0-4.5 g; betaine hydrochloride 4.0-4.5 g; methyluracil 3.0-4.0 g; trimecaine 2.0-3.0 g; polyethylene oxide 400 87.0-84.0 ml. First stage is washing residual cavity through drainage tube with micro irrigator with usual antiseptic solution. Then "Bemetrim" preparation is introduced in amount of 2/3 of residual cavity volume and drain tube and micro irrigator are closed for 2 h. Through 2 hours evacuation of residual cavity contents by suction is performed. Therapeutic course is 1 procedure a day, 15±1.0 day. EFFECT: method provides increase in active surface of action and, as result, effective penetration of antiseptic in folds of residual cavity without injuring walls of fibrous capsule, has necrolytic, bactericidal, local anesthetic, draining, cytoprotective, buffer, stimulating regeneration effect and provides higher clinical effectiveness. 1 cl, 2 ex

Prodrugs containing exendin conjugate-linker // 2593774
FIELD: medicine. SUBSTANCE: invention relates to an exendin prodrug, which is characterised by a chemical structure including an exendin fragment, linker fragment and hydrogel, connected with linker fragment. Hydrogel consists of frame fragments with quaternary carbon of formula C(A-Hyp)4, where A is -(CH2)n1(OCH2CH2)nX1-; n1=1-2; n=5-50; X1 is a chemical functional group covalently bonding A and Hyp. Hyp consists of 5 to 32 lysine residues. Frame fragments of hydrogel are cross-linked by cross-linking fragments based on poly(ethylene glycol). Invention also relates to methods of producing prodrugs and to a pharmaceutical composition containing prodrug. EFFECT: prolonged action of prodrug and prolonged half-life. 18 cl, 20 ex, 1 dwg, 1 tbl
Cross-linked polymers and implants derived from electrophilic-activated polyoxazoline // 2593755
FIELD: chemistry. SUBSTANCE: invention relates to biocompatible with glue for fabric, covalently cross-linked polymer, a kit for producing cross-linked polymer, as well as to a medical product and biocompatible medical article. Kit for preparing biocompatible cross-linked polymer contains electrophilically activated polyoxazoline (EL-POX) and nucleophilic cross-linking agent, which are not identical. Polymer EL-POX has molecular weight of at least 5,000 g/mol, and has m electrophilic groups. Nucleophilic cross-linking agent contains n nucleophilic groups. Wherein m electrophilic groups are capable of reacting with n nucleophilic groups to form covalent bonds, where m ≥ 2, n ≥ 2, and m + n ≥ 5. At least one of m electrophilic groups is a lateral electrophilic group. Number of electrophilic groups m can be at least 13. Polymer EL-POX contains excess amount of electrophilic groups in relation to number of nucleophilic groups. Covalently cross-linked polymer contains free electrophilic groups, which are not coming into a reaction with nucleophilic groups of cross-linking agent. Biocompatible medical product contains at least 1 wt% of said covalently cross-linked polymer and represents an implant sealant for fabric, an adhesive tape for fabric, an adhesive film for fabric material for surgical suture, stent with polymer coating, haemostatic (porous) material. Adhesive tape and adhesive film include glue for fabric. EFFECT: invention enables to obtain biodegradable polymer, having excellent film-forming capacity, and good characteristics of implant and/or sealant. 15 cl, 8 ex
Nicotine replacement cytisine oral atomised liquid and method of its preparation // 2593362
FIELD: pharmaceutics. SUBSTANCE: invention refers to pharmaceutical industry and represents a nicotine replacement cytisine oral atomised liquid containing the following components per 1 l of the oral atomised liquid: tobacco extract - 0.1-10 wt%, water extract of cocoa - 0.3-15 wt%, cytisine - 0.1-0.9 wt%, Tween 80 - 0.1-0.5 wt% and the base - 75-90 wt%. EFFECT: invention ensures the following advantages: adding natural aromatic ingredient from plants into the nicotine replacement cytisine oral atomised liquid provides pleasant aroma, more close to flavour of cigarettes, that brings the user sensations close to the ones of natural smoking, and also the invention allows to preserve natural aroma of nicotine replacement cytisine oral atomised liquid for a long time, to improve flavor of the liquid for electronic cigarettes, to improve taste of the liquid for electronic cigarettes and to reduce nicotine dependence. 5 cl, 6 ex

Pharmaceutical composition for topical application in treating and/or preventing infections of skin damages // 2591832
FIELD: pharmaceutics.SUBSTANCE: invention is a topical composition in form of an aerosol powder for treatment and/or prevention of infection of skin lesions containing silver sulfadiazine and at least one silicate, characterised in that said composition contains silver sulfadiazine in an amount from 0.1 to 5 wt% relative to total weight of composition, at least one silicate in an amount of 92 to 99 wt% relative to total weight of composition, and a pharmaceutically acceptable excipient - balance, wherein pharmaceutically acceptable excipient has a particle size less than 13 mcm, and/or 90 % of particles have a size of from 5 to 10 mcm, and/or 50 % of particles are smaller than 4 mcm and wherein silicate is selected from hydrated magnesium silicate, aluminum silicate, calcium silicate or mixtures thereof.EFFECT: invention provides intensified therapeutic effectiveness.11 cl, 2 dwg, 2 ex

Agent for treating intestinal infections and conditions caused by dysbacteriosis, "biobalance a" // 2589843
FIELD: pharmaceutics.SUBSTANCE: invention refers to pharmaceutical industry, namely, to a preparation for treatment of intestinal infections and conditions caused by dysbacteriosis (versions). Preparation in liquid form consists of Lactobacillus acidophilus of strain 100 AC 1×109-1×1010 CFU/g and nutrient medium for cultivation of lactobacteria in certain ratio of components. In the form of tablets, the preparation consists of Lactobacillus acidophilus of strain 100 AC 1×1010 CFU/g, calcium stearate, talc, girasol and lactose in certain ratio of components.EFFECT: preparations described above are characterised by an increased probiotic activity, accelerated resettlement of normoflora on mucous membranes, higher stability (for 60 days).2 cl, 1 tbl, 4 ex
Injectable composition based on group b vitamins and lidocaine // 2589824
FIELD: pharmaceutics.SUBSTANCE: invention relates to pharmaceutical industry and medicine and represents a pharmaceutical composition for parenteral administration in diseases and disorders associated with syndromes of nervous system of various origin, including from 4.5 to 6.25 wt% thiamine hydrochloride, from 4.5 to 5.5 wt% pyridoxine hydrochloride, from 0.045-0.055 % cyanocobalamin, from 0.9 to 1.1 wt% lidocaine hydrochloride, 0.105 to 0.095 wt% sodium hexapolyphosphate, from 0.95 to 1.05 wt% linear sodium polyphosphate, from 0.009-0.015 wt% potassium ferricinide (III), sodium hydroxide to pH 4.54 ± 0.05, from 1.8 to 2.2 wt% benzyl alcohol and water for injections - balance.EFFECT: invention provides high stability of preparation for up to 2 years at temperature higher than 15 degrees Celsius, as well as avoiding formation of suspension in injection solution.4 cl, 1 ex

etabiotic composition to ensure colonisation resistance of human intestinal microbiocenosis // 2589818
FIELD: medicine.SUBSTANCE: invention can be used for production of meta-biotic composition to ensure colonisation resistance of human intestinal micro-biocenosis. Meta-biotic component is a rational combination of metabolites of probiotic strains of microorganisms and additionally includes sterilised dried culture liquids containing metabolites of Enterococcus faecium L-3, Lactobacillus delbrueckii TS1-06 and Lactobacillus fermentum TS3-06. Prebiotic component is represented by oat flakes. Composition is presented in a solid dosage form in the shape of capsules, and the number of ingredients in one capsule constitutes, MP: sterilised dried culture liquid containing metabolites of a probiotic strain of bacteria Bacillus subtilis VKPM No. B-2335 - 1.9; the sterilised dried culture liquid containing metabolites of probiotic strain of bacteria Enterococcus faecium L-3 - 4.5; the sterilised dried culture liquid containing metabolites of probiotic strain of bacteria Lactobacillus delbrueckii TS1-06 - 4.5; the sterilised dried culture liquid containing metabolites of probiotic bacterial strain Lactobacillus fermentum TS3-06 - 4.5; zeolite - 64.3; oat flakes - 20.0; calcium stearate or aerosil - 0.3.EFFECT: use of this composition allows to normalise microbiocenosis of the intestine due to selective stimulation of growth and reproduction of Lactobacilli and bifidus bacteria of indigent component of normoflora of a biotope providing specific antagonistic activity with respect to a wide range of pathogenic and opportunistic microorganisms.1 cl, 4 dwg, 19 tbl

ethods of producing a stable liquid drugs and compositions thereof // 2589697
FIELD: medicine.SUBSTANCE: invention describes a method for administering a pharmaceutically active compound to patient. Method includes obtaining a powdered composition, mixing composition with a liquid or semi-solid product to obtain a stable solution or dispersion and oral administration of solution or dispersion to a patient. Powdered composition contains from 1 to 30 wt% of pharmaceutically active compounds and from 70 to 99 wt% of protein, where protein is a bovine serum albumin or human serum albumin. Pharmaceutically active compound is characterised as lipophilic or hydrophobic, capable of binding with protein plasma and orally biologically available. Albumin is not covalently bound with pharmaceutically active compound. Present invention also provides liquid or semi-solid preparations of composition; method of producing compositions and pharmaceutical kit containing composition.EFFECT: compositions are characterised by intensification of absorption and bioavailability of drug.38 cl, 4 dwg, 4 tbl, 5 ex

Haemoglobin composition // 2589254
FIELD: medicine.SUBSTANCE: group of inventions concerns a composition for therapeutic delivery to tissue oxygen or carbon monoxide, containing a covalent conjugate functional natural haemoglobin molecule and at least one polyethylene glycol molecules, a water-soluble stabilizing component, a diluent. Group of inventions also concerns a method for preparing said composition; using said composition for preparing a drug for delivery of oxygen or carbon monoxide in tissue.EFFECT: group of inventions provides oxygen delivery to tissues and improved stability of the composition during storage.27 cl, 3 ex, 6 dwg, 4 tbl
 
2551408.
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