Cations of monovalent metals of dry powders for inhalations

FIELD: pharmacology.

SUBSTANCE: dry powders for treatment of respiratory diseases, consisting of inhaled dry particles, including salts of monovalent metals in quantities of at least 3% of the weight of dry particles and a pharmaceutically active substance, which represents an antibiotic, LABA, LAMA, a corticosteroid or a combination thereof. At that, dry particles in the dry powders are characterized by a volume geometric mean diameter of 5 mcm or less, tundish density between 0.45 g/cm3 and 1.2 g/cm3 and ratio of the volumetric mean geometric diameter measured at a dispersion pressure of 1 bar divided by the volumetric mean geometric diameter measured at a dispersion pressure of 4 bar is less than 1.5. Also, dry powders application for the manufacture of drugs for treatment and prevention of respiratory diseases and their exacerbations are disclosed.

EFFECT: due to high dispersibility of dry particles, the group of inventions allows treatment and prevention of respiratory diseases through dry powders inhalation into the lungs of the patient, using only the energy of inhalation, without application of carrier particles or active inhalers.

22 cl, 20 dwg, 28 tbl, 17 ex



Same patents:

FIELD: medicine.

SUBSTANCE: group of inventions refers to medicine, particularly to treating bronchopulmonary dysplasia. A method involves administering an effective amount of citrulline into the patient. What is also presented is a pharmaceutical composition applicable for intravenous administration, containing a pharmaceutically acceptable carrier and an amount of citrulline effective for increasing blood plasma citrulline. The level is measured by comparing plasma citrulline in the patient under treatment to that in the patient having no bronchopulmonary dysplasia. The given composition is presented for producing a preparation for injections.

EFFECT: inventions provide the effective treatment of bronchopulmonary dysplasia by the polycomponent effect of citrulline on the disease process.

11 cl, 8 dwg, 2 tbl, 4 ex

FIELD: medicine.

SUBSTANCE: claimed invention relates to capsule for application with inhalator of dry powder, which contains composition in form of dry powder for pulmonary introduction, which contains mechanosynthesised microparticles, consisting of antibiotic and magnesium stearate.

EFFECT: invention relates to method of obtaining claimed capsule and its application in treatment of bacterial infection, associated with certain lungs diseases.

10 cl, 4 ex, 3 tbl, 1 dwg

FIELD: medicine.

SUBSTANCE: combined application of the following medications by children additionally to basic step-wise therapy is administered: Enterosgel per orally 1.5-2 hours before or 2 hours after meal or after application of medications to children from 5 to 10 years old - 15 g 2 times per day, from 11 to 15 years - 15 g 3 times per day with 7-day course; Polyoxydonium by injection intramuscularly in dose by 0.1 mg/kg of child weight injections with interval 1-2 days with course duration 5-8-10 days; Reamberin 1.5% solution by injection drop-wise at age from 5 to 10 years - 200 ml 1 time per day or every second day, from 11 to 15 years - 400 ml 1 time per day or after day, in quantity 5-7 injections; Phenibutum per orally after meal in age dosing under 8 years - by 0.05-0.1 g per intake, over 8 years - 0.25 g per intake 2 times per day, with 30 day course, with course of combined application of said medications is realised 3-4 times per year.

EFFECT: effective prevention of uncontrolled forms of bronchial asthma development in children above 5, associated with influence of chemical toxicants - manganese and vanadium, which comes from atmospheric air, increase of organism resistance to claimed toxicants.

4 tbl

FIELD: medicine.

SUBSTANCE: what is presented is using Histochrom (same as echinochrome A or pentahydroxyethyl naphthoquinone) as an agent able to prevent pulmonary fibrosis developed under cytostatic agents. The invention can be used for the pharmacological prevention and correction of the pulmonary tissue disorders caused by administering the cytostatic agents.

EFFECT: preventing hypertrophy of interalveolar connective tissue in the lungs associated with administering bleomycin.

4 dwg, 1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a compound of formula , which is a methylhydrofumarate (MHF) prodrug. In formula (I), radicals and symbols have the values specified in the patent claim. The invention also refers to a pharmaceutical composition containing the declared methylhydrofumarate drugs, to using the declared methylhydrofumarate drugs and the pharmaceutical composition containing them, for treating diseases, such as psoriasis, asthma, multiple sclerosis, inflammatory intestinal disease and arthritis, and to a method of treating the above diseases.

EFFECT: higher oral bioavailability and plasma MHF, dimethylfumarate and/or other metabolites.

47 cl, 1 tbl, 54 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel compounds of formula I, possessing ability of binding with delta-opioid receptors. In formula R1 is selected from the group, consisting of i) phenyl, optionally substituted with one-two substituents, independently selected from the group, consisting of C1-4alkyl, C1-4alcoxy, C1-4alkylthio, hydroxyl, di(C1-4alkyl), aminocarbonyl, chlorine and fluorine, in such a way that only one di(C1-4alkyl)aminocarbonyl is present; ii) naphthyl; iii) pyridinyl, optionally substituted with one substituent, selected from the group, consisting of C1-4alkyl, C1-4alcoxy, C1-4alkylthio, hydroxy, fluorine, chlorine and cyano; iv) pyrimidin-5-yl; v) furanyl; vi) thienyl; vii) 5-oxo-4,5-dihydro-[1,2,4]oxodiazol-3-yl; and viii) di(C1-2alkyl)aminocarbonyl; Y represents ethyl, vinyl or bond; or Y represents O, when R1 represents optionally substituted phenyl, where substituent represents C1-4alcoxy; R2 represents phenyl, optionally substituted with one-two substituents, independently selected from the group, consisting of C1-4alkyl, C1-4alcoxy, fluorine, chlorine and cyano, trifluoromethoxy and hydroxy; or R2 represents phenyl, substituted with one aminocarbonyl, di(C1-4alkyl)aminocarbonyl, C1-4alcoxycarbonyl or carboxysubstituent; R3 is selected from the group, consisting of i) 3-aminocyclohexyl; ii) 4-aminocyclohexyl; iii) piperidin-3-yl; iv) piperidin-4-yl; v) pyrrolodin-2-yl-methyl, in which pyrrolodin-2-yl is optionally substituted by 3-rd or 4-th position with one or two fluorine-substituents; vi) azetidin-3-yl; vii) 2-(N-methylamino)ethyl; viii) 3-hydroxy-2-aminopropyl; ix) piperidin-3-yl-methyl; x) 1-azabicyclo[2.2.2]octan-3-yl; and xi) 8-azabicyclo[3.2.1]octan-3-yl; or R3 together with Ra and nitrogen atom, which they both are bound to, form piperazinyl, optionally substituted with 4-C1-4alkyl; Ra represents hydrogen, 2-(N-methylamino)ethyl or C1-2alkyl, optionally substituted with azetidin-3-yl.

EFFECT: compounds can be used in treatment of pain in the range from medium to strong, caused by diseases or conditions, such as osteoarthritis, migraine, burn, fibromyalgia, cystitis, rhenite, neuropathic pain, idiopathic neuralgia, toothache, etc.

21 cl, 4 tbl, 26 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to pharmaceutics. A medication represents derivatives of glutarimides of the general formula (I) or their pharmaceutically acceptable salts. The invention also relates to pharmaceutical compositions and a method of treatment.

EFFECT: ensured by the application of non-toxic derivatives of the said glutarimides for the treatment of eosinophilic diseases, mainly of an allergic origin.

16 cl, 12 tbl, 7 ex

FIELD: medicine.

SUBSTANCE: invention relates to a method of treatment or relieving the severity of cystic fibrosis in a patient, where the patient has the cystic fibrosis transmembrane receptor (CFTR) with R117H mutation, including a stage of introduction to the said patient of an effective quantity of N-(5-hydroxy-2,4-ditert-butyl-phenyl)-N-methyl-4-oxo-1H-quinoline-3-carboxamide.

EFFECT: elaborated is the method of treating cystic fibrosis, based on the application of N-(5-hydroxy-2,4-ditert-butyl-phenyl)-N-methyl-4-oxo-1H-quinoline-3-carboxamide.

3 cl, 4 tbl, 30 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely represents a method for the therapy of respiratory symptom. The method involves administering a liquid composition containing a gel former and/or a mucoactive polymer, a non-menthol cooling substance; and contacting the oral mucosa with the liquid composition. The invention also describes liquid compositions applicable in the method for the therapy of a respiratory disease.

EFFECT: implementing the method provides improving the cooling properties of the cooling agent N-(4-cyanomethylphenyl)-n-menthane carboxamide in the liquid composition by combining the non-menthol cooling substance with the gel former.

14 cl, 2 tbl, 5 dwg

FIELD: chemistry.

SUBSTANCE: disclosed are copolymers based on N-vinylpyrrolidone, having as terminal fragments a cyanovaleric acid residue and a hydrogen atom, having general formula (I) where the monomer link is a 4-vinylpyridine (4-VP) fragment, if X is or a 2-methyl-5-vinylpyridine (2-M-5-VP) fragment, if X is , wherein the content of monomer links which are 4-VP or 2-M-5-VP fragments is 20-90 mol%; the viscosity-average molecular weight Mµ of the copolymers is equal to 10-350 kDa, and the acid number is equal to (0.1-5.6)·10-3 mg KOH/g. Also disclosed is use of said copolymers as an anti-pneumoconiosis agent.

EFFECT: high efficiency of using the compound.

2 cl, 2 tbl, 11 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to pharmaceutical industry, namely to pharmaceutical composition in form of dry, free-flowing, compressible powder, which contains (a) rapamycin and mixture of (b) hydrophobic polyoxyethylene and polyoxypropylene block-copolymer and (c) hydrophilic polyoxyethylene and polyoxypropylene block-copolymer with weight proportions b:c equal from 1:3 to 1:9.

EFFECT: invention provides increase of powder compressibility and increase of rapamycin stability and bioavailability.

15 cl, 8 ex, 5 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutics and represents a suspension for treating psoriasis, containing calcipotriol monohydrate in the form of nanocrystals having the particle size distribution within the range of 200-600 nm; the particles are dispersed in an aqueous phase containing a non-ionic polymer surfactant specified in a group consisting of a surfactant in the form of poloxamers or polysorbates, in the amount of 0.01-5 wt % calculated using a suspension for preventing development of aggregation and/or calcipotriol monohydrate nanocrystal growth; the calcipotriol monohydrate nanocrystals are produced in the suspension by processing the suspension by a method involving the stages of reduction in crystalline calcipotriol monohydrate particle size in an aqueous phase to form microparticles having the particle size distribution within the approximate range of 5-20 mcm and the average approximate particle size of 10 mcm; the suspension is exposed to three high-pressure homogenisation cycles for 7-15 minutes each; in the first, second and third cycles, the pressure makes 300-800 bars, 800-1,200 bars and 1,200-1,700 bars respectively.

EFFECT: invention provides creating the local composition containing calcipotriol as an active agent, however being free from propylene glycol as a solvent.

34 cl, 8 ex, 5 tbl, 9 dwg

FIELD: chemistry.

SUBSTANCE: method includes the following steps: obtaining pores under the effect of electrolysis in a plate with thickness of 700-730 mcm and area of up to 32 cm2 of monocrystalline silicon, which is the anode, with p-type conductivity, doped with boron with concentration of about 10-19 cm-3, with resistivity of 3-7·10-3 ohm·cm, the surfaces of which are directed in parallel to the crystallographic planes in a glass-carbon cup, which is the cathode; wherein the electrolyte used is a solution consisting of different volume parts of hydrofluoric acid and ethyl alcohol; subsequent separation of the obtained porous layers from the remaining part of the bulk crystal by increasing the applied voltage by 5-90%, which changes the mechanism of the electrochemical process and switches from pore-formation to continuous polishing etching; washing the separated layers in ethanol and drying in air, followed by stepwise thermal annealing and grinding to fine powder state. Annealing is carried out first for 2 hours at 250°C and then for 20 minutes at 650°C in a hydrogen atmosphere.

EFFECT: obtaining silicon biocompatible nanocarriers with porosity of 40-80% and size of end-to-end pores of 5-20 nm.

3 cl, 7 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: pro-apoptotic solid dispersion contains a compound, e.g. ABT-263 taken in a substantially non-crystalline form to inhibit Bcl-2 proteins and dispersed in a solid binding substance containing (a) a pharmaceutically acceptable water-soluble polymer carrier and (b) a pharmaceutically acceptable surfactant. A method for preparing this solid dispersion involving dissolving the compound, polymer carrier and surfactant in an acceptable dissolution medium and removing the dissolution medium to form the solid binding substance containing the polymer carrier and surfactant and possessing a compound dispersed therein in the substantially non-crystalline form.

EFFECT: solid dispersion is orally applicable in the individual in need thereof for treating a disease characterised by the overexpression of one or more anti-apoptotic Bcl-2 proteins, eg a malignant new growth.

22 cl, 6 ex, 2 tbl, 3 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to medicine, in particular to a pharmaceutical composition in the form of the extrudate, containing at least one pharmaceutically active substance in the form of needles, characterised by the fact that the ratio of the particle size of the needle-like active substance to the diameter of strands constitutes at least 1:25.

EFFECT: invention makes it possible to obtain the more homogeneous extrudate.

11 cl, 13 ex, 10 dwg

FIELD: medicine.

SUBSTANCE: this invention aims at pharmaceutical compositions and methods for making these compositions containing a number of controlled-release particles. At least one assembly of said particles comprises a nucleus containing weakly basic drug substance, an alkaline buffer layer above the nucleus, and a controlled-release coating. The weakly basic drug substance contains at least one nitrogen-containing fragment with pKa from approximately 5 to approximately 14, with a solubility from at least 200 mg/ml at room temperature in an aqueous solution at pH approximately pH 1.2-6.8 and solubility of no more than approximately 10 mg/ml at pH 8 and more. The controlled-release coating contains a water-insoluble polymer. The pharmaceutical composition also contains rapidly degrading microgranules. This invention also aims at pharmaceutical dosage forms containing orally degrading tablets, classical tablets and capsules, as well as methods for making them.

EFFECT: invention provides the sustained release of the weakly basic drug substance in the small intestine.

65 cl, 1 dwg, 1 tbl, 7 ex

FIELD: medicine.

SUBSTANCE: therapeutic agent contains anastrozole, poly(lactic-co-glycolic acid), polyvinyl alcohol and D-mannitol. The therapeutic agent represents sub-micron particles and can be presented in the form of capsules, granules, powder, as well as a suspension for injections.

EFFECT: using the developed therapeutic agent enables achieving the therapeutic effect with lower therapeutic doses and making the antitumour therapy more comfortable for the patient.

2 cl, 1 tbl, 2 dwg, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to medicine and consists in a pharmaceutical substance, representing an instantly soluble in water powder of a crystalline chemical compound of dextrose with sodium chloride - (C6H12O6)2·NaCl·H2O, which has a specific rotation of a polarised light plane initial at 113°, equilibrium at 52.9°, constant of the mutarotation rate of 6.7·10-3 and moisture content of not more than 4.3%. The invention also relates to a method of obtaining the pharmaceutical substance.

EFFECT: pharmaceutical substance has stable quality, is easily packaged, it is possible to prepare a solution for injections from it in a fast and easy way, its storage and transportation are considerably more simple.

2 cl, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to a method for producing a tablet by (i) compressing a powder mixture in a mould plate of one device for producing a tabletted form with the powder mixture comprising a pharmaceutically active substance and a fusible binding agent, and (ii) exposing the above tabletted form to radio-frequency radiation generated by the above device over a period of time adequate to soften or melt the binding agent inside the above tabletted form to produce a tablet. Oral absorption of the produced tablet placed on the tongue takes less than approximately 30 s.

EFFECT: more effective method for producing the tablet by (i) compression.

18 cl, 14 dwg, 7 tbl, 9 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to medicine and concerns a stable composition of nanostructured Sildenafil inhibiting cyclic guanosine monophosphate (cGMP) specific phosphodiesterase type 5 (PDEV) containing a nanostructured Sildenafil base or its pharmaceutically acceptable salts having an average particle size of less than approximately 500nm, a stabilising agent, wherein the composition is prepared in a microfluidics-based continuous-flow tank reactor, and the composition possesses a semi-amorphous structure. The group of inventions also concerns a method for preparing the composition of nanostructured Sildenafil; using the above composition for preparing the pharmaceutical composition for treating male or female sexual dysfunction and pulmonary arterial hypertension.

EFFECT: group of inventions provides the improved solubility of the composition.

8 cl, 11 ex, 14 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a microbiologically stable pharmaceutical composition containing an active agent specified in prostaglandins, and a carrier. The carrier contains an aqueous electrochemically activated saline containing 1 to 500 mg/l of free chlorine and having an oxidation-reduction potential from +150 to +1350 mV. The active agent is present in a phase separated from the electrochemically activated saline; the electrochemically activated saline is a hypochlorite solution.

EFFECT: invention refers to using the pharmaceutical composition for treating and/or preventing dry eye syndrome and for cleansing contact lenses.

14 cl, 5 tbl, 2 ex