Peroral dabigatran etexilate pharmaceutical compositions

FIELD: pharmacology.

SUBSTANCE: composition comprises particulate mix, where a) the first particulate type comprises the dabigatran etexilate in the form of the free base or in the form of its pharmaceutically acceptable salts, polymorphs, solvates or hydrates and which does not have acids; and b) the second particulate type comprises at a minimum one pharmaceutically acceptable organic acid, where at a minimum one particulate type is encased in an outer protection sheathe. The composition is destined for the reduction of the stroke and the systemic embolism risk in patients with the nonvalvular atrial fibrillation and/or for the preventive measures for the venous thromboembolic complication in adult patients that had a surgical operation on elective total hip replacement or the surgical operation on total knee arthroplasty.

EFFECT: implementation of the invention allows to get the composition, which differs by fast dissolution and significant bioactivation.

18 cl, 3 ex, 11 tbl

 



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to using dermatan sulphate recovered from sulodexide for treating diseases involving metalloproteinase MMP-9: varicose veins and vascular malformations accompanied by a risk of thrombosis.

EFFECT: reducing and/or inhibiting individual's blood serum and saphena segments MMP-9 has been shown.

4 cl, 3 dwg, 13 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the field of biotechnology, namely, to obtaining inhibitors of adhesion and/or aggregation of platelets, and can be used in medicine. A polypeptide, used as a component of a pharmaceutical composition and in sets for screening of the inhibitors of platelet adhesion or aggregation, is obtained in a recombinant way with the application of a matrix of the salivary gland cDNA of Anopheles stephensi.

EFFECT: invention makes it possible to obtain the polypeptide, possessing inhibiting activity with respect to platelet aggregation and/or inhibiting activity with respect to platelet adhesion.

10 cl, 4 dwg, 5 ex

FIELD: medicine.

SUBSTANCE: invention represents a mixture of two structural isomers: 2,6-di(1,7,7-trimethylbicyclo[2.2.1]hept-2-yl)-4-methylphenol and its diastereomers, and 2-(1,7,7-trimethylbicyclo[2.2.1]hept-2-yl)-6-(2,2,1-trimethylbicyclo[2.2.1]hept-5-yl)-4-methylphenol, and their diastereomers with the ratio of the first and second structural isomer isomers from 60:40 wt % to 95:5 wt %.

EFFECT: extension of the arsenal of means, possessing simultaneously haemorheological, anti-aggregate, anti-thrombogenic, retinoprotecting, endothelium-protecting, neuroprotecting, anti-arrhythmia and anti-ischemic activity, enhancing the cerebral blood flow.

4 dwg, 20 tbl, 6 ex

FIELD: medicine.

SUBSTANCE: before operation analysis of patient's haemostasis by means of thrombodynamics is carried out, and 12 hours before beginning operation anticoagulant prophylaxis with enoxaparin in dose 40 mg s/c 1 time per day performed. Analysis of thrombodynamics and coagulogram are repeated one day after operation, In case of detection of hypercoagulation (increase of one or some indices of thrombodynamics - initial speed of clot growth, stationary speed of clot growth, clot density, appearance of spontaneous clots) dose of enoxaparin is increased to 60 mg one time per day, and in case of detection of hypocoagulation (reduction of one or several indices of thrombodynamics - initial speed of clot growth, stationary speed of clot growth, clot density, delay of clot growth) dose of anticoagulant is reduced twice - 20 mg of enoxaparin per day.

EFFECT: method makes it possible to prevent development of post-operative venous thromboembolic complications in patients with colorectal cancer; said regimen of enoxaparin introduction provides prevention of both thromboembolic and hemorrhagic complications in said group of patients.

2 ex

FIELD: chemistry.

SUBSTANCE: thrombocyte aggregation-inhibiting heteromeric peptides based on imidazo[4,5-e]benzo[1,2-c;3,4-c']difuroxane are disclosed: , where R=Phe-Ile-Ala-Asp-Thr; Arg-Tyr-Gly-Asp-Arg; Lys-Ile-Ala-Asp-Asp; His-Ile-Gly-Asp-Asp.

EFFECT: improved properties.

1 dwg, 2 tbl, 4 ex

FIELD: chemistry.

SUBSTANCE: invention relates to N-carb(arginyl)oxymethylimidazo[4,5-e]benzo[1,2-c; 3,4-c']difuroxane of formula .

EFFECT: improved properties of the compound.

1 dwg, 1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the field of pharmaceutics and represents a medication, possessing venomotor and anticoagulant action, which includes a dry extract of vine leaves, a base, preservatives, solvents, and is characterised by the fact that it additionally contains heparin in the form of a pharmaceutically acceptable salt, as the base it contains a hydrophilic gel-generating agent, as the solvents it contains purified water, propyleneglycol, ethyl alcohol rectified 95%, as the preservatives it contains nipagin, nipasol, with the following component ratio, wt %: dry extract of vine leaves with the content of the sum of flavonoides counter per rutin no less than 8% - 0.1-30.0; heparin in the form of a pharmaceutically acceptable salt - 100-1000 Units, hydrophilic gel-generating agent - 0.2-20.0; nipagin - 0.01-0.2; nipasol - 0.01-0.2, propyleneglycol - 3.0-70.0; ethyl alcohol rectified 95% - 3.0-70.0; purified water - the remaining part.

EFFECT: invention provides the creation of the medication in the form of a gel with good absorption, fast soaking, storage stability and acceptable organoleptic properties.

4 cl, 8 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to a citrate of a compound described by formula (II) below, and a pharmaceutical composition containing said citrate.

EFFECT: experimental results of the present inventions prove that said citrate can inhibit activity of phosphodiesterase type 5 and can be used for treating erectile dysfunction, for inhibiting thrombocyte aggregation and treating thrombosis, for reducing pulmonary hypertension and treating cardiovascular diseases, asthma and diabetic gastroparesis.

2 cl

FIELD: medicine.

SUBSTANCE: invention concerns preparing systemic and topical solid and soft dosage forms for external application in the form of a 1.5% hydrophilic gel and rectal capsules containing a 7.5% hydrophilic gel 1.9 g (in terms of the amount of the active substance of 0.14 g/capsule), for preventing and treating chronic venous insufficiency possessing anticoagulant, antithrombotic, anti-inflammatory, antiexudative and antitranssudative, capillary protective activities and improving haemorheology. An active pharmacologically active substance is presented by a substance of a potassium salt of sulphated arabinogalactan; a hydrophilic base is Aerosil, glycerol and pure water; the ingredients of the agent are taken in certain proportions, wt %.

EFFECT: invention provides the effective prevention and treatment of chronic venous insufficiency, has a broad spectrum of therapeutic action, improves haemorheology, tones the vessels and can be used in particular for treating varicose veins, thrombosis and posttraumatic oedema.

5 cl, 7 ex, 8 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, particularly to pharmaceutical industry, and describes a dosage form of Clopidogrel presented in the form of a solid gelatine capsule. The dosage form contains Clopidogrel hydrogen sulphate, lactose anhydride, microcrystalline cellulose, sodium croscarmellose, colloidal silicon dioxide and magnesium stearate.

EFFECT: according to the invention, the dosage form of Clopidogrel contains a high amount of the active ingredient; it is prepared without the use of a wet granulation technique, and provides the more accurate dosage of the ingredients and the stability of the substances used.

9 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to nanotechnology, particularly a method of producing aspirin nanocapsules in a carrageenan envelope. The disclosed method includes preparing an aspirin suspension in benzene; dispersing the obtained mixture into a carrageenan suspension in butanol in the presence of an E472c preparation while mixing at 1000 rps; adding tetrachloromethane; filtering the obtained nanocapsule suspension and drying at room temperature.

EFFECT: method provides a simpler and faster process of producing nanocapsules and increases mass output.

1 dwg, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to field of bioencapsulation and represents method of obtaining microcapsules by method of precipitation with non-solvent, which consists in the fact that water-soluble medication of cephalosporin group, applied as core of microcapsules, and E472c as surface-active substance, are added to water solution of human leukocyte interferon in α- or β- form, applied as envelope of microcapsules, mixture is mixed, after dissolution of components carbinol is added as first precipitator, with the following addition of acetone as second precipitator, with ratio of carbinol to acetone constituting 1:5, obtained suspension of microcapsules is filtered, washed and dried at 25°C.

EFFECT: invention ensures simplification and acceleration of the process of obtaining microcapsules and reduction of loss (increase of output by weight).

4 ex

FIELD: chemistry.

SUBSTANCE: invention relates to microencapsulation, in particular, to microencapsulation of antioxidants. Carrageenan was used for the capsule shells, an antioxidant was selected from the group of: vitamins A, C, E, Q10, eleuterococcus, green tea extract, ginseng extract; wherein an antioxidant product portion was dissolved in dimethylsulfoxide, and the mixture was dispersed in a solution of carrageenan in ethanol in the presence of the preparation E472c under stirring at the rate of 1300 rev/s, the antioxidant/carrageenan weight ratio was 1:3, after which a mixture of benzene and water taken in volume ratio of 2:1 was added to the above mix, the resulted suspension was filtered and dried at a room temperature.

EFFECT: simplified and fast process of antioxidant product microencapsulation in carrageenan.

1 ex

FIELD: nanotechnology.

SUBSTANCE: suspension of aspirin in benzene is produced. The resulting mixture is dispersed into suspension of sodium alginate in butanol in the presence of the preparation E472s when stirring at 1000 rpm/sec. Then chloroform is poured, the resulting suspension of nanocapsules is filtered and dried at room temperature.

EFFECT: simplification and acceleration of the process of production of the nanocapsules, and increase in the yield by weight.

1 dwg, 4 ex

FIELD: chemistry.

SUBSTANCE: invention relates to microencapsulation, in particular, to microencapsulation of flavours. Carrageenan was used for the capsules, wherein an aromatic product portion was dissolved in dimethylsulfoxide, and the mixture was dispersed in a solution of carrageenan in ethanol in the presence of the preparation E472c, under stirring at the rate of 1300 rev/s, the aromatic product/carrageenan weight ratio was 1:3 respectively, after which mixture of butanol and distilled water taken in volume ratio 3:1 respectively was added, the resulted microcapsule suspension was filtered and dried, the process of production of "cherry" or "tomato" flavour microcapsules was carried out at 25°C.

EFFECT: simplified and fast process of aromatic product microencapsulation, with the reduced amount of waste.

3 ex, 7 dwg

FIELD: food industry.

SUBSTANCE: organoleptical properties improvement is achieved by the fish oil microcapsules production method characterised by obtainment of an oil-in-water emulsion by way of mixing fish oil and an encapsulation ingredient in water; the components are taken at a ratio 30-35 and 25-30 wt %, water - balance; the method additionally involves homogenisation and dispersion of the obtained emulsion in an ultrasonic field and microemulsion subsequent spray drying; ultrasonic dispersion is carried out with insonification frequency equal to 28 kHz and intensity equal to 40 W/cm2; spray drying is carried out with a parallel hot air flow with the temperature at the inlet and outlet equal to 160-180°C respectively.

EFFECT: simplification and enhancement of microencapsulation processes efficiency during production of deodorised and encapsulated fat-soluble food products, in particular, improvement of organoleptic properties of fish oils used for food products enrichment.

4 cl, 6 ex, 1 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to the encapsulation of active ingredients and to processing textile materials. Claimed are: a method of processing textile materials, containing microcapsules of active ingredients, fibres and/or textile materials, obtained from the said method, and their cosmetic or pharmaceutical application and/or their application as a repellent.

EFFECT: claimed invention makes it possible to increase the active ingredient stability for an acceptable number of washings.

16 cl, 6 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to microencapsulation of water-soluble preparations, particularly to encapsulation of common jujube possessing the therapeutic properties. The method for common jujube encapsulation involves dispersing common jujube powder suspension in isopropanol in the presence of the preparation E472 and precipitating with carbon tetrachloride as a non-solvent. There are produced microcapsules containing common jujube as a core in xanthane gum as a shell in core:shell ratio 1:3, 1:1 and 3:1 with 100% yield.

EFFECT: invention provides simplifying and accelerating the microencapsulation process and higher weight yield.

3 ex

FIELD: food industry.

SUBSTANCE: invention relates to food industry. The method for production of dry girasol extract in pectin envisages usage of a microcapsule shell, represented by low-etherified and high-etherified apple and citrus pectins, and a nucleus, represented by dry girasol extract. The microcapsules are produced by way of the pectin mixture stirring in benzol, with the surfactant represented by preparation E472c, in a magnetic stirrer. Then dry girasol extract is added into the mixture which is deposited with acetonitrile. Then the produced microcapsule suspension is filtered, washed with acetonitrile and dried.

EFFECT: invention allows to simplify and accelerate the microcapsules production process and increase weight yield.

7 ex

FIELD: chemistry.

SUBSTANCE: invention relates to field of encapsulation, in particular to method of obtaining microcapsules of vitamins A, C, E or Q10 in coating from highly etherified or low etherified apple or citrus pectin. In accordance with method by invention preparation E472c is added to suspension of highly etherified or low etherified apple or citrus pectin in ethanol and mixed. After that, suspension of vitamin in dimethylsulphoxide is added to suspension of pectin in ethanol, with further addition of benzene and distilled water. Obtained suspension of microcapsules is filtered and dried. Process of obtaining microcapsules is realised at 25°C for 15 min.

EFFECT: invention provides simplification and acceleration of process of obtaining microcapsules, reduction of loss in the process of their obtaining (increase of output by weight).

16 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

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