Method of producing dalfampridin tablets with prolonged action

FIELD: pharmaceutics.

SUBSTANCE: invention relates to chemical-pharmaceutical industry and medicine. Method of producing dalfampridin pellets is disclosed, characterized by preparing intra-granulated mixture by screening dalfampridin together with hydroxypropyl methyl cellulose with viscosity of 80–120 MPA˙s, mixing with microcrystalline cellulose with particle size of 50–90 mcm and aerosil, compaction, mixing with magnesium stearate, it is followed by granulation of mixture by rolling, extra-granulated mixture is added to obtained granules consisting of microcrystalline cellulose with particle size of 50–90 mcm and aerosil, mixed to homogeneous state, magnesium stearate is added, tablets are pressed and coated with their shell by spraying water solution of white Opadraja till tablet weight increases by 1.0–3.0 %.

EFFECT: obtained solid shape has improved pharmacological and process characteristics.

6 cl, 1 dwg, 3 tbl, 3 ex

 



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine and describes a pharmaceutical composition of dioctahedral smectite presented in the form of a dispersible tablet, as well as a method for producing it. The dispersible tablet is formed by pressing the granules containing dioctahedral smectite in an amount of 800 to 1,200 mg, as well as excipients and target additives in an amount of no more than 50% from a tablet weight. The produced tablet is water-dispersible for 3 minutes to form a dispersion consisting of particles of less than 710 mcm in size, as well as possesses high stability and physical integrity, good mechanical properties in a combination with fast dispersion ability in aqueous solutions.

EFFECT: specified tablet composition enables providing good stability of the technological process of the dispersible tablet.

2 cl, 2 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to thermoformed pharmaceutical dosage form having a minimum tensile strength of 300 N; the above dosage form contains an opioid, a free physiologically acceptable carboxylic acid in an amount from 0.1 to 5.0 wt %, at total weight of the pharmaceutical dosage form and polyalkylene oxide having a minimum average molecular weight Mm of 500,000 g/mole. Carboxylic acid is specified in a group consisting of maleic acid, fumaric acid, glutaric acid, malonic acid and citric acid. The opioid is specified in a group consisting of oxymorphone, oxycodone, hydromorphone and their physiologically acceptable salts. The pharmaceutical dosage form can be packaged.

EFFECT: pharmaceutical dosage for according to the invention is characterised by the improved storage stability.

14 cl, 11 tbl, 9 ex

Hypotensive means // 2554815

FIELD: medicine.

SUBSTANCE: invention represents a hypotensive means, which contains felodipinum as an active component, as well as target additional components: mesoporous silicon dioxide, lactose, hypromeloza. Realisation of the invention ensures the high technological efficiency of the claimed medical means production with the provision of a prolonged release of an active substance with the application of available components. Felodipinum is included into spherical particles with a highly developed mesoporous structure of silicon oxide.

EFFECT: increase of stability in storage and protection from unfavorable environmental factors.

4 cl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: pharmaceutical composition in the form of a tablet with an erodible matrix, which contains one or more fumaric acid ethers, as well as a rate-controlling agent, representing hydroxypropylcellulose and a binding agent, representing lactose, with the decomposition of the said degradable matrix providing the controlled release of the said fumaric acid ether (ethers).

EFFECT: provision of the controlled release of fumaric acid ether (ethers).

19 cl, 43 ex, 2 tbl, 2 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, and represents a sustained release solid therapeutic agent containing a combination of praziquantel with emodepside, polyvinylpyrrolidone and/or a polyvinylpyrrolidone derivative in an amount of 10 to 50 wt %, polyvinylpyrrolidone and/or the polyvinylpyrrolidone derivative is a mixture of one short-chain polyvinylpyrrolidone and one polyvinylpyrrolidone or the polyvinylpyrrolidone derivative with longer chains, and at least one excipient in an amount of 5 to 80 wt %.

EFFECT: sustained release of active substances and no lump formation in the gastrointestinal tract if two or more tablets taken.

4 cl, 7 ex, 4 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to oral pharmaceutical composition in the form of a granulate produced without spheronisation. The composition contains 92-98 wt % of mesalazine or its pharmaceutically acceptable salt, 2-8 wt % of polyvinylpyrrolidone and an ethylcellulose coating, wherein the above coating weight relates to the above mesalazine weight as 0.3-1.5% and the ethylcellulose coating weight makes 0.11-0.15 mg/cm2. The granulate is packed in a sachet, a capsule or a blister. What is also described is a method for preparing a pharmaceutical composition.

EFFECT: ethylcellulose-coated mesalazine granulate combines a high drug load and a desired mesalazine release profile, namely, 5-25% of released mesalazine 15 min later, 30-70% of released mesalazine 90 min later and 75-100% of released mesalazine 240 min later.

10 cl, 1 ex

FIELD: medicine.

SUBSTANCE: establishing the diagnosis of myocardial infarction is immediately followed by prescribing trimetazidine MB, a modified-release cardiocytoprotector trimetazidine in a dose of 35 mg 2 times a day accompanied by enhancing motion activity gradually: degree Ia activity - turning to the sides; degree Ib activity - sitting for 5-10 minutes 2-3 times a day; degree IIa activity - sitting for 20 minutes, sitting meals, changing on a chair; degree IIb activity - walking along the chamber; degree IIIa activity - coming out into the corridor, unlimited sitting; degree IIIb activity - walking along the corridor, going up the stairs one level higher; degree IVa activity - going for a walk; degree IVb activity - taking 1.0-1.5km walk. The next degree is started in accordance with the patient's chronotropic response to physical exercises providing a heart rate gain to age-specific submaximal values.

EFFECT: method enables providing the more effective rehabilitation of the patients by the combined use of physical exercises and drug treatment accompanied by controlling an age-specific chronotropic criterion.

3 ex, 4 tbl, 1 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine and represents a controlled-release preparative form of diacerein administered once a day for treating or autoimmune diseases or their complications. The preparative form contains a core, an active layer, a sustained-release film layer and a delayed-release film layer, wherein the active layer is followed by the sustained-release film, and the delayed-release film layer thereafter. The sustained-release film layer contains ethyl cellulose polymer, povidone, triethylacetate and talc; the delayed-release film layer contains Eudragit polymer, triethylacetate and talc.

EFFECT: reducing the negative side action of diacerein.

18 cl, 23 ex, 33 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutics and represents a controlled-release aceclofenac preparation for oral administration once a day, exhibiting the fast analgesic and anti-inflammatory action, containing a fast-release layer containing aceclofenac, a solubiliser, a water-soluble additive, a disintegrating agent, a vehicle and a fast-acting additive, as well as a sustained-release layer containing aceclofenac, a solubiliser and a release control base consisting of mixture of hydroxypropyl methyl cellulose (HPMC) with a viscosity of 80,000 sP to 120,000 sP and carbomer taken in mass ratio 7:1 to 9:1.

EFFECT: invention provides a sequential and uniform dissolution rate and a controlled release of the active agent.

7 cl, 12 tbl, 11 dwg, 10 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, specifically to pharmaceutical compositions possessing prolonged antiarrhythmic actions and applicable to correct the cardiac arrhythmia, including that of the ischemic origin. What is presented is a pharmaceutical composition with the prolonged antiarrhythmic acitivity containing bis[2-(diethylamino)]-N-(2,6-dimethylphenyl)acetamide L-glutaminate, L-glutamic acid, 2-aminoethane sulpho-acid and excipients.

EFFECT: prolonged antiarrhythmic action and stability of the dosage form (tablets, capsules for oral application or solution for injections).

3 cl, 4 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to organic chemistry, namely to benzimidazole-4-carboxamide derivatives of formula , wherein X means an alkenyl group C2-C7 substituted by two methyls, nitro-radical mono-substituted thienyl, unsubstituted quinolinyl, unsubstituted indolyl, unsubstituted pyridazinyl, unsubstituted piperazinyl, C1-C6-alkyl disubstituted piperazinyl, unsubstituted piperidinyl, unsubstituted pyrazinyl, unsubstituted imidazolyl, unsubstituted pyrimidinyl, phenyl monosubstituted pyrimidinyl, pyrimidinyl disubstituted by an amine radical and a radical specified in a group containing -F, -Cl, -Br or -I, hydroxyl trisubstituted phenyl, methoxy-radical trisubstituted phenyl, hydroxyl and methoxy-radical disubstituted phenyl, pyrazolyl disubstituted by a radical specified in a group containing a C1-C6-alkyl, and by a radical specified in a group containing -F, -C1, -Br or -I; Y means aminophenyl monosubstituted by a radical of -F, -O, -Br or -I phenyl, hydroxyethyl disubstituted by hydroxymethyl or C1-C6-alkyl and phenyl monosubstituted by a nitro group, an amino group or a halogen atom; Y also means unsubstituted piperazinyl, unsubstituted pyridyl, unsubstituted pyrazinyl, C1-C6-alkyl monosubstituted thiazol, unsubstituted pyrimidinyl, unsubstituted purinyl. The invention also refers to a pharmaceutical composition based on the compound of formula (I), using the compound of formula (I), a method for producing the compound of formula (I).

EFFECT: there are prepared new benzimidazol-4-carboxamide derivatives possessing antiviral activity.

5 cl, 6 dwg, 4 tbl, 688 ex

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry and specifically to novel heterocyclic compounds of general formula (I) or enantiomers, diastereomers or pharmaceutically acceptable salts thereof, where Y is: phenyl or a heteroaryl selected from thiazolyl, pyridyl, pyrimidinyl, 1,3,5-triazinyl, benzoxazolyl, benzisoxazolyl, benzothiazolyl and 1,3,4-thiadiazolyl; wherein the phenyl or heteroaryl is optionally substituted with one substitute selected from fluorine, chlorine, bromine, iodine, C1-4alkyl, trifluoromethyl, C1-4alkoxy, C1-4alkylthio, nitro and cyano; r=1-2; R2 is absent or is an oxo-group; Z is: (a) phenyl substituted with NRaRb; where Ra is: H or C1-4alkyl; where Rb is: C1-4alkyl, cycloalkyl, phenyl, furanylmethyl, or phenyl(C1-2alkyl); and wherein the phenyl or the furanyl are optionally substituted with iodine; alternatively, Ra and Rb are taken together with the nitrogen atom to which they are bonded to form a 5-8 member heterocyclyl, which is optionally condensed to a benzene ring; (b) biphenyl-3-yl or biphenyl-4-yl; where the interior phenyl ring, attached to the carbonyl in formula (I) is optionally substituted with a fluorine atom; and where the terminal phenyl ring is optionally substituted with a substitute selected from trifluoromethyl, C1-4alkoxy, chlorine, dichloro, fluorine, and iodine; (c) phenyl substituted with a substitute selected from C5-8cycloalkyl, -NHC(=O)cyclohexyl, phenyloxy, phenylcarbonyl, phenyl(C1-3)alkyl, phenyl(C1-3)alkoxy, pyrrolyl, pyrazolyl, imidazolyl, isoindol-2-yl-l,3-dione, 2,3-dihydro-isoindol-2-yl; l-(tert- butoxycarbonyl)piperidin-4-yloxy, and 1-(tert-butoxycarbonyl)piperidin-4-yl; (d) phenyl substituted with 1-2 substitutes independently selected from: C1-6alkyl, C1-4alkoxy, iodine, chlorine and nitro; (e) phenyl(C1-2)alkyl; where the phenyl is optionally substituted with 1 or 2 substitutes independently selected from iodine, fluorine, C1-6alkyl, phenyl and NRcRd; where Rc: H or C1-4alkyl; where Rd is: C1-4alkyl or C1-6cycloalkyl(C1-4)alkyl; and where the C1-2alkyl of phenyl(C1-2)alkyl is optionally substituted with phenyl; (f) phenyl(C2-4)alkenyl; where the phenyl is optionally substituted with a substitute selected from C1-4alkyl, C1-4alkoxy, trifluoromethyl, trifluoromethylthio and phenyl; (g) naphthyl; where the naphthyl is optionally substituted with one C1-4alkoxy substitute; (h) fluorenyl or xanthenyl; where the fluorenyl or xanthenyl is optionally substituted with an oxo group; (i) C5-8cycloalkyl; where the C5-8cycloalkyl is optionally substituted with one C1-6alkyl substitute; (j) benzene ring-condensed C5-8cycloalkyl or benzene ring-condensed C5-8cycloalkyl(C1-4)alkyl; where said C5-8cycloalkyl fragment is optionally substituted with 1-4 methyl groups; (k) bicyclo[2.2.2]octyl-1-yl; where the bicyclo[2.2.2]octyl-l-yl is optionally substituted with C1-6alkyl; (1) a heteroaryl or benzene ring-condensed heteroaryl selected from benzooxazolyl, quinolinyl, benzimidazolyl, pyridinyl, indolyl, thienyl, furanyl, pyrazolyl, oxazolyl, benzothienyl and benzofuranyl; where the heteroaryl or benzene ring-condensed heteroaryl is optionally substituted with 1 or 2 substitutes independently selected from C1-4alkyl, trifluoromethyl, C5-8cycloalkyl, phenyl, phenyl(C1-2)alkoxy, phenyl(C2-4)alkynyl and dichlorophenoxy; and where the phenyl substitute in the heteroaryl is further optionally substituted with C1-4alkyl, C1-4alkoxy or trifluoromethyl; (m) l,5-diphenyl-lH-pyrazol-3-yl; where the pyrazol-3-yl is optionally substituted with a methyl group; and where each of the phenyl groups of the 1,5-diphenyl substitutes is also optionally substituted with substitutes selected from chlorine, dichloro or aminosulphonyl; (n) 1,2,3,4-tetrahydroquinolin-6-yl; where the 1,2,3,4-tetrahydroquinolin-6-yl is optionally substituted with phenyl or trifluoromethyl-substituted phenyl; and (o) benzene ring-condensed heterocyclyl(C2-4)alkenyl; where the benzene ring-condensed heterocyclyl is attached to the C2-4alkenyl via the benzene ring; and where benzene ring-condensed heterocyclyl is further optionally substituted with C5-6cycloalkyl; taking into account constraining conditions indicated in claim 1. The invention also relates to a pharmaceutical composition based on the compound of formula (I), a method of producing said pharmaceutical composition, a method of treating said pathological conditions and use of the compound of formula (I).

EFFECT: obtaining novel heterocyclic compounds having MGL inhibiting activity.

21 cl, 5 tbl, 11 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the pharmaceutical industry and describes a peroral combined medication for the treatment of arterial hypertension in patients with diabetes mellitus. The medication is made in the form of a tablet. The combined tablet contains perindopril erbumine, amlodipine besylate, sorbitol, microcrystalline cellulose, sodium carboxymethyl starch, povidone, magnesium stearate in quantities, given in the invention formula.

EFFECT: combination of perindopril, amlodipine and sorbitol in the composition of one tablet provides enhancement of the therapeutic effect.

6 tbl

FIELD: medicine.

SUBSTANCE: method involves chelation of ferric (III) ions both in vivo, and in vitro with using 2-ethyl-6-methyl-3-hydroxypyridine succinate (Mexidol) to produce a stable stained complex having a high molecular weight and a complex (organic-inorganic) composition not identified among the known compounds.

EFFECT: high effectiveness of the chelation process and low toxicity of Mexidol that makes it promising for biomedical application.

4 dwg, 3 tbl, 3 ex

FIELD: chemistry.

SUBSTANCE: invention represents method of obtaining substations based on oxidated dextran and isonicotinic acid hydrazide, which includes obtaining dextran water solution, dextran oxidation with potassium permanganate in acidic medium at heating, removal of admixtures from solution by filtration, purification of oxidated dextran water solution from manganese ions by passing at rate 100-600 ml/min through cation exchange resin, represented by cationite based on styrene copolymer with static volume capacity 1.9 g-eq/cm3, addition of powder of isonicotinic acid hydrazide and distilled water or water solution of isonicotinic acid hydrazide.

EFFECT: simplification of process of obtaining substance based on oxidated dextran and isonicotinic acid hydrazide for pharmaceutical application due to creation of conditions for minimisation of stages and used reagents with elimination of application of dangerous reagents and simultaneous obtaining target product, free of manganese ions.

2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to chemical-pharmaceutical industry and represents application of substituted nitrocatechols of formula for prevention or treatment of disorders, associated with central and peripheral nervous system, which obtain use from inhibition of catechol-O-methyltransferase (COMT), in accordance with schedule of dosing in the range from one time per three days to one time per week.

EFFECT: obtaining composition for prevention or treatment of disorders, associated with central and peripheral nervous system.

45 cl, 1 dwg, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to compound, represented by the following formula

,

or its pharmaceutically acceptable salt. In claimed formula each symbol has values, determined in formula of invention. Versions of formula [I] compound and particular compounds are also objects of invention. In addition, invention relates to pharmaceutical composition, ITK inhibitor and means for treatment or prevention of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection and other diseases and methods of treating said diseases.

EFFECT: claimed compounds inhibit induced T-cellular kinase (ITK).

32 cl, 86 tbl, 387 ex

FIELD: medicine.

SUBSTANCE: invention relates to medicine, namely to ophthalmology, and can be used for the treatment of a primary open-angle cataract at the background of pseudoexfoliation syndrome in a combination with the cataract. Normalisation of the intra-ocular pressure is carried out by the instillation of b-adrenoblockers and/or carboanhydrase inhibitors. Selective laser trabeculoplasty is performed. Phacoemulsification of the cataract with the implantation of an intraocular lens is performed to the patient the following day after exposure to laser. In the course of performing the phacoemulsification of the cataract washing out pseudoexfoliative particles and pigment granules from the angle of the anterior eye chamber is realised.

EFFECT: method provides an improvement of the outflow of the intraocular fluid, normalisation of the intra-ocular pressure, reduction of the intervention volume and acceleration of the patient rehabilitation due to the elimination of the trabecular net pigmentation, removal of pseudoexfoliative material in a combination with the ablation of cataract masses and increase of the width of the anterior eye chamber angle.

1 ex

Hypotensive means // 2554815

FIELD: medicine.

SUBSTANCE: invention represents a hypotensive means, which contains felodipinum as an active component, as well as target additional components: mesoporous silicon dioxide, lactose, hypromeloza. Realisation of the invention ensures the high technological efficiency of the claimed medical means production with the provision of a prolonged release of an active substance with the application of available components. Felodipinum is included into spherical particles with a highly developed mesoporous structure of silicon oxide.

EFFECT: increase of stability in storage and protection from unfavorable environmental factors.

4 cl, 4 ex

FIELD: medicine.

SUBSTANCE: invention concerns activating P450CYP3A4 isoenzyme in patients with chronic cardiac failure. That is ensured by administering ethylmethylhydroxypyridine malate in a single dose of 50-200 mg.

EFFECT: higher clinical effectiveness of chronic cardiac failure.

9 ex, 11 dwg

FIELD: medicine, endocrinology, pharmacology, pharmacy.

SUBSTANCE: invention relates to a pharmaceutical combined composition used for treatment or prophylaxis of hypertension in patients suffering with diabetes mellitus. The composition comprises AT1-antagonist valsartan or its pharmaceutically acceptable salt and calcium channel blocking agent or its pharmaceutically acceptable salt, and pharmaceutically acceptable carrier. The composition elicits synergistic effect and expanded spectrum effect.

EFFECT: improved and valuable medicinal properties of composition.

10 cl, 3 tbl

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