Rasagiline compositions of prolonged release and use thereof

FIELD: pharmaceutics.

SUBSTANCE: group of inventions refers to pharmaceutics. Oral pharmaceutical composition is described in form of prolonged release for treating neurodegenerative disease or damage of nervous system. Above composition contains R(+)-N-propargyl-1-aminoindan (rasagiline) as active substance. Composition contains pellets with prolonged release and pharmaceutically acceptable carrier. Said pellet includes: I) inert core of pellet; II) layer with active substance, polyvinyl pyrrolidone and talc; III) optionally insulating layer with polyvinyl pyrrolidone; IV) prolonged release coating layer with ethylcellulose and polyethylene glycol. Use of said composition and method of treating neurodegenerative disease or damage of nervous system are also described.

EFFECT: invention provides intensified effect on above diseases.

16 cl, 9 dwg, 17 tbl, 11 ex



Same patents:

FIELD: biotechnology.

SUBSTANCE: biologically active peptide is obtained, which has curative effect against Alzheimer disease, and consisting of the amino acid sequence Ala-Trp-Lys-Val-Leu-Ser-Pro-Gln-Gly-Gly-Gly-Pro-Trp-Asp-Ser-Val-Ala.

EFFECT: invention enables to use the resulting peptide to create a drug effective in the therapy of Alzheimer disease.

1 dwg, 2 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a hexapeptide of formula Thr-Gly-Glu-Asn-His-Arg-NH2, having neuroprotective and nootropic activity. Disclosed novel pharmaceutical composition based on a peptide, which is highly effective in low doses and is used as nasal drops.

EFFECT: high efficiency in preventing and treating neurodegenerative and cerebrovascular diseases.

2 cl, 3 dwg, 6 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to novel water-soluble potassium salt of N-(4-acetoxybenzoyl)glycine of formula

given below, which possesses cerebroprotective activity.

EFFECT: invention can be used in chemical-pharmaceutical industry for obtaining effective cerebroprotective medications.

2 dwg, 3 tbl, 6 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of structural formula


having Aβ42 secretion inhibiting activity. In formula I , hetaryl I is a five- or six-member heteroaryl group containing 1-3 heteroatoms selected from O, S or N, hetaryl II is a five- or six-member heteroaryl group containing 1-3 heteroatoms as defined above for hetaryl I, or is a bicyclic ring system containing 1-4 heteroatoms selected from S, O or N, where at least one ring is aromatic by nature, R1 is C1-7-alkyl, C1-7-alkoxy, C1-7-alkyl substituted with a halogen, or a halogen; R2 is a halogen, C1-7-alkyl, C1-7-alkoxy, hydroxy, C1-7-alkyl substituted with a halogen, C1-7-alkyl substituted with a hydroxy, or benzo[1,3]dioxolyl or is -(CHR)p-phenyl, optionally substituted with a halogen, C1-7-alkyl, C1-7-alkoxy, S(O)2-C1-7-alkyl, cyano, nitro, C1-7-alkoxy substituted with a halogen, dimethylamino, -(CH2)p-NHC(O)O-C1-7-alkyl or C1-7-alkyl, substituted with a halogen. The values of radicals R, R3, R4,p, n, m, o are given in the claim.

EFFECT: invention relates to a method of producing said compounds, a medicinal agent containing said compounds and a method of treating Alzheimer's disease, cerebral amyloid angiopathy, Hereditary cerebral hemorrhage with amyloidosis-Dutch type (HCHWA-D), vascular dementia, dementia pugilistica or Down syndrome, associated with β amyloid activity.

21 cl, 283 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions relates to medicine and deals with the application of at least one peptide, selected from the group, including SEFKHG(C), TLHEFRH(C), ILFRHG(C), TSVFRH(C), SQFRHY(C), LMFRHN(C), SPNQFRH(C), ELFKHHL(C), THTDFRH(C), DEHPFRH(C), QSEFKHW(C), ADHDFRH(C), YEFRHAQ(C) and TEFRHKA(C), for the production of a medication for the prevention and/or treating Alzheimer's disease. The group of inventions relates a vaccine, containing at least one said peptide, intended for the induction of immune response aimed against Aβ.

EFFECT: group of invention provides the favourable effect of vaccination with vaccines with mimotopes in the treatment of Alzheimer's disease.

24 cl, 3 ex, 10 dwg, 5 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to biotechnology and immunology. What is presented is a hybridoma cell line FP12H3-C2 deposited under No. DSM ACC2750 producing the anti-beta-amyloid antibody. Presented are methods for preparing an antibody, including a humanised antibody with using a hybridoma line according to the invention, as well as diagnostic techniques for a beta-amyloid associated disease or condition in a patient or a liability to such disease or condition, a method for determining a degree of the tissue involvement into amyloidogenic plaques, a method for monitoring minimal residual signs of the disease into a patient following treating with the antibody or its active fragment, a method for prediction of sensitivity in the patient treated with the antibody or its active fragment.

EFFECT: present invention can find further application in diagnosing and therapy of beta-amyloid related diseases, such as Alzheimer disease.

9 cl, 4 dwg, 5 tbl, 17 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to a pharmaceutical composition based on a compound of formula (I) or its pharmaceutically acceptable salt or solvate. wherein X is S or O, and provided X is S, R1 is OH or NH2; and provided X is O, R1 is OH, NH2 or NHMe. The invention also refers to a compound of formula (I) and a based kit.

EFFECT: there are prepared new imidazolidine derivatives effective in treating prostate cancer.

28 cl, 14 tbl, 14 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to pharmaceutical composition for treating insomnia. Said composition includes root of Polygonum multiflorum and/or its extracts, seeds of Ziziphus spinosa and/or its extracts, mulberry fruit and/or its extracts, Ganoderma and/or its extracts, lily bulb and/or its extracts, Anemarrhena rhizome and/or its extracts, root of Salvia miltiorrhiza and/or its extracts, chrysanthemum flower and/or its extracts, Poria and/or its extracts and Albizia flower and/or its extracts. Invention also relates to application of said composition.

EFFECT: claimed invention provides sedative and soporific effect, contributes to memory stimulation.

17 cl, 6 tbl, 14 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the field of organic chemistry, namely to novel derivatives of pyrazole pyridine of formula , as well as to its tautomers, geometrical isomers, enantiomers, diastereomers, racemates and pharmaceutically acceptable salts, where G1 represents H; G2 represents -CHR1R2; R1 and R2 independently on each other are selected from H; C1C6-alkoxy-C1C6-alkyl; C1-C6-alkyl; optionally substituted phenyl; optionally substituted phenyl-C1-C6-alkyl; optionally substituted morpholine-C1-C6-alkyl; or -CHR1R2 together form a ring, selected from an optionally substituted C3-C8-cycloalkyl and substituted piperidine; G3 is selected from an optionally substituted C1C6-alkoxy -C1-C6-alkyl; C1-C6-alkyl; substituted phenyl; substituted phenyl-C1C6-alkyl; G4 is selected from a substituted acyl-C1C6-alkyl, where acyl represents a group -CO-R and R stands for H or morpholine; optionally substituted C1-C6-alkyl; optionally substituted phenyl or indene; substituted phenyl-C1-C6-alkyl; optionally substituted pyridine- or furanyl-C1C6-alkyl; morpholine- or piperidine-C1-C6-alkyl; G5 represents H; where the term "substituted" stands for the groups, substituted with 1 to 5 substituents, selected from the group, which includes a "C1-C6-alkyl," "morpholine", "C1-C6-alkylphenyl", "di-C1-C6-alkylamino", "acylamino", which stands for the group NRCOR", where R represents H and R" represents a C1-C6-alkyl, "phenyl", "fluorine-substituted phenyl", "C1-C6-alkoxy", "C1-C6-alkoxycarbonyl", "halogen". The invention also relates to a pharmaceutical composition based on the formula (I) compound and particular compounds.

EFFECT: obtained are the novel derivatives of pyrasole pyridine, useful for the treatment and/or prevention of disorders or states, associated with NADPH-oxidase.

12 cl, 3 tbl, 21 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to field of biochemistry, in particular to cyclic peptide, capable of inducing antibody response. Peptide consists of formula X2X3VGSNK-Z or X3VGSNKG-Z, where X2 represents E, G, Q or K, X3 represents D or N and Z represents agent, stabilising bent, present inside peptide sequence, with peptide being cyclised by covalent bonding of N-end amino acid with Z, where Z represents peptide fragment YNGK. Conjugate, containing said cyclic peptide, conjugated with immunogenic carrier molecule is also claimed. peptide and conjugate, which contains it, can be applied for production of medication or as vaccine against Alzheimer's disease. Methods of obtaining cyclic peptide and conjugate are also claimed.

EFFECT: invention makes it possible to obtain improved, less toxic vaccine against Alzheimer's disease.

8 cl, 11 dwg, 1 tbl, 2 ex

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.

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