RU2012122886A - CAPSULES OF ACTIVE PHARMACEUTICAL INGREDIENTS AND COMPOUND ETHERS OF POLYUNSATURATED FATTY ACID FOR TREATMENT OF CARDIOVASCULAR DISEASES - Google Patents

CAPSULES OF ACTIVE PHARMACEUTICAL INGREDIENTS AND COMPOUND ETHERS OF POLYUNSATURATED FATTY ACID FOR TREATMENT OF CARDIOVASCULAR DISEASES Download PDF

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RU2012122886A
RU2012122886A RU2012122886/15A RU2012122886A RU2012122886A RU 2012122886 A RU2012122886 A RU 2012122886A RU 2012122886/15 A RU2012122886/15 A RU 2012122886/15A RU 2012122886 A RU2012122886 A RU 2012122886A RU 2012122886 A RU2012122886 A RU 2012122886A
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pharmaceutical capsule
group formed
alkyl esters
pharmaceutical
polyunsaturated fatty
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Паоло КАРМИНАТИ (умер)
ДУЭНЬЯ Антонио ПАРЕНТЕ
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ДжиПи ФАРМ С.А.
Дефианте Фармасеутика, С.А.
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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    • A61K31/20—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
    • A61K31/202—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids having three or more double bonds, e.g. linolenic
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Abstract

1. Фармацевтическая капсула, содержащая суспензию полимерных микрокапсул, содержащих по меньшей мере один полимер и активный фармацевтический ингредиент, выбранный из группы, сформированной ингибиторами ангиотензин-превращающих ферментов и блокаторами рецептора ангиотензина, причем эти микрокапсулы суспендированы в масле, которое содержит алкильные сложные эфиры полиненасыщенной жирной кислоты.2. Фармацевтическая капсула по п.1, где полиненасыщенные жирные кислоты этих алкильных сложных эфиров принадлежат к ряду омега-3.3. Фармацевтическая капсула по п.2, где полиненасыщенные жирные кислоты этих алкильных сложных эфиров выбраны из группы, сформированной эйкозапентаеновой кислотой, докозагексаеновой кислотой и/или их смесями.4. Фармацевтическая капсула по п.1, где алкильный радикал этих алкильных сложных эфиров выбран из группы, сформированной алкильными радикалами с короткой цепью от 1 до 8 атомов углерода.5. Фармацевтическая капсула по п.4, где алкильный радикал этих алкильных сложных эфиров выбран из группы, сформированной этилом, метилом, пропилом, бутилом и/или их смесями.6. Фармацевтическая капсула по п.1, где это масло содержит более чем 50% алкильных сложных эфиров полиненасыщенной жирной кислоты.7. Фармацевтическая капсула по п.1, где этот ингибитор ангиотензин-превращающего фермента выбран из группы, сформированной каптоприлом, эналаприлом, эналаприлатом, рамиприлом, хинаприлом, периндоприлом, лизиноприлом, беназеприлом, фозиноприлом, спираприлом, трандолаприлом, моэксиприлом, цилазаприлом, имидаприлом, рентиаприлом, темокаприлом, алацеприлом, делаприлом, мовелтиприлом, зофеноприлом, пентоприлом1. A pharmaceutical capsule containing a suspension of polymer microcapsules containing at least one polymer and an active pharmaceutical ingredient selected from the group formed by angiotensin converting enzyme inhibitors and angiotensin receptor blockers, these microcapsules suspended in oil that contains polyunsaturated fatty alkyl esters acids. 2. The pharmaceutical capsule of claim 1, wherein the polyunsaturated fatty acids of these alkyl esters belong to the omega-3.3 series. The pharmaceutical capsule of claim 2, wherein the polyunsaturated fatty acids of these alkyl esters are selected from the group formed by eicosapentaenoic acid, docosahexaenoic acid and / or mixtures thereof. The pharmaceutical capsule of claim 1, wherein the alkyl radical of these alkyl esters is selected from the group formed by short chain alkyl radicals of 1 to 8 carbon atoms. The pharmaceutical capsule of claim 4, wherein the alkyl radical of these alkyl esters is selected from the group formed by ethyl, methyl, propyl, butyl and / or mixtures thereof. The pharmaceutical capsule of claim 1, wherein the oil contains more than 50% polyunsaturated fatty acid alkyl esters. The pharmaceutical capsule according to claim 1, wherein the angiotensin-converting enzyme inhibitor is selected from the group formed by captopril, enalapril, enalaprilat, ramipril, hinapril, perindopril, lisinopril, benazepril, fosinopril, spirapril, trandolapril, moexipripril, impripril, trimethyl, , alacepril, delapril, moveltipril, zofenopril, pentopril

Claims (17)

1. Фармацевтическая капсула, содержащая суспензию полимерных микрокапсул, содержащих по меньшей мере один полимер и активный фармацевтический ингредиент, выбранный из группы, сформированной ингибиторами ангиотензин-превращающих ферментов и блокаторами рецептора ангиотензина, причем эти микрокапсулы суспендированы в масле, которое содержит алкильные сложные эфиры полиненасыщенной жирной кислоты.1. A pharmaceutical capsule containing a suspension of polymer microcapsules containing at least one polymer and an active pharmaceutical ingredient selected from the group formed by angiotensin converting enzyme inhibitors and angiotensin receptor blockers, these microcapsules suspended in an oil that contains polyunsaturated fatty alkyl esters acids. 2. Фармацевтическая капсула по п.1, где полиненасыщенные жирные кислоты этих алкильных сложных эфиров принадлежат к ряду омега-3.2. The pharmaceutical capsule according to claim 1, where the polyunsaturated fatty acids of these alkyl esters belong to the omega-3 series. 3. Фармацевтическая капсула по п.2, где полиненасыщенные жирные кислоты этих алкильных сложных эфиров выбраны из группы, сформированной эйкозапентаеновой кислотой, докозагексаеновой кислотой и/или их смесями.3. The pharmaceutical capsule according to claim 2, where the polyunsaturated fatty acids of these alkyl esters are selected from the group formed by eicosapentaenoic acid, docosahexaenoic acid and / or mixtures thereof. 4. Фармацевтическая капсула по п.1, где алкильный радикал этих алкильных сложных эфиров выбран из группы, сформированной алкильными радикалами с короткой цепью от 1 до 8 атомов углерода.4. The pharmaceutical capsule of claim 1, wherein the alkyl radical of these alkyl esters is selected from the group formed by short chain alkyl radicals of 1 to 8 carbon atoms. 5. Фармацевтическая капсула по п.4, где алкильный радикал этих алкильных сложных эфиров выбран из группы, сформированной этилом, метилом, пропилом, бутилом и/или их смесями.5. The pharmaceutical capsule of claim 4, wherein the alkyl radical of these alkyl esters is selected from the group formed by ethyl, methyl, propyl, butyl and / or mixtures thereof. 6. Фармацевтическая капсула по п.1, где это масло содержит более чем 50% алкильных сложных эфиров полиненасыщенной жирной кислоты.6. The pharmaceutical capsule of claim 1, wherein the oil contains more than 50% polyunsaturated fatty acid alkyl esters. 7. Фармацевтическая капсула по п.1, где этот ингибитор ангиотензин-превращающего фермента выбран из группы, сформированной каптоприлом, эналаприлом, эналаприлатом, рамиприлом, хинаприлом, периндоприлом, лизиноприлом, беназеприлом, фозиноприлом, спираприлом, трандолаприлом, моэксиприлом, цилазаприлом, имидаприлом, рентиаприлом, темокаприлом, алацеприлом, делаприлом, мовелтиприлом, зофеноприлом, пентоприлом, либензаприлом, пивоприлом, церонаприлом, индолаприлом, тепротидом, их фармацевтически приемлемыми солями и их кислотами.7. The pharmaceutical capsule according to claim 1, where the angiotensin-converting enzyme inhibitor is selected from the group formed by captopril, enalapril, enalaprilat, ramipril, quinapril, perindopril, lisinopril, benazpril, fosinopril, spirapril, trandolapril, moexipril, imexprilipril, imexprilpril, , temocapril, alacepril, delapril, moveltipril, zofenopril, pentopril, libenzapril, pivopril, ceronapril, indolapril, thermotide, their pharmaceutically acceptable salts and their acids. 8. Фармацевтическая капсула по п.1, где этот блокатор рецептора ангиотензина II выбран из группы, сформированной кандесартаном, эпросартаном, ирбесартаном, лозартаном, олмесартаном, телмисартаном, валсартаном, тазосартаном, пратосартаном, азилсартаном, саралазином, риписартаном, элисартаном, милфасартаном, эмбусартаном, фонсартаном, саприсартаном, золасартаном, форасартаном, помисартаном, абитесартаном, фимасартаном, N-бензил-лозартаном, ненолтазосартаном, глицил-лозартаном, опомисартаном, тритил-лозартаном, сармезином, изотеолином и их фармацевтически приемлемыми солями.8. The pharmaceutical capsule according to claim 1, where this angiotensin II receptor blocker is selected from the group formed by candesartan, eprosartan, irbesartan, losartan, olmesartan, telmisartan, valsartan, tazosartan, pratosartan, azilsartan, saralazine, risisartan, milasartan, embarisartan, milisartan, embryso fonsartan, saprisartan, zolasartan, forasartan, pomisartan, abitesartan, fimasartan, N-benzyl-losartan, nenoltazosartan, glycyl-losartan, opomisartan, trityl-losartan, sarmesin, isoteolin and their armatsevticheski acceptable salts. 9. Фармацевтическая капсула по п.1, где полимер этих микрокапсул выбран из группы, сформированной белками, сложными полиэфирами, полиакрилатами, полицианоакрилатами, полисахаридами, полиэтиленгликолем и/или их смесями.9. The pharmaceutical capsule according to claim 1, where the polymer of these microcapsules is selected from the group formed by proteins, polyesters, polyacrylates, polycyanoacrylates, polysaccharides, polyethylene glycol and / or mixtures thereof. 10. Фармацевтическая капсула по п.9, где полимер этих микрокапсул выбран из группы, сформированной желатином, альбумином, альгинатами, каррагенанами, пектинами, гуммиарабиком, хитозаном, карбоксиметилцеллюлозой, этилцеллюлозой, гидроксипропилметилцеллюлозой, нитроцеллюлозой, ацетобутиратом целлюлозы, ацетофталатом целлюлозы, фталатом гидроксипропилметилцеллюлозы, ацетосукцинатом гидроксипропилметилцеллюлозы, поливинилацетофталатом, поли(ε-капролактоном), поли(п-диоксаноном), поли(β-валеролактоном), поли(β-гидроксибутиратом), сополимерами поли(β-гидроксибутирата) и β-гидроксивалерата, поли(β-гидроксипропионатом), сополимерами метакриловой кислоты, сополимерами диметиламиноэтилметакрилата, сополимерами этилметакрилата триэтиламмония, полимерами и сополимерами молочной и гликолевой кислот, полимерами и сополимерами молочной и гликолевой кислот и полиэтиленгликоля и/или их смесями.10. The pharmaceutical capsule according to claim 9, where the polymer of these microcapsules is selected from the group formed by gelatin, albumin, alginates, carrageenans, pectins, gum arabic, chitosan, carboxymethyl cellulose, hydroxypropyl methyl cellulose, hydrocellulose cellulose acetate, cellulose acetate, cellulose acetate, hydroxypropyl methylcellulose, polyvinyl acetophthalate, poly (ε-caprolactone), poly (p-dioxanone), poly (β-valerolactone), poly (β-hydroxybutyrate), copoly with poly (β-hydroxybutyrate) and β-hydroxyvalerate, poly (β-hydroxypropionate) copolymers, methacrylic acid copolymers, dimethylaminoethyl methacrylate copolymers, triethylammonium ethyl methacrylate copolymers, lactic and glycolic acid polymers and copolymers, milk and glycol polymers and copolymers of polyethylene and glycol or glycol their mixtures. 11. Фармацевтическая капсула по п.1, где эти микрокапсулы составляют от 0,001% до 80% общего веса капсулы.11. The pharmaceutical capsule according to claim 1, where these microcapsules comprise from 0.001% to 80% of the total weight of the capsule. 12. Фармацевтическая капсула по п.1, где количество активного фармацевтического ингредиента, включенного в эти микрокапсулы, составляет от 1% до 80% по весу.12. The pharmaceutical capsule according to claim 1, where the amount of active pharmaceutical ingredient included in these microcapsules is from 1% to 80% by weight. 13. Фармацевтическая капсула по п.1, где полимер этих микрокапсул содержит по меньшей мере один пластификатор, разжижающее средство и/или антиоксидант.13. The pharmaceutical capsule according to claim 1, where the polymer of these microcapsules contains at least one plasticizer, a thinning agent and / or an antioxidant. 14. Фармацевтическая капсула по п.1, где композиция покрытия этой капсулы выбрана из группы, сформированной желатином, гидроксипропилметилцеллюлозой, пуллуланом, модифицированными крахмалами, каррагенанами и/или их смесями.14. The pharmaceutical capsule according to claim 1, where the coating composition of this capsule is selected from the group formed by gelatin, hydroxypropyl methylcellulose, pullulan, modified starches, carrageenans and / or mixtures thereof. 15. Фармацевтическая капсула по п.14, где это покрытие сделано из мягкого желатина.15. The pharmaceutical capsule of claim 14, wherein the coating is made of soft gelatin. 16. Фармацевтическая капсула по п.1, где эта капсула содержит энтеросолюбильное покрытие.16. The pharmaceutical capsule according to claim 1, where this capsule contains an enteric coating. 17. Фармацевтическая капсула по п.1, для лечения и/или предупреждения сердечно-сосудистых заболеваний. 17. The pharmaceutical capsule according to claim 1, for the treatment and / or prevention of cardiovascular disease.
RU2012122886/15A 2009-11-20 2010-11-19 CAPSULES OF ACTIVE PHARMACEUTICAL INGREDIENTS AND COMPOUND ETHERS OF POLYUNSATURATED FATTY ACID FOR TREATMENT OF CARDIOVASCULAR DISEASES RU2012122886A (en)

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