RU2011148363A - Фармацевтические композиции, содержащие ера и сердечно-сосудистое средство, и способ их применения - Google Patents
Фармацевтические композиции, содержащие ера и сердечно-сосудистое средство, и способ их применения Download PDFInfo
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Abstract
1. Фармацевтическая композиция для лечения или профилактики сердечно-сосудистых заболеваний, где фармацевтическая композиция содержит по меньшей мере приблизительно 90% ЕРА по массе от всех жирных кислот, присутствующих в композиции, и сердечно-сосудистое средство.2. Композиция по п.1, где сердечно-сосудистое средство представляет собой ингибитор АСАТ, ингибитор АСЕ, альфа-блокатор, альфа/бета-блокатор, антагонист рецепторов ангиотензина II, антиаритмическое средство, антитромбоцитарное средство, бета-блокатор, блокатор кальциевых каналов, ингибитор редуктазы HMG-CoA, миметик ароА-1, ингибитор СЕТР, усилитель экскреции желчных кислот, ингибитор всасывания холестерина, диуретик, средство против дислипидемии, антагонист рецепторов эндотелина, индуктор рецепторов LDL, ингибитор Lp-PLA2, ингибитор скваленэпоксидазы, активатор LCAT, ингибитор микросомального белка-переносчика триглицеридов, ингибитор SPLA2, ингибитор 5-липоксигеназы, агонист/активатор PPAR, тромболитическое средство, активатор бета-рецепторов щитовидной железы, ингибитор агрегации тромбоцитов или антагонист альдостерона.3. Композиция по п.1, где сердечно-сосудистое средство выбрано из группы, включающей ингибитор 5-LO 6, А-0002, абциксимаб, АВТ-335, АВТ-761, ацебутолол, аденозин, AEGR-733, альдактон, алискирен, алискирен гемифумарат, аллиин, амиодарон, амлодипин, анацетрапиб, АРА-01, апиксабан, APL180, АРР018, аспирин, атенолол, аторвастатин, AVE5530, AZD-2479, BAY-60-5521, беназеприл, BMS-200150, бозентан, бутенафин, кандесартан, каптоприл, карведилол, CER-002, хлортиазид натрия, хлорпропамид, холинфенофибрат, CI-1011, цилостазол, бутират клевидипина, клонидин, клопидогрель, CMI 977, колесевелам, колестипол, С
Claims (35)
1. Фармацевтическая композиция для лечения или профилактики сердечно-сосудистых заболеваний, где фармацевтическая композиция содержит по меньшей мере приблизительно 90% ЕРА по массе от всех жирных кислот, присутствующих в композиции, и сердечно-сосудистое средство.
2. Композиция по п.1, где сердечно-сосудистое средство представляет собой ингибитор АСАТ, ингибитор АСЕ, альфа-блокатор, альфа/бета-блокатор, антагонист рецепторов ангиотензина II, антиаритмическое средство, антитромбоцитарное средство, бета-блокатор, блокатор кальциевых каналов, ингибитор редуктазы HMG-CoA, миметик ароА-1, ингибитор СЕТР, усилитель экскреции желчных кислот, ингибитор всасывания холестерина, диуретик, средство против дислипидемии, антагонист рецепторов эндотелина, индуктор рецепторов LDL, ингибитор Lp-PLA2, ингибитор скваленэпоксидазы, активатор LCAT, ингибитор микросомального белка-переносчика триглицеридов, ингибитор SPLA2, ингибитор 5-липоксигеназы, агонист/активатор PPAR, тромболитическое средство, активатор бета-рецепторов щитовидной железы, ингибитор агрегации тромбоцитов или антагонист альдостерона.
3. Композиция по п.1, где сердечно-сосудистое средство выбрано из группы, включающей ингибитор 5-LO 6, А-0002, абциксимаб, АВТ-335, АВТ-761, ацебутолол, аденозин, AEGR-733, альдактон, алискирен, алискирен гемифумарат, аллиин, амиодарон, амлодипин, анацетрапиб, АРА-01, апиксабан, APL180, АРР018, аспирин, атенолол, аторвастатин, AVE5530, AZD-2479, BAY-60-5521, беназеприл, BMS-200150, бозентан, бутенафин, кандесартан, каптоприл, карведилол, CER-002, хлортиазид натрия, хлорпропамид, холинфенофибрат, CI-1011, цилостазол, бутират клевидипина, клонидин, клопидогрель, CMI 977, колесевелам, колестипол, СР-346086, СР-800569, CRD-5, CS-505, CSL111, далцетрапиб, далтепарин, дарапладиб, дефибротид, диаллилдисульфид, диаллилтрисульфид, дигоксин, дилтиазем, дипиридамол, дирлотапид, дизопирамид, доксазозин, эналаприл, эналаприлат, эноксапарин, эплеренон, эпросартан, эпротиром, эптифибатид, ЕТС-1001, ЕТС-216, ЕТС-588-липосому, ETC-642, этакриновую кислоту, эзетимиб, фенофибрат, флекаинид, флувастатин, фондапаринукс, фозиноприл, FR194738, фуросемид, гемфиброзил, GFT14, GFT505, глимепирид, глибурид, GSK-256073, GW501516, гидрохлоротиазид, имплитапид, индапамид, ирбесартан, исрадипин, JTT-130, JTT-705, KD-3010, ларопипрант, фермент LCAT, LCP-AtorFen, лидокаин, лизиноприл, лонапален, лозартан, ловастатин, LY 333013, MAHDL01, МВ07811, МВХ-8025, метилдофа, метопролол сукцинат, мексилетин, метопролол, МК-886, моэксиприл, надолол, NB-598, NCX6560, небиволол, ниацин, ниаспан, никардипин, нимодипин, нисолдипин, олмесартан, орлистат, РНКи PCSK9, PD-348292, периндоприл, PF-3185043, пиндолол, пиоглитазон, PLX204, правастатин, празозин, прокаинамид, гидрохлорид пропафенона, гидрохлорид пропранолола, хинаприл, хинидинглюконат, R7232, рамиприл, рекомбинантный ароА-1, рекомбинантный LCAT, ресвератрол (транс-3,41,5-тригидроксистильбен), обратный D-4F, рилапладиб, росиглитазон, росиглитазонмалеат, розувастатин, RVX-208, RWJ 800025, S-аллилцистеин, селеноцистеин, силденафил, симвастатин, SLx-4090, зобетиром (QRX-431), тадалафил, телмисартан, теразозин, телин, тиклопидин, тирофибан, токайнид, толазамид, торцетрапиб, торсемид, трандолаприл, TRIA-662, триамтерен, гримерный АроА-1, валсартан, варденафил, VIA-2291, верапамил, вареспладиб, волибрис, WA8242A, WA8242A2, WA8242B, ZD2138 или их фармацевтически приемлемая комбинация.
4. Композиция по п.1, дополнительно содержащая дополнительное сердечно-сосудистое средство.
5. Композиция по п.4, где дополнительное сердечно-сосудистое средство выбрано из ингибитора АСАТ, ингибитора АСЕ, альфа-блокатора, альфа/бета-блокатора, антагониста рецепторов ангиотензина II, антиаритмического средства, антитромбоцитарного средства, бета-блокатора, блокатора кальциевых каналов, ингибитора редуктазы HMG-CoA, миметика ароА-1, ингибитора СЕТР, усилителя экскреции желчных кислот, ингибитора всасывания холестерина, диуретика, средства против дислипидемии, антагониста рецепторов эндотелина, индуктора рецепторов LDL, ингибитора Lp-PLA2, ингибитора скваленэпоксидазы, активатора LCAT, ингибитора микросомального белка-переносчика триглицеридов, агониста/активатора PPAR, тромболитического средства, активатора бета-рецепторов щитовидной железы, ингибитора агрегации тромбоцитов или антагониста альдостерона.
6. Композиция по п.1, дополнительно содержащая фармацевтически приемлемый эксципиент.
7. Композиция по п.6, где эксципиент выбран из носителя, разбавителя, антиоксиданта, ароматизатора, подсластителя, красителя, суспендирующего средства или их сочетания.
8. Композиция по п.1, где ЕРА присутствует в количестве приблизительно от 100 мг до приблизительно 1500 мг.
9. Композиция по п.1, где композиция содержит менее 0,5% DHA или ее производного по массе от всех жирных кислот.
10. Композиция по п.1, где композиция по существу не содержит DHA или ее производного.
11. Композиция по п.1, где массовое отношении ЕРА к другим жирным кислотам составляет по меньшей мере приблизительно 96:4.
12. Композиция по п.1, где ЕРА содержит сложный C1-C5-алкиловый эфир.
13. Композиция по п.12, где сложный С1-С5-алкиловый эфир содержит этиловый эфир ЕРА.
14. Композиция по п.1, где композиция содержит менее 1% токоферолов по массе, если вообще содержит.
15. Композиция по п.1, где композиция находится в перорально доставляемой лекарственной форме.
16. Композиция по п.15, где лекарственная форма включает таблетку, каплет, капсулу, порошок, таблетку-леденец, саше, крахмальную капсулу, пастилку, пилюлю, гранулу, микрогранулу, инкапсулированную микрогранулу или порошковый аэрозоль.
17. Композиция по п.1, где сердечно-сосудистое средство суспендируют в ЕРА.
18. Композиция по п.17, где суспензия по существу является однородной.
19. Композиция по п.18, где композиция находится в капсуле.
20. Композиция по п.1, где сердечно-сосудистое средство включает орлистат или метформин.
21. Способ лечения связанного с сердечно-сосудистой системой заболевания, включающий введение нуждающемуся в этом индивидууму композиции, содержащей по меньшей мере 90% этил-ЕРА по массе от всех жирных кислот, присутствующих в композиции, и сердечно-сосудистого средства.
22. Способ по п.21, где связанное с сердечно-сосудистой системой заболевание выбрано из группы, состоящей из острых ишемических нарушений сердца, острого инфаркта миокарда, болезни Альцгеймера, стенокардии, грудной жабы, аритмии, фибрилляции предсердий, атеросклероза, фибрилляции предсердий, сердечной недостаточности, сердечно-сосудистого заболевания, хронической сердечной недостаточности, хронической стабильной стенокардии, застойной сердечной недостаточности, ишемической болезни сердца, атеросклеротической болезни сердца, тромбоза глубоких вен, диабета, сахарного диабета, диабетической нейропатии, диастолической дисфункции у индивидуумов с сахарным диабетом, отека, первичной артериальной гипертензии, потенциальной эмболии сосудов легких, жировой болезни печени, сердечного заболевания, сердечной недостаточности, гомозиготной семейной гиперхолестеринемии (HoFH), гомозиготной семейной ситостеролемии, гиперхолестеринемии, гиперлипидемии, гиперлипидемии у ВИЧ-положительных индивидуумов, гипертензии, гипертриглицеридемии, ишемических осложнений при нестабильной стенокардии и инфаркте миокарда, низкого артериального давления, метаболического синдрома, смешанной дислипидемии, сердечной недостаточности от умеренной до мягкой, инфаркта миокарда, контроля ожирения, пароксизмальной фибрилляции/трепетания предсердий (PAF), пароксизмальных наджелудочковых тахикардии (PSVT), очень тяжелого отека или отека с быстрым началом, агрегации тромбоцитов, первичной гиперхолестеринемии, первичной гиперлипидемии, легочной артериальной гипертензии, легочной гипертензии, пароксизмальной гемодинамически нестабильной желудочковой тахикардии (VT), пароксизмальных желудочковых аритмий, пароксизмальных фибрилляций желудочков (VF), разорвавшейся аневризмы, ситостеролемии, инсульта, наджелудочковой тахикардии, симптоматической фибрилляции/трепетания предсердий, тахикардии, диабета II типа, сосудистого заболевания, венозной тромбоэмболии и желудочковых аритмий.
23. Способ по п.22, где сердечно-сосудистое средство выбрано из группы, состоящей из ингибитора АСАТ, ингибитора АСЕ, альфа-блокатора, альфа/бета-блокатора, антагониста рецепторов ангиотензина II, антиаритмического средства, антитромбоцитарного средства, бета-блокатора, блокатора кальциевых каналов, ингибитора редуктазы HMG-CoA, миметика ароА-1, ингибитора СЕТР, усилителя экскреции желчных кислот, ингибитора всасывания холестерина, диуретика, средства против дислипидемии, антагониста рецепторов эндотелина, индуктора рецепторов LDL, ингибитора Lp-PLA2, ингибитора скваленэпоксидазы, активатора LCAT, ингибитора микросомального белка-переносчика триглицеридов, агониста/активатора PPAR, тромболитического средства, активатора бета-рецепторов щитовидной железы, ингибитора агрегации тромбоцитов или антагониста альдостерона.
24. Способ по п.23, где сердечно-сосудистое средство выбрано из группы, состоящей из ингибитора 5-LO 6, А-0002, абциксимаба, АВТ-335, АВТ-761, ацебутолол, аденозина, AEGR-733, альдактона, алискирена, гемифумарата алискирена, аллиина, амиодарона, амлодипина, анацетрапиба, АРА-01, апиксабана, APL180, АРР018, аспирина, атенолола, аторвастатина, AVE5530, AZD-2479, BAY-60-5521, беназеприла, BMS-200150, бозентана, бутенафина, кандесартана, каптоприла, карведилола, CER-002, хлортиазида натрия, хлорпропамида, холинфенофибрата, CI-1011, цилостазола, бутирата клевидипина, клонидина, клопидогреля, CMI 977, колесевелама, колестипола, СР-346086, СР-800569, CRD-5, CS-505, CSL111, далцетрапиба, далтепарина, дарапладиба, дефибротида, диаллилдисульфида, диаллилтрисульфида, дигоксина, дилтиазема, дипиридамола, дирлотапида, дизопирамида, доксазозина, эналаприла, эналаприлата, эноксапарина, эплеренона, эпросартана, эпротирома, эптифибатида, ЕТС-1001, ЕТС-216, ЕТС-588-липосомы, ЕТС-642, этакриновой кислоты, эзетимиба, фенофибрата, флекаинида, флувастатина, фондапаринукса, фозиноприла, FR194738, фуросемида, гемфиброзила, GFT14, GFT505, глимепирида, глибурида, GSK-256073, GW501516, гидрохлоротиазида, имплитапида, индапамида, ирбесартана, исрадипина, JTT-130, JTT-705, KD-3010, ларопипранта, фермента LCAT, LCP-AtorFen, лидокаина, лизиноприла, лонапалена, лозартана, ловастатина, LY 333013, MAHDL01, МВ07811, МВХ-8025, метилдофы, метопрололсукцината, мексилетина, метопролола, МК-886, моэксиприла, надолола, NB-598, NCX6560, небиволола, ниацина, ниаспана, никардипина, нимодипина, нисолдипина, олмесартана, орлистата, РНКи PCSK9, PD-348292, периндоприла, PF-3185043, пиндолола, пиоглитазона, PLX204, правастатина, празозина, прокаинамида, гидрохлорида пропафенона, гидрохлорида пропранолола, хинаприла, хинидинглюконата, R7232, рамиприла, рекомбинантного ароА-1, рекомбинантного LCAT, ресвератрола (транс-3,4',5-тригидроксистильбена), обратного D-4F, рилапладиба, росиглитазона, росиглитазонмалеата, розувастатина, RVX-208, RWJ 800025, S-аллилцистеина, селеноцистеина, силденафила, симвастатина, SLx-4090, зобетиромаа (QRX-431), тадалафила, телмисартана, теразозина, телина, тиклопидина, тирофибана, токайнида, толазамида, торцетрапиба, торсемида, трандолаприла, TRIA-662, триамтерена, гримерного АроА-1, валсартана, варденафила, VIA-2291, верапамила, вареспладиба, волибриса, WA8242A, WA8242A2, WA8242B, ZD2138 или их фармацевтически приемлемая комбинация.
25. Способ по п.21, где сердечно-сосудистое средство и ЕРА вводят совместно в виде отдельных единиц дозирования.
26. Способ по п.21, где ЕРА и сердечно-сосудистое средство формулируют совместно и вводят в виде одной единицы дозирования.
27. Способ по п.26, где единицу дозирования вводят от одного до множества раз в сутки.
28. Способ лечения гипертриглицеридемии у ВИЧ+индивидуума, где способ включает введение индивидууму фармацевтической композиции, содержащей ингибитор протеазы ВИЧ-1 и по меньшей мере приблизительно 90% этил-ЕРА по массе от всех жирных кислот, присутствующих в фармацевтической композиции.
29. Способ по п.28, где ингибитор протеазы ВИЧ-1 включает ампренавир, фосампренавир, индинавир, лопинавир, нелфинавир, ритонавир, саквинавир или их сочетание.
30. Способ лечения или предотвращение ожирения у нуждающегося в этом индивидуума, где способ включает введение индивидууму фармацевтической композиции, содержащей по меньшей мере приблизительно 90% этил-ЕРА по массе от всех жирных кислот, присутствующих в композиции и орлистат.
31. Способ по п.30, где ЕРА и орлистат вводят в одной единице дозирования.
32. Способ по п.30, где ЕРА и орлистат вводят совместно в раздельных единицах дозирования.
33. Способ лечения диабета II типа у нуждающегося в этом индивидуума, где способ включает введение индивидууму фармацевтической композиции, содержащей по меньшей мере приблизительно 90% ЕРА по массе от всех жирных кислот, присутствующих в композиции, и метформин.
34. Способ по п.33, где ЕРА и метформин вводят в одной единице дозирования.
35. Способ по п.33, где ЕРА и метформин вводят совместно в раздельных единицах дозирования.
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