RU2015134143A - Композиции твердых растворов и их применение при сердечно-сосудистом заболевании - Google Patents

Композиции твердых растворов и их применение при сердечно-сосудистом заболевании Download PDF

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RU2015134143A
RU2015134143A RU2015134143A RU2015134143A RU2015134143A RU 2015134143 A RU2015134143 A RU 2015134143A RU 2015134143 A RU2015134143 A RU 2015134143A RU 2015134143 A RU2015134143 A RU 2015134143A RU 2015134143 A RU2015134143 A RU 2015134143A
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pharmaceutical composition
disease
glycerol
solid solution
heart
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RU2015134143A
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RU2674982C2 (ru
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Робин Марк Баннистер
Джон Брю
Ричард Роберт РЕЙЛИ
Уилсон КАПАРРОС-ВАНДЕРЛЕЙ
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ИнФерст Хэлткэр Лимитед
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Claims (23)

1. Фармацевтическая композиция твердого раствора, включающая:
a) один или несколько статинов в количестве от приблизительно 1 до приблизительно 30% от массы фармацевтической композиции;
b) один или более фармацевтически приемлемых твердых жиров в количестве от приблизительно 30 до приблизительно 75% от массы фармацевтической композиции;
c) один или более фармацевтически приемлемых моноглицеридов или ацетилированных моноглицеридов, которые являются жидкими при комнатной температуре, в количестве от приблизительно 8 до приблизительно 40% от массы фармацевтической композиции,
где фармацевтическая композиция твердого раствора приготовлена так, что она является твердой при температуре приблизительно 15°C или ниже.
2. Фармацевтическая композиция твердого раствора по п. 1, где количество одного или более статинов составляет от приблизительно 1 до приблизительно 15% от массы фармацевтической композиции.
3. Фармацевтическая композиция по п. 1, где один или более статинов включают аторвастатин, флувастатин, ловастатин, питавастатин, правастатин, розувастатин и симвастатин.
4. Фармацевтическая композиция твердого раствора по п. 1, где количество одного или более фармацевтически приемлемых твердых жиров составляет, по меньшей мере, 55% от массы фармацевтической композиции.
5. Фармацевтическая композиция твердого раствора по п. 1, где один или более фармацевтически приемлемых твердых жиров имеют температуру плавления от приблизительно 40 до приблизительно 50°C.
6. Фармацевтическая композиция твердого раствора по п. 5, где один или более фармацевтически приемлемых твердых жиров включают один или более глицеролипидов.
7. Фармацевтическая композиция твердого раствора по п. 6, где один или более глицеролипидов включают триглицерид с одной насыщенной или ненасыщенной жирной кислотой, имеющей длину углеродной цепи C12-C24, двумя насыщенными или ненасыщенными жирными кислотами, каждая из которых имеет длину углеродной цепи C12-C24, или тремя насыщенными или ненасыщенными жирными кислотами, каждая из которых имеет длину углеродной цепи C12-C24.
8. Фармацевтическая композиция твердого раствора по п. 6, где один или более глицеролипидов включают смесь насыщенных C10-C18 триглицеридов, имеющих температуру плавления от приблизительно 41 до 45°C.
9. Фармацевтическая композиция твердого раствора по п. 8, где один или более глицеролипидов включают смесь насыщенных C10-C18 триглицеридов, имеющих температуру плавления приблизительно 43°C.
10. Фармацевтическая композиция твердого раствора по п. 1, где количество одного или более фармацевтически приемлемых моноглицеридов или ацетилированных моноглицеридов составляет менее чем 35% от массы фармацевтической композиции.
11. Фармацевтическая композиция твердого раствора по п. 10, где один или более фармацевтически приемлемых моноглицеридов или ацетилированных моноглицеридов включают глицерина мономиристолеат, глицерина монопальмитолеат, глицерина моносапиенат, глицерина моноолеат, глицерина моноэлаидат, глицерина моновакценат, глицерина монолинолеат, глицерина монолиноэлаидат, глицерина монолиноленат, глицерина моностеаридонат, глицерина моноэйкозеноат, глицерина мономеадат, глицерина моноарахидонат, глицерина моноэйкозапентаеноат, глицерина моноэрукат, глицерина монодокозагексаеноат, глицерина мононервонат.
12. Фармацевтическая композиция твердого раствора по п. 11, где один или более фармацевтически приемлемых моноглицеридов или ацетилированных моноглицеридов включают глицерина монолинолеат.
13. Применение фармацевтической композиции по любому одному из пп. 1-12 в производстве лекарственного препарата для лечения сердечно-сосудистого заболевания.
14. Применение по п. 13, где сердечно-сосудистое заболевание связано с гиперлипидемией, коронарной болезнью сердца, атеросклерозом, заболеванием периферических кровеносных сосудов, окклюзивным заболеванием сосудов, кардиомиопатей, васкулитом, воспалительным заболеванием сердца, ишемической болезнью сердца, сердечной недостаточностью с застойными явлениями, гипертонической болезнью сердца, пороком клапана сердца, гипертензией, инфарктом миокарда, диабетическими сердечными состояниями, аневризмой, эмболией, расслоением, псевдоаневризмой, сосудистой патологией, каверномой, тромбозом, варикозом вен или инсультом.
15. Применение фармацевтической композиции по любому одному из пп. 1-12 для лечения сердечно-сосудистого заболевания.
16. Применение по п. 15, где сердечно-сосудистое заболевание связано с гиперлипидемией, коронарной болезнью сердца, атеросклерозом, заболеванием периферических кровеносных сосудов, окклюзивным заболеванием сосудов, кардиомиопатей, васкулитом, воспалительным заболеванием сердца, ишемической болезнью сердца, сердечной недостаточностью с застойными явлениями, гипертонической болезнью сердца, пороком клапана сердца, гипертензией, инфарктом миокарда, диабетическими сердечными состояниями, аневризмой, эмболией, расслоением, псевдоаневризмой, сосудистой патологией, каверномой, тромбозом, варикозом вен или инсультом.
17. Способ лечения индивидуума, страдающего сердечно-сосудистым заболеванием, где способ включает стадию введения индивидууму, если это ему необходимо, фармацевтической композиции по пп. 1-12, где введение приводит в результате к уменьшению интенсивности симптома, связанного с сердечно-сосудистым заболеванием, вследствие чего происходит лечение индивидуума.
18. Способ по п. 17, где сердечно-сосудистое заболевание связано с гиперлипидемией, коронарной болезнью сердца, атеросклерозом, заболеванием периферических кровеносных сосудов,
окклюзивным заболеванием сосудов, кардиомиопатей, васкулитом, воспалительным заболеванием сердца, ишемической болезнью сердца, сердечной недостаточностью с застойными явлениями, гипертонической болезнью сердца, пороком клапана сердца, гипертензией, инфарктом миокарда, диабетическими сердечными состояниями, аневризмой, эмболией, расслоением, псевдоаневризмой, сосудистой патологией, каверномой, тромбозом, варикозом вен или инсультом.
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