RU2019120821A - Твердые порошковые композиции, способ их получения, препараты и их применение - Google Patents

Твердые порошковые композиции, способ их получения, препараты и их применение Download PDF

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RU2019120821A
RU2019120821A RU2019120821A RU2019120821A RU2019120821A RU 2019120821 A RU2019120821 A RU 2019120821A RU 2019120821 A RU2019120821 A RU 2019120821A RU 2019120821 A RU2019120821 A RU 2019120821A RU 2019120821 A RU2019120821 A RU 2019120821A
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manufacturing
solid powder
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organic solvent
production
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Массимо РОНКИ
Джакомо МОМБЕЛЛИ
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Индена С.П.А.
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    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
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    • A61K47/24—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
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Claims (18)

1. Способ производства твердой порошковой композиции, включающий следующие стадии:
a) диспергирование водно-спиртового экстракта плодов бергамота в по меньшей мере одном полярном органическом растворителе и поддерживание при перемешивании до получения раствора или дисперсии; необязательно применение нагревания; при этом экстракт содержит флавоноиды неоэриоцитрин, нарингин и неогесперидин;
b) затем добавление по меньшей мере одиного фосфолипида к раствору/дисперсии экстракта плодов бергамота и поддержание смеси при перемешивании; где массовое отношение между по меньшей мере одним фосфолипидом и флавоноидами экстракта варьируется от 6 до 30; необязательно примеение нагревания;
c) затем удаление органического растворителя с получением твердой порошковой композиции.
2. Способ производства по п. 1, где массовое отношение варьируется от 6 до 20, предпочтительно от 6 до 12.
3. Способ производства по п. 1 или 2, где по меньшей мере один фосфолипид выбирают из группы, состоящей из лецитинов из сои, подсолнечника или яйца, фосфатидилхолина, фосфатидилсерина, фосфатидилэтаноламина, где ацильные группы, которые являются одинаковыми или отличными друг от друга, в основном происходят из пальмитиновой, стеариновой, олеиновой, линолевой и линоленовой кислот; или их комбинаций.
4. Способ производства по п. 3, где по меньшей мере один фосфолипид представляет собой лецитин.
5. Способ производства по пп. 1-4, также включающий дополнительное поверхностно-активное вещество, отличное от лецитина, с значением ГЛБ равным или больше чем 12.
6. Способ производства по п. 5, где дополнительное поверхностно-активное вещество выбирают из группы, состоящей из сложных эфиров сахарозы, полисорбатов, полиоксиэтиленовых производных касторового масла, полиоксиэтиленстеаратов, D-α-токоферил-полиэтиленгликоль сукцината или их комбинаций.
7. Способ производства по п. 6, где дополнительное поверхностно-активное вещество выбрано из сложных эфиров сахарозы и D-α-токоферил-полиэтиленгликоль сукцината.
8. Способ производства по п. 1, где полярный органический растворитель представляет собой полярный протонный растворитель или полярный апротонный растворитель.
9. Способ производства по п. 8, где полярный протонный растворитель представляет собой линейный или разветвленный С1-С8 алкиловый спирт.
10. Способ производства по п. 8, где полярный aпротонный растворитель выбирают из линейного или разветвленного С1-С8 алкилового эфира или С1-С8 диалкилкетона.
11. Способ производства по пп. 1-10, где полярный органический растворитель выбирают из группы, состоящей из этилового спирта, этилацетата, ацетона, изобутилового спирта, изопропилового спирта и их комбинаций.
12. Способ производства по п. 11, где органический растворитель выбирают из этилового спирта и этилацетата.
13. Твердая порошковая композиция, полученная способом производства по пп. 1-12.
14. Фармацевтический, нутрицевтический и косметический препараты, включающие твердую порошковую композицию по п. 13 и по меньшей мере один физиологически приемлемый эксципиент и/или носитель.
15. Твердая порошковая композиция по п. 13 или препарат по п. 14 для применения в профилактике и/или лечении метаболических синдромов, дислипидемий и диабета 2 типа.
RU2019120821A 2016-12-06 2017-11-29 Твердые порошковые композиции, способ их получения, препараты и их применение RU2765716C2 (ru)

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Application Number Priority Date Filing Date Title
EP16202405.3A EP3332768A1 (en) 2016-12-06 2016-12-06 Powder solid compositions comprising flavonoids, process for their preparation, formulations and use thereof
EP16202405.3 2016-12-06
PCT/EP2017/080866 WO2018104131A1 (en) 2016-12-06 2017-11-29 Powder solid compositions, process for their preparation, formulations and use thereof

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EP (2) EP3332768A1 (ru)
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