RU2356550C2 - Комбинации активатора (активаторов) рецептора, активируемого пролифератором пероксисом (рапп), и ингибитора (ингибиторов) всасывания стерина и лечение заболеваний сосудов - Google Patents

Комбинации активатора (активаторов) рецептора, активируемого пролифератором пероксисом (рапп), и ингибитора (ингибиторов) всасывания стерина и лечение заболеваний сосудов Download PDF

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RU2356550C2
RU2356550C2 RU2003126184/15A RU2003126184A RU2356550C2 RU 2356550 C2 RU2356550 C2 RU 2356550C2 RU 2003126184/15 A RU2003126184/15 A RU 2003126184/15A RU 2003126184 A RU2003126184 A RU 2003126184A RU 2356550 C2 RU2356550 C2 RU 2356550C2
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Тедди КОСОГЛОУ (US)
Тедди КОСОГЛОУ
Гарри Р. ДЭВИС (US)
Гарри Р. ДЭВИС
Жилль Жан Бернар ПИКАР (BE)
Жилль Жан Бернар ПИКАР
Винг-Ки Филип ШО (US)
Винг-Ки Филип ШО
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Abstract

Изобретение относится к области фармакологии и медицины и касается фармацевтической композиции для лечения или предупреждения сосудистого патологического состояния, диабета, ожирения или снижения концентрации стерина в плазме млекопитающего, включающей ингибитор всасывания стерина формулы (II), моногидрат лактозы, микрокристаллическую целлюлозу, поливинилпирролидон, натриевую соль кроскармелозы, лаурилсульфат натрия и стеарат магния. Изобретение обеспечивает улучшенную растворимость композиции. 20 з.п. ф-лы, 4 табл.

Description

Текст описания приведен в факсимильном виде.
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Claims (23)

1. Фармацевтическая композиция, обладающая свойствами агента для лечения или предупреждения сосудистого патологического состояния, диабета, ожирения или снижения концентрации стерина в плазме млекопитающего, включающая
(а) ингибитор всасывания стерина формулы (II)
Figure 00000120

или его фармацевтически приемлемые соли или сольваты,
(b) моногидрат лактозы,
(c) микрокристаллическую целлюлозу,
(d) поливинилпирролидон,
(е) натриевую соль кроскармелозы,
(f) лаурилсульфат натрия, и
(g) стеарат магния.
2. Фармацевтическая композиция по п.1, содержащая от около 0,1 до около 1000 мг соединения формулы (II) или его фармацевтически приемлемой соли или сольвата.
3. Фармацевтическая композиция по п.2, содержащая от около 0,25 до около 50 мг соединения формулы (II) или его фармацевтически приемлемой соли или сольвата.
4. Фармацевтическая композиция по п.3, содержащая около 10 мг соединения формулы (II) или его фармацевтически приемлемой соли или сольвата.
5. Фармацевтическая композиция по п.1, содержащая от около 0,1 до около 90 мас.% моногидрата лактозы в расчете на полную массу композиции.
6. Фармацевтическая композиция по п.5, содержащая около 55 мг моногидрата лактозы.
7. Фармацевтическая композиция по п.1, содержащая от около 0,1 до около 90 мас.% микрокристаллической целлюлозы в расчете на полную массу композиции.
8. Фармацевтическая композиция по п.7, содержащая около 20 мг микрокристаллической целлюлозы.
9. Фармацевтическая композиция по п.1, содержащая от около 0,1 до около 90 мас.% поливинилпирролидона в расчете на полную массу композиции.
10. Фармацевтическая композиция по п.9, содержащая около 4 мг поливинилпирролидона.
11. Фармацевтическая композиция по п.1, содержащая от около 0,1 до около 90 мас.% натриевой соли кроскармелозы в расчете на полную массу композиции.
12. Фармацевтическая композиция по п.11, содержащая около 8 мг натриевой соли кроскармелозы.
13. Фармацевтическая композиция по п.1, содержащая от около 0,1 до около 90 мас.% лаурилсульфата натрия в расчете на полную массу композиции.
14. Фармацевтическая композиция по п.13, содержащая около 2 мг лаурилсульфата натрия.
15. Фармацевтическая композиция по п.1, содержащая от около 0,1 до около 90 мас.% стеарата магния в расчете на полную массу композиции.
16. Фармацевтическая композиция по п.15, содержащая около 1 мг стеарата магния.
17. Фармацевтическая композиция по п.1, дополнительно включающая, по крайней мере, один активатор рецептора, активируемого пролифератором пероксисом.
18. Фармацевтическая композиция по п.17, в которой, по крайней мере, один активатор рецептора, активируемого пролифератором пероксисом, представляет собой производное фибриновой кислоты, выбранное из группы, включающей фенофибрат, клофибрат, гемфиброзил, ципрофибрат, безафибрат, клинофибрат, бинифибрат, лифиброл и их смеси.
19. Фармацевтическая композиция по п.18, в которой производное фибриновой кислоты представляет собой фенофибрат.
20. Фармацевтическая композиция по п.1, в которой ингредиенты взяты в следующем количественном соотношении, мас.%:
Соединение формулы (II) 10 Лактозы моногидрат 55 Микрокристаллическая целлюлоза 20 Поливинилпирролидон 4 Натриевая соль кроскармелозы 8 Лаурилсульфат натрия 2 Стеарат магния 1
21. Фармацевтическая композиция по п.1, в которой ингредиенты взяты в следующем количестве, мг:
Соединение формулы (II) 10 Лактозы моногидрат 55 Микрокристаллическая целлюлоза 20 Поливинилпирролидон 4 Натриевая соль кроскармелозы 8 Лаурилсульфат натрия 2 Стеарат магния 1

Приоритет по пунктам:
26.01.2001 по пп.1-16, 19-21;
21.09.2001 по пп.17, 18.
RU2003126184/15A 2001-01-26 2002-01-25 Комбинации активатора (активаторов) рецептора, активируемого пролифератором пероксисом (рапп), и ингибитора (ингибиторов) всасывания стерина и лечение заболеваний сосудов RU2356550C2 (ru)

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