RU2016128400A - Фармацевтические композиции спиро-оксиндольного соединения для местного введения и их применение в качестве терапевтических агентов - Google Patents

Фармацевтические композиции спиро-оксиндольного соединения для местного введения и их применение в качестве терапевтических агентов Download PDF

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RU2016128400A
RU2016128400A RU2016128400A RU2016128400A RU2016128400A RU 2016128400 A RU2016128400 A RU 2016128400A RU 2016128400 A RU2016128400 A RU 2016128400A RU 2016128400 A RU2016128400 A RU 2016128400A RU 2016128400 A RU2016128400 A RU 2016128400A
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Конрад Стюарт ВИНТЕРС
Мэйдун ЯН
Хайган ЧЭНЬ
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Ксенон Фармасьютикалз Инк.
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Claims (14)

1. Фармацевтическая композиция для местного введения млекопитающему, содержащая терапевтически эффективное количество спиро-оксиндольного соединения, имеющего следующую формулу:
Figure 00000001
где спиро-оксиндольное соединение присутствует при концентрации от приблизительно 1% вес./вес. до приблизительно 8% вес./вес.; и растворитель, агент, улучшающий проникновение, загуститель и мазевую основу, где растворитель выбирают из PEG 400 или PEG 3350, агент, улучшающий проникновение, выбирают из Transcutol® P, олеинового спирта или изопропилмиристата, загуститель представляет собой стеариловый спирт, мазевую основу выбирают из PEG 400 или PEG 3350.
2. Фармацевтическая композиция по п.1, в которой PEG 400 присутствует при концентрации от приблизительно 46,9% вес./вес. до приблизительно 53,9% вес./вес., Transcutol® P присутствует при концентрации от приблизительно 5% вес./вес. до приблизительно 10% вес./вес., олеиновый спирт присутствует при концентрации приблизительно 5% вес./вес., изопропилмиристат присутствует при концентрации приблизительно 5% вес./вес., стеариловый спирт присутствует при концентрации от приблизительно 5% вес./вес. до приблизительно 10% вес./вес., и PEG 3350 присутствует при концентрации приблизительно 20% вес./вес.
3. Фармацевтическая композиция по п.2, в которой спиро-оксиндольное соединение присутствует при концентрации от приблизительно 2% вес./вес. до приблизительно 8% вес./вес.
4. Фармацевтическая композиция по п.1, содержащая спиро-оксиндольное соединение при концентрации 2,0% вес./вес.; PEG 400 при концентрации 52,9% вес./вес.; Transcutol® P при концентрации 10% вес./вес.; олеиновый спирт при концентрации 5% вес./вес.; изопропилмиристат при концентрации 5% вес./вес.; стеариловый спирт при концентрации 5% вес./вес.; и PEG 3350 при концентрации 20% вес./вес. фармацевтической композиции.
5. Фармацевтическая композиция по п.1, содержащая спиро-оксиндольное соединение при концентрации 4% вес./вес.; PEG 400 при концентрации 50,9% вес./вес.; Transcutol® P при концентрации 10% вес./вес.; олеиновый спирт при концентрации 5% вес./вес.; изопропилмиристат при концентрации 5% вес./вес.; стеариловый спирт при концентрации 5% вес./вес.; и PEG 3350 при концентрации 20% вес./вес. фармацевтической композиции.
6. Фармацевтическая композиция по п.1, содержащая спиро-оксиндольное соединение при концентрации 4% вес./вес.; PEG 400 при концентрации 50,9% вес./вес.; Transcutol® P при концентрации 5% вес./вес.; олеиновый спирт при концентрации 5% вес./вес.; изопропилмиристат при концентрации 5% вес./вес.; стеариловый спирт при концентрации 10% вес./вес.; и PEG 3350 при концентрации 20% вес./вес. фармацевтической композиции.
7. Фармацевтическая композиция по п.1, содержащая спиро-оксиндольное соединение при концентрации 8% вес./вес.; PEG 400 при концентрации 46,9% вес./вес.; Transcutol® P при концентрации 10% вес./вес.; олеиновый спирт при концентрации 5% вес./вес.; изопропилмиристат при концентрации 5% вес./вес.; стеариловый спирт при концентрации 5% вес./вес.; и PEG 3350 при концентрации 20% вес./вес. фармацевтической композиции.
8. Способ лечения, предотвращения или улучшения заболевания или состояния, опосредованного натриевыми каналами, у млекопитающего, включающий местное введение нуждающемуся в лечении млекопитающему терапевтически эффективного количества фармацевтической композиции по п.1.
9. Способ по п.8, в котором заболевание или состояние выбрано из группы, состоящей из невропатической боли, воспалительной боли, висцеральной боли, постгерпетической невралгии, боли при раке, боли при химиотерапии, боли в результате травмы, операционной боли, постоперационной боли, прурита, остеоартрита, невралгии тройничного нерва, семейной эритромелалгии, первичной эритромелалгии, семейной ректальной боли, боли при родах, боли при родовых схватках, нейрогенного мочевого пузыря, язвенного колита, хронической боли, постоянной боли, периферически опосредованной боли, центрально опосредованной боли, хронической головной боли, мигрени, синусовой головной боли, головной боли напряжения, фантомной боли конечностей, травмы периферических нервов и их комбинаций.
10. Способ по п.8, в котором млекопитающим является человек.
11. Способ лечения боли за счет ингибирования ионного тока через потенциал-зависимые натриевые каналы у млекопитающего, включающий местное введение нуждающемуся в лечении млекопитающему терапевтически эффективного количества фармацевтической композиции по п.1.
12. Способ по п.11, в котором млекопитающим является человек.
RU2016128400A 2010-02-26 2011-02-25 Фармацевтические композиции спиро-оксиндольного соединения для местного введения и их применение в качестве терапевтических агентов RU2016128400A (ru)

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