RU2018101473A - Депо-препарат, содержащий сложный эфир лимонной кислоты - Google Patents

Депо-препарат, содержащий сложный эфир лимонной кислоты Download PDF

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RU2018101473A
RU2018101473A RU2018101473A RU2018101473A RU2018101473A RU 2018101473 A RU2018101473 A RU 2018101473A RU 2018101473 A RU2018101473 A RU 2018101473A RU 2018101473 A RU2018101473 A RU 2018101473A RU 2018101473 A RU2018101473 A RU 2018101473A
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depot composition
composition according
trialkyl citrate
citrate
depot
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Тацуя Миязаки
Кендзи МАСАКИ
Кёхей ТАКАХАСИ
Кацухито ЯМАДА
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Сантэн Фармасьютикал Ко., Лтд.
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Claims (22)

1. Депо-композиция, содержащая триалкилцитрат и/или ацетилтриалкилцитрат, где алкильные группы, которыми обладает каждый из триалкилцитрата и ацетилтриалкилцитрата, являются одинаковыми или разными и имеют число атомов углерода от 3 до 5.
2. Депо-композиция по п. 1, где число атомов углерода алкильной группы составляет 4.
3. Депо-композиция по п. 1, где триалкилцитрат представляет собой три-н-бутилцитрат, и ацетилтриалкилцитрат представляет собой ацетил-три-н-бутилцитрат.
4. Депо-композиция по п. 1, дополнительно содержащая лекарственное средство.
5. Депо-композиция по п. 4, где лекарственное средство представляет собой соединение формулы (1) или его соль:
[Химическая структура 1]
Figure 00000001
,
где R1 означает атом водорода, атом галогена, гидроксильную группу, С1-6алкильную группу, C1-6алкильную группу, замещенную одним или более атомами галогена, С1-6алкоксильную группу или C1-6алкоксильную группу, замещенную одним или более атомами галогена; и
R2 означает атом водорода, C1-6алкильную группу, С1-6алкилкарбонильную группу или C1-6алкилкарбонильную группу, замещенную одной или более гидроксильными группами.
6. Депо-композиция по п. 5, где соединение формулы (1) представляет собой 2-[[[2-[(гидроксиацетил)амино]-4-пиридинил]метил]тио]-N-[4-(трифторметокси)фенил]-3-пиридинкарбоксамид или его соль.
7. Депо-композиция по п. 4, где лекарственное средство представляет собой изопропил-(6-{[4-(пиразол-1-ил)бензил](пиридин-3-илсульфонил)аминометил}пиридин-2-иламино)ацетат или его соль.
8. Депо-композиция по п. 4, где лекарственное средство представляет собой непафенак, дексаметазон, индометацин, диклофенак натрия, левофлоксацин, INCB28050, циклоспорин А, тимолола малеат, флуоцинолона ацетонид, триамцинолона ацетонид, будесонид, олопатадин, латанопрост, изопропил-(6-{[4-(пиразол-1-ил)бензил](пиридин-3-илсульфонил)аминометил}пиридин-2-иламино)ацетат, 2-[[[2-[(гидроксиацетил)-амино]-4-пиридинил]метил]тио]-N-[4-(трифторметокси)фенил]-3-пиридинкарбоксамид или сиролимус.
9. Депо-композиция по п. 4, содержащая от 0,001 до 30% (масс./масс.) лекарственного средства.
10. Депо-композиция по п. 1, содержащая по меньшей мере 0,1% (масс./масс.) триалкилцитрата и/или ацетилтриалкилцитрата.
11. Депо-композиция по любому из пп. 1-10 для глазного местного введения.
12. Депо-композиция по п. 11 для интравитреального введения, субконъюнктивального введения или интракамерального введения.
13. Депо-композиция по любому из пп. 1-10 для предупреждения и/или лечения глазного заболевания.
14. Способ образования депо, включающий приведение жидкой композиции, содержащей триалкилцитрат и/или ацетилтриалкилцитрат, в контакт с водой, фосфатным буферным раствором, жидкостью организма или имитированной жидкостью организма,
где алкильные группы, которыми обладает каждый из триалкилцитрата и ацетилтриалкилцитрата, являются одинаковыми или разными и имеют число атомов углерода от 3 до 5.
15. Способ предупреждения и/или лечения глазного заболевания, включающий введение депо-композиции по любому из пп. 1-10 пациенту, который нуждается в предупреждении и/или лечении глазного заболевания.
16. Способ по п. 15, при котором осуществляют глазное местное введение депо-композиции.
17. Способ по п. 15 или 16, при котором депо-композицию вводят интравитреально, интракамерально или субконъюнктивально.
RU2018101473A 2015-07-01 2016-06-30 Депо-препарат, содержащий сложный эфир лимонной кислоты RU2749952C2 (ru)

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US10682340B2 (en) 2016-06-30 2020-06-16 Durect Corporation Depot formulations
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AR105215A1 (es) 2017-09-13
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