RU2018119121A - Лекарственные формы местных анастетиков с замедленным высвобождением - Google Patents
Лекарственные формы местных анастетиков с замедленным высвобождением Download PDFInfo
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- RU2018119121A RU2018119121A RU2018119121A RU2018119121A RU2018119121A RU 2018119121 A RU2018119121 A RU 2018119121A RU 2018119121 A RU2018119121 A RU 2018119121A RU 2018119121 A RU2018119121 A RU 2018119121A RU 2018119121 A RU2018119121 A RU 2018119121A
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- pharmaceutical composition
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- local anesthetic
- pva coating
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5005—Wall or coating material
- A61K9/5021—Organic macromolecular compounds
- A61K9/5026—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
- A61K9/0024—Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0085—Brain, e.g. brain implants; Spinal cord
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5089—Processes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P23/00—Anaesthetics
- A61P23/02—Local anaesthetics
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Anesthesiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Dermatology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Psychology (AREA)
- Neurology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (23)
1. Фармацевтическая композиция, содержащая:
множество микрочастиц, каждая микрочастица включает:
один или несколько кристаллов местного анестетика; а также
покрытие из поливинилового спирта (PVA), полностью инкапсулирующее один или несколько кристаллов, где PVA-покрытие гидролизуется не менее 85% и составляет около 1-30 мас.% микрочастицы, и где один или несколько кристаллов местного анестетика составляют около 70-99 мас.% микрочастицы, и каждый из них имеет по меньшей мере один размер в диапазоне 35-500 мкм.
2. Фармацевтическая композиция по п. 1, где PVA-покрытие является по меньшей мере на 99% гидролизованным.
3. Фармацевтическая композиция по любому из пп. 1-2, где PVA-покрытие является сшитым.
4. Фармацевтическая композиция по любому из пп. 1-3, где PVA-покрытие термически отверждается и физически сшивается.
5. Фармацевтическая композиция по п. 4, где термическое отверждение происходит при 100-135°С в течение 2-8 ч.
6. Фармацевтическая композиция по любому из пп. 1-3, где PVA-покрытие химически сшивается в присутствии сшивающего агента.
7. Фармацевтическая композиция по п. 6, где PVA-покрытие содержит менее 5 мас.% сшивающего агента.
8. Фармацевтическая композиция по п. 6 или 7, где сшивающий агент представляет собой лимонную кислоту.
9. Фармацевтическая композиция по любому из пп. 1-8, где PVA-покрытие имеет молекулярную массу 2-200 кДа.
10. Фармацевтическая композиция по п. 9, где PVA-покрытие имеет молекулярную массу 140-190 кДа.
11. Фармацевтическая композиция по любому из пп. 1-10, где местный анестетик имеет скорость растворения по меньшей мере в 5 раз медленнее, чем у местного анестетика, когда он не покрыт оболочкой, в той же среде растворения.
12. Фармацевтическая композиция по любому из пп. 1-10, где местный анестетик имеет скорость растворения по меньшей мере в 7 раз медленнее, чем у местного анестетика, когда он не покрыт оболочкой, в той же среде растворения.
13. Фармацевтическая композиция по любому из пп. 1-10, где местный анестетик имеет скорость растворения по меньшей мере в 10 раз медленнее, чем у местного анестетика, когда он не покрыт оболочкой, в той же среде растворения.
14. Фармацевтическая композиция по любому из пп. 1-13, где местный анестетик представляет собой аминоамидное лекарственное средство.
15. Фармацевтическая композиция по любому из пп. 1-14, где местный анестетик содержит более одного кристалла, связанного терапевтически неактивным агентом.
16. Фармацевтическая композиция по любому из пп. 1-15, где местным анестетиком является ропивакаин.
17. Применение фармацевтической композиции по любому из пп. 1-16 для лечения послеоперационной боли на месте раны.
18. Применение фармацевтической композиции по п. 17, где местный анестетик проявляет замедленное высвобождение в течение 3-5 д после операции.
19. Способ коррекции послеоперационной боли на месте раны пациента, нуждающегося в этом, включающий введение в место раны терапевтически эффективного количества фармацевтической композиции по любому из пп. 1-16.
20. Способ коррекции послеоперационной боли на месте раны пациента, нуждающегося в этом, включающий введение лекарственной формы для инъекций в фасцию периферического нерва или в область, окружающую фасцию периферического нерв, терапевтически эффективного количества фармацевтической композиции любого из пп. 1-16.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562247159P | 2015-10-27 | 2015-10-27 | |
| US62/247,159 | 2015-10-27 | ||
| PCT/US2016/059141 WO2017075232A1 (en) | 2015-10-27 | 2016-10-27 | Sustained release formulations of local anesthetics |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2018119121A true RU2018119121A (ru) | 2019-11-28 |
| RU2018119121A3 RU2018119121A3 (ru) | 2020-03-10 |
Family
ID=57249923
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2018119121A RU2018119121A (ru) | 2015-10-27 | 2016-10-27 | Лекарственные формы местных анастетиков с замедленным высвобождением |
Country Status (20)
| Country | Link |
|---|---|
| US (2) | US11351124B2 (ru) |
| EP (1) | EP3206672B1 (ru) |
| JP (1) | JP2018531951A (ru) |
| KR (1) | KR20180069055A (ru) |
| CN (1) | CN108289857A (ru) |
| AU (1) | AU2016343952A1 (ru) |
| BR (1) | BR112018008415A2 (ru) |
| CA (1) | CA3003159A1 (ru) |
| CL (1) | CL2018001098A1 (ru) |
| DK (1) | DK3206672T3 (ru) |
| ES (1) | ES2672993T3 (ru) |
| IL (1) | IL258852A (ru) |
| MX (1) | MX2018005035A (ru) |
| PL (1) | PL3206672T3 (ru) |
| PT (1) | PT3206672T (ru) |
| RU (1) | RU2018119121A (ru) |
| SG (1) | SG11201803156TA (ru) |
| TR (1) | TR201808237T4 (ru) |
| TW (1) | TW201720427A (ru) |
| WO (1) | WO2017075232A1 (ru) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201505527D0 (en) | 2015-03-31 | 2015-05-13 | Jmedtech Pte Ltd | Composition |
| ES2672993T3 (es) * | 2015-10-27 | 2018-06-19 | Eupraxia Pharmaceuticals Inc. | Formulaciones de liberación sostenida de anestésicos locales |
| CA3078555A1 (en) | 2017-10-06 | 2019-04-11 | Foundry Therapeutics, Inc. | Implantable depots for the controlled release of therapeutic agents |
| WO2020210720A1 (en) * | 2019-04-10 | 2020-10-15 | Eupraxia Pharmaceuticals Inc. | Process for making drug crystals of desired size distribution and morphology |
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- 2016-10-27 ES ES16791778.0T patent/ES2672993T3/es active Active
- 2016-10-27 RU RU2018119121A patent/RU2018119121A/ru not_active Application Discontinuation
- 2016-10-27 WO PCT/US2016/059141 patent/WO2017075232A1/en active Application Filing
- 2016-10-27 CA CA3003159A patent/CA3003159A1/en not_active Abandoned
- 2016-10-27 JP JP2018520592A patent/JP2018531951A/ja active Pending
- 2016-10-27 CN CN201680062982.4A patent/CN108289857A/zh active Pending
- 2016-10-27 SG SG11201803156TA patent/SG11201803156TA/en unknown
- 2016-10-27 TW TW105134859A patent/TW201720427A/zh unknown
- 2016-10-27 TR TR2018/08237T patent/TR201808237T4/tr unknown
- 2016-10-27 BR BR112018008415A patent/BR112018008415A2/pt not_active Application Discontinuation
- 2016-10-27 PT PT167917780T patent/PT3206672T/pt unknown
- 2016-10-27 KR KR1020187014599A patent/KR20180069055A/ko unknown
- 2016-10-27 MX MX2018005035A patent/MX2018005035A/es unknown
- 2016-10-27 EP EP16791778.0A patent/EP3206672B1/en active Active
- 2016-10-27 US US15/770,414 patent/US11351124B2/en active Active
- 2016-10-27 PL PL16791778T patent/PL3206672T3/pl unknown
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| Publication number | Publication date |
|---|---|
| EP3206672B1 (en) | 2018-03-14 |
| RU2018119121A3 (ru) | 2020-03-10 |
| TW201720427A (zh) | 2017-06-16 |
| MX2018005035A (es) | 2018-09-06 |
| CN108289857A (zh) | 2018-07-17 |
| TR201808237T4 (tr) | 2018-07-23 |
| SG11201803156TA (en) | 2018-05-30 |
| BR112018008415A2 (pt) | 2018-10-30 |
| PL3206672T3 (pl) | 2018-09-28 |
| DK3206672T3 (en) | 2018-06-18 |
| US20230089355A1 (en) | 2023-03-23 |
| CA3003159A1 (en) | 2017-05-04 |
| ES2672993T3 (es) | 2018-06-19 |
| PT3206672T (pt) | 2018-06-20 |
| US11351124B2 (en) | 2022-06-07 |
| EP3206672A1 (en) | 2017-08-23 |
| IL258852A (en) | 2018-06-28 |
| KR20180069055A (ko) | 2018-06-22 |
| JP2018531951A (ja) | 2018-11-01 |
| WO2017075232A1 (en) | 2017-05-04 |
| US20180311173A1 (en) | 2018-11-01 |
| CL2018001098A1 (es) | 2018-06-15 |
| AU2016343952A1 (en) | 2018-05-10 |
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