RU2007128812A - Препараты производных азетидина для инъекций или перорального введения - Google Patents
Препараты производных азетидина для инъекций или перорального введения Download PDFInfo
- Publication number
- RU2007128812A RU2007128812A RU2007128812/15A RU2007128812A RU2007128812A RU 2007128812 A RU2007128812 A RU 2007128812A RU 2007128812/15 A RU2007128812/15 A RU 2007128812/15A RU 2007128812 A RU2007128812 A RU 2007128812A RU 2007128812 A RU2007128812 A RU 2007128812A
- Authority
- RU
- Russia
- Prior art keywords
- pharmaceutical composition
- injection
- solutol
- peg
- solvent
- Prior art date
Links
- 238000002347 injection Methods 0.000 title claims 6
- 239000007924 injection Substances 0.000 title claims 6
- HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical class C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 11
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims 9
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 6
- 239000013543 active substance Substances 0.000 claims 4
- 239000006184 cosolvent Substances 0.000 claims 4
- JVKUCNQGESRUCL-UHFFFAOYSA-N 2-Hydroxyethyl 12-hydroxyoctadecanoate Chemical compound CCCCCCC(O)CCCCCCCCCCC(=O)OCCO JVKUCNQGESRUCL-UHFFFAOYSA-N 0.000 claims 3
- SHBUUTHKGIVMJT-UHFFFAOYSA-N Hydroxystearate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OO SHBUUTHKGIVMJT-UHFFFAOYSA-N 0.000 claims 3
- 229920001304 Solutol HS 15 Polymers 0.000 claims 3
- 229940072106 hydroxystearate Drugs 0.000 claims 3
- 229920001223 polyethylene glycol Polymers 0.000 claims 3
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 claims 3
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims 3
- 229920000053 polysorbate 80 Polymers 0.000 claims 3
- 229940068968 polysorbate 80 Drugs 0.000 claims 3
- 125000004211 3,5-difluorophenyl group Chemical group [H]C1=C(F)C([H])=C(*)C([H])=C1F 0.000 claims 2
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 2
- 229920002565 Polyethylene Glycol 400 Polymers 0.000 claims 2
- 125000004567 azetidin-3-yl group Chemical group N1CC(C1)* 0.000 claims 2
- 239000008103 glucose Substances 0.000 claims 2
- HNQIVZYLYMDVSB-UHFFFAOYSA-N methanesulfonimidic acid Chemical compound CS(N)(=O)=O HNQIVZYLYMDVSB-UHFFFAOYSA-N 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 239000000243 solution Substances 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 229910002056 binary alloy Inorganic materials 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 239000004094 surface-active agent Substances 0.000 claims 1
Classifications
-
- 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
- A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
-
- 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
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- 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
- 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
- A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
-
- 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
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
-
- 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
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Dermatology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Plural Heterocyclic Compounds (AREA)
Claims (8)
1. Фармацевтическая композиция для инъекций, отличающаяся тем, что она представляет собой систему, содержащую действующее вещество формулы (Ia) или (Ib)
в которых Ar представляет собой ароматическую или гетероароматическую группу, замещенную при необходимости одним или несколькими заместителями, такими, как (C1-C4)алкил, галоген, NO2, CN, (C1-C4)алкокси или OH, и в качестве эксципиента Polysorbate 80 (моноолеат POE) или Solutol HS15 (гидроксистеарат PEG), и при необходимости в качестве сорастворителя этанол, PEG 400 или пропиленгликоль.
2. Фармацевтическая композиция для инъекций, отличающаяся тем, что она представляет собой бинарную систему, содержащую в качестве действующего вещества N-{1-[бис-(4-хлорфенил)метил]азетидин-3-ил}-N-(3,5-дифторфенил)метилсульфонамид и в качестве эксципиента Polysorbate 80 (моноолеат POE) или Solutol HS15 (гидроксистеарат PEG).
3. Фармацевтическая композиция для инъекций, отличающаяся тем, что она представляет собой тернарную систему, содержащую в качестве действующего вещества N-{1-[бис-(4-хлорфенил)метил]азетидин-3-ил}-N-(3,5-дифторфенил)метилсульфонамид, в качестве поверхностно-активного вещества Polysorbate 80 (моноолеат POE) или Solutol HS15 (гидроксистеарат PEG) и в качестве сорастворителя этанол, PEG 400 или пропиленгликоль.
4. Фармацевтическая композиция для инъекций по пп.1, 2 или 3, отличающаяся тем, что содержание действующего вещества составляет от 0,01 до 60 мас.% по отношению к общей массе фармацевтической композиции.
5. Фармацевтическая композиция для инъекций по п.1 или 3, отличающаяся тем, что содержание сорастворителя составляет от 1 до 70 мас.% по отношению к общей массе фармацевтической композиции.
6. Фармацевтическая композиция для введения перорально по п.5, отличающаяся тем, что содержание сорастворителя составляет от 20 до 40 мас.% по отношению к общей массе фармацевтической композиции.
7. Фармацевтическая композиция по п.2, отличающаяся тем, что в ней соотношение Solutol/этанол составляет 80/20 в 5%-ном растворе глюкозы.
8. Фармацевтическая композиция по п.2, отличающаяся тем, что в ней соотношение Solutol/пропиленгликоль составляет 70/30 в 5%-ном растворе глюкозы.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR0413937 | 2004-12-27 | ||
| FR0413937A FR2879932B1 (fr) | 2004-12-27 | 2004-12-27 | Formulations injectable ou administrable par voie orale de derives d'azetidine |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2007128812A true RU2007128812A (ru) | 2009-02-10 |
Family
ID=34952941
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2007128812/15A RU2007128812A (ru) | 2004-12-27 | 2005-12-23 | Препараты производных азетидина для инъекций или перорального введения |
Country Status (20)
| Country | Link |
|---|---|
| US (2) | US20070244085A1 (ru) |
| EP (1) | EP1835906A1 (ru) |
| JP (1) | JP2008525390A (ru) |
| KR (1) | KR20070092970A (ru) |
| CN (1) | CN101090719A (ru) |
| AR (1) | AR052181A1 (ru) |
| AU (1) | AU2005321112A1 (ru) |
| BR (1) | BRPI0519271A2 (ru) |
| CA (1) | CA2586895A1 (ru) |
| FR (1) | FR2879932B1 (ru) |
| GT (1) | GT200500387A (ru) |
| IL (1) | IL183483A0 (ru) |
| MX (1) | MX2007006926A (ru) |
| PA (1) | PA8658201A1 (ru) |
| PE (1) | PE20060743A1 (ru) |
| RU (1) | RU2007128812A (ru) |
| SV (1) | SV2006002355A (ru) |
| TW (1) | TW200635581A (ru) |
| UY (1) | UY29318A1 (ru) |
| WO (1) | WO2006070129A1 (ru) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20110056516A (ko) * | 2008-09-12 | 2011-05-30 | 크리티컬 파머수티컬스 리미티드 | 점막 또는 피부를 통한 치료제의 흡수 개선 |
| FR2948568B1 (fr) * | 2009-07-30 | 2012-08-24 | Sanofi Aventis | Formulation pharmaceutique |
| WO2016164770A1 (en) | 2015-04-10 | 2016-10-13 | Bioresponse, L.L.C. | Self-emulsifying formulations of dim-related indoles |
| US11471437B2 (en) | 2019-06-18 | 2022-10-18 | Opiant Pharmaceuticals, Inc. | Compositions and methods for treating cannabinoid hyperemesis syndrome with a cannabinoid receptor antagonist |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR0177158B1 (ko) * | 1990-03-01 | 1999-03-20 | 후지사와 도모기찌로 | 면역억제 활성을 갖는 트리사이클릭 화합물 함유 용액 제제 |
| US5516770A (en) * | 1993-09-30 | 1996-05-14 | American Home Products Corporation | Rapamycin formulation for IV injection |
| WO2000071163A1 (en) * | 1999-05-24 | 2000-11-30 | Sonus Pharmaceuticals, Inc. | Emulsion vehicle for poorly soluble drugs |
| FR2833842B1 (fr) * | 2001-12-21 | 2004-02-13 | Aventis Pharma Sa | Compositions pharmaceutiques a base de derives d'azetidine |
-
2004
- 2004-12-27 FR FR0413937A patent/FR2879932B1/fr not_active Expired - Fee Related
-
2005
- 2005-12-14 PE PE2005001449A patent/PE20060743A1/es not_active Application Discontinuation
- 2005-12-22 SV SV2005002355A patent/SV2006002355A/es unknown
- 2005-12-22 GT GT200500387A patent/GT200500387A/es unknown
- 2005-12-22 AR ARP050105502A patent/AR052181A1/es not_active Application Discontinuation
- 2005-12-22 PA PA20058658201A patent/PA8658201A1/es unknown
- 2005-12-23 EP EP05850602A patent/EP1835906A1/fr not_active Withdrawn
- 2005-12-23 CN CNA2005800450089A patent/CN101090719A/zh active Pending
- 2005-12-23 AU AU2005321112A patent/AU2005321112A1/en not_active Abandoned
- 2005-12-23 JP JP2007547578A patent/JP2008525390A/ja active Pending
- 2005-12-23 KR KR1020077014546A patent/KR20070092970A/ko not_active Withdrawn
- 2005-12-23 BR BRPI0519271-4A patent/BRPI0519271A2/pt not_active Application Discontinuation
- 2005-12-23 RU RU2007128812/15A patent/RU2007128812A/ru not_active Application Discontinuation
- 2005-12-23 WO PCT/FR2005/003263 patent/WO2006070129A1/fr not_active Ceased
- 2005-12-23 CA CA002586895A patent/CA2586895A1/fr not_active Abandoned
- 2005-12-23 MX MX2007006926A patent/MX2007006926A/es unknown
- 2005-12-26 TW TW094146437A patent/TW200635581A/zh unknown
- 2005-12-27 UY UY29318A patent/UY29318A1/es unknown
-
2007
- 2007-05-28 IL IL183483A patent/IL183483A0/en unknown
- 2007-05-29 US US11/754,569 patent/US20070244085A1/en not_active Abandoned
-
2009
- 2009-10-05 US US12/573,465 patent/US20100022501A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| CA2586895A1 (fr) | 2006-07-06 |
| US20070244085A1 (en) | 2007-10-18 |
| IL183483A0 (en) | 2007-09-20 |
| PE20060743A1 (es) | 2006-09-13 |
| SV2006002355A (es) | 2006-06-28 |
| EP1835906A1 (fr) | 2007-09-26 |
| TW200635581A (en) | 2006-10-16 |
| AR052181A1 (es) | 2007-03-07 |
| GT200500387A (es) | 2006-07-03 |
| US20100022501A1 (en) | 2010-01-28 |
| KR20070092970A (ko) | 2007-09-14 |
| AU2005321112A1 (en) | 2006-07-06 |
| PA8658201A1 (es) | 2006-08-03 |
| CN101090719A (zh) | 2007-12-19 |
| BRPI0519271A2 (pt) | 2009-01-06 |
| UY29318A1 (es) | 2006-07-31 |
| FR2879932B1 (fr) | 2007-03-23 |
| MX2007006926A (es) | 2007-08-06 |
| JP2008525390A (ja) | 2008-07-17 |
| WO2006070129A1 (fr) | 2006-07-06 |
| FR2879932A1 (fr) | 2006-06-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20090317 |