JP5552118B2 - 吸入用の新規な埋込み粒子 - Google Patents
吸入用の新規な埋込み粒子 Download PDFInfo
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- JP5552118B2 JP5552118B2 JP2011512957A JP2011512957A JP5552118B2 JP 5552118 B2 JP5552118 B2 JP 5552118B2 JP 2011512957 A JP2011512957 A JP 2011512957A JP 2011512957 A JP2011512957 A JP 2011512957A JP 5552118 B2 JP5552118 B2 JP 5552118B2
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- Prior art keywords
- lactide
- molecular weight
- polymer
- moiety
- amino
- Prior art date
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- 229920000642 polymer Polymers 0.000 claims description 60
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- 238000000034 method Methods 0.000 claims description 28
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- 238000001694 spray drying Methods 0.000 claims description 14
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- RKDVKSZUMVYZHH-UHFFFAOYSA-N 1,4-dioxane-2,5-dione Chemical group O=C1COC(=O)CO1 RKDVKSZUMVYZHH-UHFFFAOYSA-N 0.000 claims description 11
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- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 description 8
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- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 8
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- 229940123932 Phosphodiesterase 4 inhibitor Drugs 0.000 description 7
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- 229940121647 egfr inhibitor Drugs 0.000 description 7
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 7
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- CPELXLSAUQHCOX-UHFFFAOYSA-M Bromide Chemical compound [Br-] CPELXLSAUQHCOX-UHFFFAOYSA-M 0.000 description 6
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- CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical compound Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 description 6
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 description 6
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 6
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- 238000009826 distribution Methods 0.000 description 6
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- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 6
- 239000008055 phosphate buffer solution Substances 0.000 description 6
- 229940095064 tartrate Drugs 0.000 description 6
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 6
- VOVIALXJUBGFJZ-KWVAZRHASA-N Budesonide Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1C[C@H]3OC(CCC)O[C@@]3(C(=O)CO)[C@@]1(C)C[C@@H]2O VOVIALXJUBGFJZ-KWVAZRHASA-N 0.000 description 5
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 5
- 150000003842 bromide salts Chemical class 0.000 description 5
- 229960004436 budesonide Drugs 0.000 description 5
- 239000003246 corticosteroid Substances 0.000 description 5
- 150000004677 hydrates Chemical class 0.000 description 5
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 description 4
- FIMXSEMBHGTNKT-UHFFFAOYSA-N Scopine Natural products CN1C2CC(O)CC1C1C2O1 FIMXSEMBHGTNKT-UHFFFAOYSA-N 0.000 description 4
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 4
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- ODELFXJUOVNEFZ-UHFFFAOYSA-N 2,2-diphenylpropanoic acid Chemical compound C=1C=CC=CC=1C(C(O)=O)(C)C1=CC=CC=C1 ODELFXJUOVNEFZ-UHFFFAOYSA-N 0.000 description 3
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 description 3
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- DTZDZCNXNYMMOW-UHFFFAOYSA-N 9-hydroxyxanthene-9-carboxylic acid Chemical compound C1=CC=C2C(C(=O)O)(O)C3=CC=CC=C3OC2=C1 DTZDZCNXNYMMOW-UHFFFAOYSA-N 0.000 description 3
- PUPWRKQSVGUBQS-UHFFFAOYSA-N 9-methylfluorene-9-carboxylic acid Chemical compound C1=CC=C2C(C)(C(O)=O)C3=CC=CC=C3C2=C1 PUPWRKQSVGUBQS-UHFFFAOYSA-N 0.000 description 3
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 description 3
- 230000008021 deposition Effects 0.000 description 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 3
- 238000000691 measurement method Methods 0.000 description 3
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- 0 *CC(CC[N+](CCCOc1ccccc1)C1)C1OC(C(c1ccc[s]1)(c1ccc[s]1)O)=O Chemical compound *CC(CC[N+](CCCOc1ccccc1)C1)C1OC(C(c1ccc[s]1)(c1ccc[s]1)O)=O 0.000 description 2
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- ZMXHONJJTQSZKY-UHFFFAOYSA-N 2,2-bis(3,4-difluorophenyl)-2-hydroxyacetic acid Chemical compound C=1C=C(F)C(F)=CC=1C(O)(C(=O)O)C1=CC=C(F)C(F)=C1 ZMXHONJJTQSZKY-UHFFFAOYSA-N 0.000 description 2
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- YKZXWNCXGVYCKF-UHFFFAOYSA-N 2,2-bis(4-fluorophenyl)-2-hydroxyacetic acid Chemical compound C=1C=C(F)C=CC=1C(O)(C(=O)O)C1=CC=C(F)C=C1 YKZXWNCXGVYCKF-UHFFFAOYSA-N 0.000 description 2
- MAGCRYYXZYUDSY-UHFFFAOYSA-N 2-fluoro-2,2-diphenylacetic acid Chemical compound C=1C=CC=CC=1C(F)(C(=O)O)C1=CC=CC=C1 MAGCRYYXZYUDSY-UHFFFAOYSA-N 0.000 description 2
- SMNDYUVBFMFKNZ-UHFFFAOYSA-N 2-furoic acid Chemical compound OC(=O)C1=CC=CO1 SMNDYUVBFMFKNZ-UHFFFAOYSA-N 0.000 description 2
- ZMPRRFPMMJQXPP-UHFFFAOYSA-N 2-sulfobenzoic acid Chemical class OC(=O)C1=CC=CC=C1S(O)(=O)=O ZMPRRFPMMJQXPP-UHFFFAOYSA-N 0.000 description 2
- ULMFXAMQUGLVGA-LJQANCHMSA-N 3-[[2-methoxy-4-[(2-methylphenyl)sulfonylcarbamoyl]phenyl]methyl]-1-methyl-n-[(2r)-4,4,4-trifluoro-2-methylbutyl]indole-5-carboxamide Chemical compound C=1C=C(CC=2C3=CC(=CC=C3N(C)C=2)C(=O)NC[C@H](C)CC(F)(F)F)C(OC)=CC=1C(=O)NS(=O)(=O)C1=CC=CC=C1C ULMFXAMQUGLVGA-LJQANCHMSA-N 0.000 description 2
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Images
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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
-
- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
- A61K31/573—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
-
- 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
- A61K9/007—Pulmonary tract; Aromatherapy
- A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
- A61K9/0075—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
- A61K9/1647—Polyesters, e.g. poly(lactide-co-glycolide)
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Otolaryngology (AREA)
- Pulmonology (AREA)
- Emergency Medicine (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08104316 | 2008-06-09 | ||
| EP08104316.8 | 2008-06-09 | ||
| PCT/EP2009/057059 WO2009150136A1 (de) | 2008-06-09 | 2009-06-08 | Neue einbettungspartikel für die inhalation |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011522859A JP2011522859A (ja) | 2011-08-04 |
| JP2011522859A5 JP2011522859A5 (enExample) | 2014-05-29 |
| JP5552118B2 true JP5552118B2 (ja) | 2014-07-16 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011512957A Expired - Fee Related JP5552118B2 (ja) | 2008-06-09 | 2009-06-08 | 吸入用の新規な埋込み粒子 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20110311630A1 (enExample) |
| EP (1) | EP2299990A1 (enExample) |
| JP (1) | JP5552118B2 (enExample) |
| CA (1) | CA2727309A1 (enExample) |
| WO (1) | WO2009150136A1 (enExample) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA111162C2 (uk) | 2010-08-04 | 2016-04-11 | Флекшен Терап'Ютікс, Інк. | Ін'єкційна композиція ацетоніду триамцинолону для лікування болю |
| JP2014521686A (ja) * | 2011-08-04 | 2014-08-28 | フレクシオン セラピューティックス インコーポレイテッド | 関節痛の治療のためのコルチコステロイド |
| IL262720B2 (en) | 2016-05-05 | 2024-06-01 | Liquidia Tech Inc | Dry powder treprostinil for the treatment of pulmonary hypertension |
| CN109985585A (zh) * | 2019-05-13 | 2019-07-09 | 苏州岸谷纳米技术有限公司 | 一种生物降解高分子微球的快速制备方法 |
| JP7774002B2 (ja) * | 2020-05-26 | 2025-11-20 | ローズ テクノロジーズ | 鼻腔内または吸入送達のためのカンナビノイド組成物及び投薬形態 |
| CN114272228B (zh) * | 2022-01-04 | 2023-08-22 | 丽珠医药集团股份有限公司 | 噻托溴铵吸入微球及其制备方法和吸入式制剂 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2236832T3 (es) * | 1997-01-16 | 2005-07-16 | Massachusetts Institute Of Technology | Preparacion de particulas para inhalacion. |
| WO1998046212A1 (en) * | 1997-04-17 | 1998-10-22 | Amgen Inc. | Biodegradable microparticles for the sustained delivery of therapeutic drugs |
| DE19813174A1 (de) * | 1998-03-25 | 1999-05-27 | Schering Ag | Mikropartikel aus Polymeren und mindestens einer gerüstbildenden Komponente und ihre Herstellung und Verwendung in der Ultraschalldiagnostik und zur ultraschallinduzierten Wirkstofffreisetzung |
| KR100321854B1 (ko) * | 1998-12-30 | 2002-08-28 | 동국제약 주식회사 | 루테이나이징 호르몬 릴리싱 호르몬 동족체를 함유하는 장기 서방출성 미립구 및 그의 제조방법 |
| AU2001281288A1 (en) * | 2000-07-18 | 2002-01-30 | Aeropharm Technology Incorporated | Modulated release therapeutic aerosols |
| EP1556018A1 (en) * | 2002-09-30 | 2005-07-27 | Acusphere, Inc. | Sustained release porous microparticles for inhalation |
| PL2074989T3 (pl) * | 2004-02-23 | 2014-05-30 | Euro Celtique Sa | Odporne na nadużywanie transdermalne urządzenie do podawania opioidu |
| CA2574958A1 (en) * | 2004-07-26 | 2006-02-09 | Cotherix, Inc. | Treatment of pulmonary hypertension by inhaled iloprost with a microparticle formulation |
-
2009
- 2009-06-08 WO PCT/EP2009/057059 patent/WO2009150136A1/de not_active Ceased
- 2009-06-08 US US12/996,719 patent/US20110311630A1/en not_active Abandoned
- 2009-06-08 JP JP2011512957A patent/JP5552118B2/ja not_active Expired - Fee Related
- 2009-06-08 CA CA2727309A patent/CA2727309A1/en not_active Abandoned
- 2009-06-08 EP EP09761699A patent/EP2299990A1/de not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| US20110311630A1 (en) | 2011-12-22 |
| WO2009150136A1 (de) | 2009-12-17 |
| CA2727309A1 (en) | 2009-12-17 |
| EP2299990A1 (de) | 2011-03-30 |
| JP2011522859A (ja) | 2011-08-04 |
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