JP2003518484A - サルメテロールおよびプロピオン酸フルチカゾンの医薬用エアゾル製剤 - Google Patents
サルメテロールおよびプロピオン酸フルチカゾンの医薬用エアゾル製剤Info
- Publication number
- JP2003518484A JP2003518484A JP2001548088A JP2001548088A JP2003518484A JP 2003518484 A JP2003518484 A JP 2003518484A JP 2001548088 A JP2001548088 A JP 2001548088A JP 2001548088 A JP2001548088 A JP 2001548088A JP 2003518484 A JP2003518484 A JP 2003518484A
- Authority
- JP
- Japan
- Prior art keywords
- salmeterol
- formulation
- fluticasone propionate
- concentration
- propellant
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
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- 238000009472 formulation Methods 0.000 title claims abstract description 110
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- 239000008249 pharmaceutical aerosol Substances 0.000 title claims abstract description 12
- 229940021597 salmeterol and fluticasone Drugs 0.000 title description 10
- GIIZNNXWQWCKIB-UHFFFAOYSA-N Serevent Chemical compound C1=C(O)C(CO)=CC(C(O)CNCCCCCCOCCCCC=2C=CC=CC=2)=C1 GIIZNNXWQWCKIB-UHFFFAOYSA-N 0.000 claims abstract description 105
- 229960004017 salmeterol Drugs 0.000 claims abstract description 98
- 229960000289 fluticasone propionate Drugs 0.000 claims abstract description 67
- 239000003380 propellant Substances 0.000 claims abstract description 47
- 150000003839 salts Chemical class 0.000 claims abstract description 24
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- DDMOUSALMHHKOS-UHFFFAOYSA-N 1,2-dichloro-1,1,2,2-tetrafluoroethane Chemical compound FC(F)(Cl)C(F)(F)Cl DDMOUSALMHHKOS-UHFFFAOYSA-N 0.000 description 1
- 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 1
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- YCKRFDGAMUMZLT-UHFFFAOYSA-N Fluorine atom Chemical compound [F] YCKRFDGAMUMZLT-UHFFFAOYSA-N 0.000 description 1
- 230000005526 G1 to G0 transition Effects 0.000 description 1
- 101000879758 Homo sapiens Sjoegren syndrome nuclear autoantigen 1 Proteins 0.000 description 1
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- 229920000459 Nitrile rubber Polymers 0.000 description 1
- 208000007027 Oral Candidiasis Diseases 0.000 description 1
- 206010050346 Oropharyngeal candidiasis Diseases 0.000 description 1
- 229920012266 Poly(ether sulfone) PES Polymers 0.000 description 1
- 102100037330 Sjoegren syndrome nuclear autoantigen 1 Human genes 0.000 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 1
- YYAZJTUGSQOFHG-IAVNQIGZSA-N [(6s,8s,10s,11s,13s,14s,16r,17r)-6,9-difluoro-17-(fluoromethylsulfanylcarbonyl)-11-hydroxy-10,13,16-trimethyl-3-oxo-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-17-yl] propanoate;2-(hydroxymethyl)-4-[1-hydroxy-2-[6-(4-phenylbutoxy)hexylamino]eth Chemical compound C1=C(O)C(CO)=CC(C(O)CNCCCCCCOCCCCC=2C=CC=CC=2)=C1.C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)C1(F)[C@@H]2[C@@H]2C[C@@H](C)[C@@](C(=O)SCF)(OC(=O)CC)[C@@]2(C)C[C@@H]1O YYAZJTUGSQOFHG-IAVNQIGZSA-N 0.000 description 1
- JAWMENYCRQKKJY-UHFFFAOYSA-N [3-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-ylmethyl)-1-oxa-2,8-diazaspiro[4.5]dec-2-en-8-yl]-[2-[[3-(trifluoromethoxy)phenyl]methylamino]pyrimidin-5-yl]methanone Chemical compound N1N=NC=2CN(CCC=21)CC1=NOC2(C1)CCN(CC2)C(=O)C=1C=NC(=NC=1)NCC1=CC(=CC=C1)OC(F)(F)F JAWMENYCRQKKJY-UHFFFAOYSA-N 0.000 description 1
- UOKUTYNLQFNOEV-UHFFFAOYSA-N [5-(hydroxymethyl)-5-[[6-(4-phenylbutoxy)hexylamino]methyl]cyclohexa-1,3-dien-1-yl]methanol Chemical compound C1C(CO)=CC=CC1(CO)CNCCCCCCOCCCCC1=CC=CC=C1 UOKUTYNLQFNOEV-UHFFFAOYSA-N 0.000 description 1
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- NKDDWNXOKDWJAK-UHFFFAOYSA-N dimethoxymethane Chemical compound COCOC NKDDWNXOKDWJAK-UHFFFAOYSA-N 0.000 description 1
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- HQQADJVZYDDRJT-UHFFFAOYSA-N ethene;prop-1-ene Chemical group C=C.CC=C HQQADJVZYDDRJT-UHFFFAOYSA-N 0.000 description 1
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- 229910052731 fluorine Inorganic materials 0.000 description 1
- 239000011737 fluorine Substances 0.000 description 1
- 229960002714 fluticasone Drugs 0.000 description 1
- MGNNYOODZCAHBA-GQKYHHCASA-N fluticasone Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@@H](C)[C@@](C(=O)SCF)(O)[C@@]2(C)C[C@@H]1O MGNNYOODZCAHBA-GQKYHHCASA-N 0.000 description 1
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- UORVCLMRJXCDCP-UHFFFAOYSA-N propynoic acid Chemical compound OC(=O)C#C UORVCLMRJXCDCP-UHFFFAOYSA-N 0.000 description 1
- 238000001953 recrystallisation Methods 0.000 description 1
- 238000012429 release testing Methods 0.000 description 1
- QEVHRUUCFGRFIF-MDEJGZGSSA-N reserpine Chemical compound O([C@H]1[C@@H]([C@H]([C@H]2C[C@@H]3C4=C(C5=CC=C(OC)C=C5N4)CCN3C[C@H]2C1)C(=O)OC)OC)C(=O)C1=CC(OC)=C(OC)C(OC)=C1 QEVHRUUCFGRFIF-MDEJGZGSSA-N 0.000 description 1
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Classifications
-
- 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
- A61K9/008—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI]
-
- 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
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Pulmonology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Otolaryngology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB9930878.5A GB9930878D0 (en) | 1999-12-24 | 1999-12-24 | Pharmaceutical formulation |
| GB9930878.5 | 1999-12-24 | ||
| GB0018686.6 | 2000-07-28 | ||
| GB0018686A GB0018686D0 (en) | 2000-07-28 | 2000-07-28 | Pharmaceutical formulation |
| PCT/GB2000/004939 WO2001047493A1 (en) | 1999-12-24 | 2000-12-21 | Pharmaceutical aerosol formulation of salmeterol and fluticasone propionate |
Publications (2)
| Publication Number | Publication Date |
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| JP2003518484A true JP2003518484A (ja) | 2003-06-10 |
| JP2003518484A5 JP2003518484A5 (enExample) | 2007-12-27 |
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| Country | Link |
|---|---|
| US (1) | US20030032632A1 (enExample) |
| EP (1) | EP1248597B1 (enExample) |
| JP (1) | JP2003518484A (enExample) |
| AT (1) | ATE291898T1 (enExample) |
| AU (1) | AU2206801A (enExample) |
| DE (1) | DE60019167T2 (enExample) |
| ES (1) | ES2238334T3 (enExample) |
| WO (1) | WO2001047493A1 (enExample) |
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| JP2004529108A (ja) * | 2001-03-07 | 2004-09-24 | グラクソ グループ リミテッド | R−サルメテロールおよびプロピオン酸フルチカゾンを含んでなる医薬製剤 |
| KR20170035919A (ko) * | 2014-06-25 | 2017-03-31 | 옵티노즈 에이에스 | 코 투여 |
| JP2019529427A (ja) * | 2016-09-19 | 2019-10-17 | メキシケム フロー エセ・ア・デ・セ・ヴェ | 医薬組成物 |
| US11554229B2 (en) | 2013-03-26 | 2023-01-17 | OptiNose Inc. | Nasal administration |
| JP2023519199A (ja) * | 2020-03-25 | 2023-05-10 | インスメッド インコーポレイテッド | トレプロスチニルプロドラッグの医薬製剤及びその使用方法 |
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| IT1313553B1 (it) | 1999-07-23 | 2002-09-09 | Chiesi Farma Spa | Formulazioni ottimizzate costituite da soluzioni di steroidi dasomministrare per inalazione. |
| WO2001037805A1 (en) * | 1999-11-23 | 2001-05-31 | Glaxo Group Limited | Pharmaceutical formulations of salmeterol |
| US20050048001A1 (en) * | 1999-11-23 | 2005-03-03 | Cripps Alan Leslie | Pharmaceutical formulations of salmeterol |
| IT1317846B1 (it) | 2000-02-22 | 2003-07-15 | Chiesi Farma Spa | Formulazioni contenenti un farmaco anticolinergico per il trattamentodella broncopneumopatia cronica ostruttiva. |
| US20060257324A1 (en) | 2000-05-22 | 2006-11-16 | Chiesi Farmaceutici S.P.A. | Pharmaceutical solution formulations for pressurised metered dose inhalers |
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| GB2367011A (en) * | 2000-08-26 | 2002-03-27 | Glaxo Group Ltd | Metered dose inhaler for salmeterol |
| AR030516A1 (es) * | 2000-08-31 | 2003-08-20 | Glaxo Group Ltd | Uso de una combinacion de salmeterol y fluticasona |
| GB0021927D0 (en) * | 2000-09-07 | 2000-10-25 | Glaxo Group Ltd | Use of pharmaceutical combination |
| GB0106031D0 (en) * | 2001-03-12 | 2001-05-02 | Glaxo Group Ltd | Use |
| US7482366B2 (en) | 2001-12-21 | 2009-01-27 | X-Ceptor Therapeutics, Inc. | Modulators of LXR |
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| EP1415647A1 (en) * | 2002-10-23 | 2004-05-06 | CHIESI FARMACEUTICI S.p.A. | "Long-acting beta-2 agonists ultrafine formulations" |
| CA2495875C (en) * | 2002-08-27 | 2010-06-22 | Schering Corporation | Process for producing metered dose inhaler formulations |
| EP1595531A1 (en) | 2004-05-13 | 2005-11-16 | CHIESI FARMACEUTICI S.p.A. | Stable pharmaceutical solution formulations for pressurized metered dose inhalers |
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| WO2011145109A1 (en) * | 2010-05-20 | 2011-11-24 | Sun Pharma Advanced Research Company Ltd., | Dry powder inhalation composition |
| TWI399202B (zh) * | 2011-03-17 | 2013-06-21 | Intech Biopharm Ltd | 製備用於治療呼吸道疾病之定量噴霧吸入劑的製程方法 |
| US9241904B1 (en) | 2011-08-19 | 2016-01-26 | Intech Biopharm Ltd. | Method for preparing metered dose sprayed inhaler for treating respiratory disease |
| CN102379846B (zh) * | 2011-10-21 | 2014-07-02 | 江苏长风药业有限公司 | 以氢氟烷烃和聚乙二醇为辅料氟替卡松丙酸酯气雾剂制剂 |
| JP6285419B2 (ja) | 2012-05-08 | 2018-02-28 | ニコックス アフサァルミィクス、 インコーポレイテッドNicox Ophthalmics, Inc. | 疎水性治療剤の調製物、製造方法およびその使用 |
| US8765725B2 (en) | 2012-05-08 | 2014-07-01 | Aciex Therapeutics, Inc. | Preparations of hydrophobic therapeutic agents, methods of manufacture and use thereof |
| US9815865B2 (en) | 2013-01-07 | 2017-11-14 | Nicox Ophthalmics, Inc. | Preparations of hydrophobic therapeutic agents, methods of manufacture and use thereof |
| WO2016018892A1 (en) | 2014-07-29 | 2016-02-04 | 3M Innovative Properties Company | Method of preparing a pharmaceutical composition |
| CN114712338A (zh) | 2016-09-19 | 2022-07-08 | 墨西哥氟石股份公司 | 药物组合物 |
| ES2891579T3 (es) | 2016-09-19 | 2022-01-28 | Mexichem Fluor Sa De Cv | Composición farmacéutica |
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- 2000-12-21 AU AU22068/01A patent/AU2206801A/en not_active Abandoned
- 2000-12-21 AT AT00985666T patent/ATE291898T1/de not_active IP Right Cessation
- 2000-12-21 US US10/168,672 patent/US20030032632A1/en not_active Abandoned
- 2000-12-21 EP EP00985666A patent/EP1248597B1/en not_active Expired - Lifetime
- 2000-12-21 ES ES00985666T patent/ES2238334T3/es not_active Expired - Lifetime
- 2000-12-21 JP JP2001548088A patent/JP2003518484A/ja active Pending
- 2000-12-21 WO PCT/GB2000/004939 patent/WO2001047493A1/en not_active Ceased
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Cited By (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2004529108A (ja) * | 2001-03-07 | 2004-09-24 | グラクソ グループ リミテッド | R−サルメテロールおよびプロピオン酸フルチカゾンを含んでなる医薬製剤 |
| US11554229B2 (en) | 2013-03-26 | 2023-01-17 | OptiNose Inc. | Nasal administration |
| KR20170035919A (ko) * | 2014-06-25 | 2017-03-31 | 옵티노즈 에이에스 | 코 투여 |
| JP2017520364A (ja) * | 2014-06-25 | 2017-07-27 | オプティノーズ アズ | 経鼻投与 |
| JP2020179191A (ja) * | 2014-06-25 | 2020-11-05 | オプティノーズ アズ | 経鼻投与 |
| JP7090124B2 (ja) | 2014-06-25 | 2022-06-23 | オプティノーズ アズ | 経鼻投与 |
| KR102458964B1 (ko) | 2014-06-25 | 2022-10-25 | 옵티노즈, 인크. | 코 투여 |
| JP2019529427A (ja) * | 2016-09-19 | 2019-10-17 | メキシケム フロー エセ・ア・デ・セ・ヴェ | 医薬組成物 |
| JP2023519199A (ja) * | 2020-03-25 | 2023-05-10 | インスメッド インコーポレイテッド | トレプロスチニルプロドラッグの医薬製剤及びその使用方法 |
Also Published As
| Publication number | Publication date |
|---|---|
| DE60019167D1 (de) | 2005-05-04 |
| ES2238334T3 (es) | 2005-09-01 |
| DE60019167T2 (de) | 2006-05-11 |
| EP1248597B1 (en) | 2005-03-30 |
| EP1248597A1 (en) | 2002-10-16 |
| WO2001047493A1 (en) | 2001-07-05 |
| AU2206801A (en) | 2001-07-09 |
| ATE291898T1 (de) | 2005-04-15 |
| US20030032632A1 (en) | 2003-02-13 |
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