JP5198716B2 - フォルモテロールおよびシクレソニドのエアロゾル製剤 - Google Patents
フォルモテロールおよびシクレソニドのエアロゾル製剤 Download PDFInfo
- Publication number
- JP5198716B2 JP5198716B2 JP2003583372A JP2003583372A JP5198716B2 JP 5198716 B2 JP5198716 B2 JP 5198716B2 JP 2003583372 A JP2003583372 A JP 2003583372A JP 2003583372 A JP2003583372 A JP 2003583372A JP 5198716 B2 JP5198716 B2 JP 5198716B2
- Authority
- JP
- Japan
- Prior art keywords
- formulation
- formoterol
- hfa
- ethanol
- aerosol
- 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.)
- Expired - Fee Related
Links
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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
-
- 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
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
-
- 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
- A61P11/08—Bronchodilators
-
- 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)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Otolaryngology (AREA)
- Pain & Pain Management (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Steroid Compounds (AREA)
Description
式(I)の化合物:
DMVインターナショナル・ファーマ(DMV International Pharma)により商品名ファーマトース(Pharmatose)325Mで市販されているα−ラクトース一水和物を、1回のパスで流体エネルギーミルによって微粉化した(これ以降、微粉化ラクトース一水和物」と呼ぶ)。シルバーソン高せん断ミキサー(Silverson high shear mixer)を使用して、微粉化ラクトース一水和物(100g)を無水エタノール(840g)に分散させた。この分散液をアヴェスティン・エマルジフレックス(Avestin Emulsiflex)C50ホモジナイザーの製造物タンクに加え、10,000psiで20分間再循環させた。20,000psiで30秒間再循環した後、次いで、この分散液をホモジナイザーから出した。以下の方法に従って粒径を決定した。
ラクトース/エタノールのスラリーを分析するため、均一性を確実にするために少なくとも1分間振盪されたスラリーの試料(0.5ml)を、イソオクタン(20ml)中の0.05%レシチン溶液に添加し、穏やかな超音波で1分間再分散させた。
5MDIユニット(各実施例の)から5つの透明プラスチックPETバイアルに製剤を冷却移動し(cold transferring)、バイアルをデクリンピング(de−crimping)し、PETバイアルに内容物を注ぎ、非定量バルブ上でクリンピング(crimping)した後に、実施例1および2の製剤の懸濁液沈降速度を比較した。透明バイアル中の製剤を室温と平衡化させた後、それらを目視評価により比較した。ここで、製剤を振盪し、次いで静置した後に、物理的特性を観察した。実施例1の製剤は、10分間の静置時間にわたり均質であるように見えたが、実施例2の製剤はこの時間に沈殿し、製剤の全体積の約30%を占める沈殿物体積を形成した。18時間静置した後、その製剤を再び調べた結果、実施例1の製剤は沈殿し、製剤体積の約1%の体積を占める沈殿物を形成したのに対して、実施例2の製剤は、製剤の全体積の約30%を占める沈殿物体積を有することが確認された。
実施例1および2のMDIユニットを、以下の条件:a)温度5℃;b)温度40℃および相対湿度75%;c)24時間の時間で4つの温度サイクルである、4℃〜40℃の温度サイクル下(1つのサイクルは以下のパス:2時間の継続時間で4℃;1時間で4〜40℃に上がり;2時間の間40℃、および1時間で40〜4℃に下がる;を有する);で10日間保存した(バルブ上向きに)。
実施例2からのMDIユニットを、バルブ上向きおよびバルブ下向きに50℃で5日間保存した(各向きに2つのユニット)。次いで、高性能液体クロマトグラフィーによって、シクレソニドに関連する不純物について試料を試験し、以下の結果を得た:
Claims (3)
- フォルモテロールの粒子またはその薬学的に許容される塩の粒子もしくは溶媒和化合物の粒子と、シクレソニドと、噴霧剤としての1,1,1,2−テトラフルオロエタン、エタノールと、を含有するエアロゾル医薬製剤であって、前記粒子が前記製剤中に懸濁されており、シクレソニドが前記製剤中に溶解されており、エタノールが前記製剤中に5〜8重量%の量で含有され、製剤が1ミクロン未満の質量中央径を有する充填剤をさらに含有するエアロゾル医薬製剤。
- ディスペンスバルブを備えたエアロゾルバイアルを含むディスペンサーであって、前記エアロゾルバイアルが請求項1に記載の製剤を含有するディスペンサー。
- 前記エアロゾルバイアルの内面が、フルオロカーボンポリマーを含有するコーティングでコートされている、請求項2に記載のディスペンサー。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GBGB0207899.6A GB0207899D0 (en) | 2002-04-05 | 2002-04-05 | Formoterol and cielesonide aerosol formulations |
GB0207899.6 | 2002-04-05 | ||
PCT/US2003/010285 WO2003086349A1 (en) | 2002-04-05 | 2003-04-01 | Formoterol and ciclesonide aerosol formulations |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2005529102A JP2005529102A (ja) | 2005-09-29 |
JP2005529102A5 JP2005529102A5 (ja) | 2006-06-01 |
JP5198716B2 true JP5198716B2 (ja) | 2013-05-15 |
Family
ID=9934322
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2003583372A Expired - Fee Related JP5198716B2 (ja) | 2002-04-05 | 2003-04-01 | フォルモテロールおよびシクレソニドのエアロゾル製剤 |
Country Status (9)
Country | Link |
---|---|
US (1) | US20050207984A1 (ja) |
EP (1) | EP1492500B1 (ja) |
JP (1) | JP5198716B2 (ja) |
AT (1) | ATE401056T1 (ja) |
AU (1) | AU2003262146A1 (ja) |
CA (1) | CA2481187A1 (ja) |
DE (1) | DE60322200D1 (ja) |
GB (1) | GB0207899D0 (ja) |
WO (1) | WO2003086349A1 (ja) |
Families Citing this family (16)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP4755495B2 (ja) * | 2002-12-12 | 2011-08-24 | ニコメッド ゲゼルシャフト ミット ベシュレンクテル ハフツング | 組合せ医薬品 |
CA2525943A1 (en) * | 2003-05-22 | 2004-12-02 | Altana Pharma Ag | Salmeterol and ciclesonide combination |
GB0312148D0 (en) | 2003-05-28 | 2003-07-02 | Aventis Pharma Ltd | Stabilized pharmaceutical products |
WO2004110460A1 (en) * | 2003-06-13 | 2004-12-23 | Altana Pharma Ag | Formoterol and ciclesonide combination |
GB0315889D0 (en) | 2003-07-08 | 2003-08-13 | Aventis Pharma Ltd | Stable pharmaceutical products |
GB0323684D0 (en) | 2003-10-09 | 2003-11-12 | Jagotec Ag | Improvements in or relating to organic compounds |
GB0323685D0 (en) * | 2003-10-09 | 2003-11-12 | Jagotec Ag | Improvements in or relating to organic compounds |
US20060045891A1 (en) * | 2004-08-24 | 2006-03-02 | Lovalenti Phillip M | Density-matched suspension vehicles and pharmaceutical suspensions |
DE102006053374A1 (de) * | 2006-02-09 | 2007-08-16 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Pharmazeutische Formulierung für Aerosole mit zwei oder mehr Wirkstoffen und mindestens einer oberflächenaktiven Substanz |
GB0918149D0 (en) | 2009-10-16 | 2009-12-02 | Jagotec Ag | Improved medicinal aerosol formulation |
WO2011084316A2 (en) * | 2009-12-16 | 2011-07-14 | 3M Innovative Properties Company | Formulations and methods for controlling mdi particle size delivery |
EP2846858B1 (de) * | 2012-05-09 | 2019-01-09 | Boehringer Ingelheim International GmbH | Zerstäuber |
WO2016018892A1 (en) | 2014-07-29 | 2016-02-04 | 3M Innovative Properties Company | Method of preparing a pharmaceutical composition |
CN109789107B (zh) * | 2016-09-29 | 2021-12-03 | 广东东阳光药业有限公司 | 药物组合物 |
US11877848B2 (en) | 2021-11-08 | 2024-01-23 | Satio, Inc. | Dermal patch for collecting a physiological sample |
US11964121B2 (en) | 2021-10-13 | 2024-04-23 | Satio, Inc. | Mono dose dermal patch for pharmaceutical delivery |
Family Cites Families (14)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5795564A (en) * | 1991-04-05 | 1998-08-18 | Sepracor, Inc. | Methods and compositions for treating pulmonary disorders using optically pure (R,R)-formoterol |
DE19541689A1 (de) * | 1994-11-14 | 1996-05-15 | Byk Gulden Lomberg Chem Fab | Kombinationsarzneimittel |
CN1217654C (zh) * | 1995-04-14 | 2005-09-07 | 史密丝克莱恩比彻姆公司 | 舒喘宁的计定剂量吸入器 |
GB9612297D0 (en) * | 1996-06-11 | 1996-08-14 | Minnesota Mining & Mfg | Medicinal aerosol formulations |
US6054488A (en) * | 1996-06-11 | 2000-04-25 | 3M Innovative Properties Company | Medicinal aerosol formulations of formoterol |
US6129905A (en) * | 1997-04-21 | 2000-10-10 | Aeropharm Technology, Inc. | Aerosol formulations containing a sugar as a dispersant |
US6120752A (en) * | 1997-05-21 | 2000-09-19 | 3M Innovative Properties Company | Medicinal aerosol products containing formulations of ciclesonide and related steroids |
DE19753301A1 (de) * | 1997-12-01 | 1999-06-02 | Basf Ag | Verfahren zur Herstellung von Lactamen |
US6264923B1 (en) * | 1998-05-13 | 2001-07-24 | 3M Innovative Properties Company | Medicinal aerosol formulation of ciclesonide and related compounds |
TR200003721T2 (tr) * | 1998-06-18 | 2001-06-21 | Boehringer Ingelheim Pharmaceuticals, Inc. | Spreyler için farmasötik formülasyonlar |
US6451285B2 (en) * | 1998-06-19 | 2002-09-17 | Baker Norton Pharmaceuticals, Inc. | Suspension aerosol formulations containing formoterol fumarate and a fluoroalkane propellant |
NZ509489A (en) * | 1998-08-04 | 2002-10-25 | Jago Res A | Medicinal aerosol formulations comprising cromoglycic acid and/or nedocromil |
US6004537A (en) * | 1998-12-18 | 1999-12-21 | Baker Norton Pharmaceuticals, Inc. | Pharmaceutical solution aerosol formulations containing fluoroalkanes, budesonide and formoterol |
HUP0302005A3 (en) * | 2000-05-23 | 2006-07-28 | Glaxo Group Ltd | Aerosol container for formulations of salmeterol xinafoate |
-
2002
- 2002-04-05 GB GBGB0207899.6A patent/GB0207899D0/en not_active Ceased
-
2003
- 2003-04-01 WO PCT/US2003/010285 patent/WO2003086349A1/en active Application Filing
- 2003-04-01 AU AU2003262146A patent/AU2003262146A1/en not_active Abandoned
- 2003-04-01 JP JP2003583372A patent/JP5198716B2/ja not_active Expired - Fee Related
- 2003-04-01 CA CA002481187A patent/CA2481187A1/en not_active Abandoned
- 2003-04-01 EP EP03746589A patent/EP1492500B1/en not_active Expired - Lifetime
- 2003-04-01 US US10/510,147 patent/US20050207984A1/en not_active Abandoned
- 2003-04-01 AT AT03746589T patent/ATE401056T1/de not_active IP Right Cessation
- 2003-04-01 DE DE60322200T patent/DE60322200D1/de not_active Expired - Lifetime
Also Published As
Publication number | Publication date |
---|---|
GB0207899D0 (en) | 2002-05-15 |
EP1492500B1 (en) | 2008-07-16 |
EP1492500A1 (en) | 2005-01-05 |
AU2003262146A1 (en) | 2003-10-27 |
JP2005529102A (ja) | 2005-09-29 |
ATE401056T1 (de) | 2008-08-15 |
DE60322200D1 (de) | 2008-08-28 |
CA2481187A1 (en) | 2003-10-23 |
US20050207984A1 (en) | 2005-09-22 |
WO2003086349A1 (en) | 2003-10-23 |
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