JP4357842B2 - 所定の吸入ルートによるアルプラゾラム、エスタゾラム、ミダゾラムまたはトリアゾラムの送出 - Google Patents
所定の吸入ルートによるアルプラゾラム、エスタゾラム、ミダゾラムまたはトリアゾラムの送出 Download PDFInfo
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- JP4357842B2 JP4357842B2 JP2002590937A JP2002590937A JP4357842B2 JP 4357842 B2 JP4357842 B2 JP 4357842B2 JP 2002590937 A JP2002590937 A JP 2002590937A JP 2002590937 A JP2002590937 A JP 2002590937A JP 4357842 B2 JP4357842 B2 JP 4357842B2
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- aerosol
- alprazolam
- therapeutic compound
- triazolam
- midazolam
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Description
[0036]所定の粒子の「空気力学的直径」は、所定の粒子と同一の沈降速度を有する1g/mLの密度(水の密度)を備えた球形の滴の直径を意味する。
[アルプラゾラム、エスタゾラム、ミダゾラムまたはトリアゾラム含有エアロゾルの形成]
[アルプラゾラム、エスタゾラム、ミダゾラムまたはトリアゾラム含有エアロゾルの送出]
[アルプラゾラム、エスタゾラム、ミダゾラムまたはトリアゾラム含有エアロゾルの投与量]
[アルプラゾラム、エスタゾラム、ミダゾラムまたはトリアゾラム含有エアロゾルの分析]
[アルプラゾラム、エスタゾラム、ミダゾラムまたはトリアゾラム含有エアロゾルの有用性]
(実施例1)
[アルプラゾラムの揮発]
(実施例2)
[エスタゾラムの揮発]
(実施例3)
[ミダゾラムの揮発]
(実施例4)
[ミダゾラムエアロゾルの粒子サイズ、粒子密度、および、吸入可能な粒子形成の速度]
(実施例6)
[トリアゾラムの揮発]
(実施例7)
[トリアゾラムエアロゾルの粒子サイズ、粒子密度、および、吸入可能な粒子形成の速度]
(実施例9)
[トリアゾラムのイヌへの送出]
Claims (21)
- アルプラゾラム、エスタゾラム、ミダゾラムおよびトリアゾラムからなる群より選ばれる治療化合物を含む、吸入療法に使用するための凝縮エアロゾルであって、
a)10重量%未満の前記治療化合物の分解生成物を含む粒子を含有し、
b)5μm未満の空気力学的質量中位径を有し、
ここで前記凝縮エアロゾルは、前記治療化合物を含む組成物を被覆した固体サポートを加熱し、前記治療化合物を蒸発させ、そして蒸気を凝縮して粒子を形成することによって形成される、凝縮エアロゾル。 - 前記蒸気の凝縮が、前記蒸気を冷却することにより行われることを含む、請求項1記載の凝縮エアロゾル。
- 前記粒子が、5重量%未満の治療化合物の分解生成物を含む、請求項1または2に記載の凝縮エアロゾル。
- 前記粒子が、2.5重量%未満の治療化合物の分解生成物を含む、請求項1または2に記載の凝縮エアロゾル。
- 少なくとも5重量%の前記治療化合物を含む、請求項1〜4のいずれか一項に記載の凝縮エアロゾル。
- 少なくとも90重量%の前記治療化合物を含む、請求項1〜4のいずれか一項に記載の凝縮エアロゾル。
- 3μm未満の空気力学的質量中位径を有する、請求項1〜6のいずれか一項に記載の凝縮エアロゾル。
- 請求項1〜7のいずれか一項に記載の凝縮エアロゾルを含む、前記治療化合物を送出するための組成物。
- 吸入療法に使用するための凝縮エアロゾルの形態である治療化合物を製造する方法であって、
a)アルプラゾラム、エスタゾラム、ミダゾラムおよびトリアゾラムからなる群より選ばれる治療化合物を、前記治療化合物の蒸気を形成するのに有効な条件下で蒸発させる工程であって、ここで前記蒸発は少なくとも5重量%の前記治療化合物を含む組成物を加熱することを含む工程と、
b)前記蒸気を凝縮させることにより、10重量%未満の治療化合物の分解生成物を含む粒子を含有し、5μm未満の空気力学的質量中位径を有する凝縮エアロゾルを形成する工程と
を含み、ここで工程a)は前記治療化合物を含む組成物を被覆した固体サポートを加熱し、前記治療化合物を蒸発させることを含む、方法。 - 工程a)が、前記治療化合物を含む組成物が上に置かれた固体サポートを加熱し、前記治療化合物を前記組成物から蒸発させることを含む、請求項9に記載の方法。
- 工程b)が、前記蒸気を冷却して前記凝縮エアロゾルを形成することを含む、請求項9または10に記載の方法。
- 前記粒子が、5重量%未満の治療化合物の分解生成物を含む、請求項9〜11のいずれか一項に記載の方法。
- 前記粒子が、2.5重量%未満の治療化合物の分解生成物を含む、請求項9〜11のいずれか一項に記載の方法。
- 前記凝縮エアロゾルが、少なくとも90重量%の前記治療化合物を含む、請求項9〜13のいずれか一項に記載の方法。
- 前記粒子が、0.5mg/秒より大きい速度で形成される、請求項9〜14のいずれか一項に記載の方法。
- 前記粒子が1mg/秒より大きい速度で形成される、請求項9〜14のいずれか一項に記載の方法。
- 前記凝縮エアロゾルが、3μm未満の空気力学的質量中位径を有する、請求項9〜16のいずれか一項に記載の方法。
- 吸入療法に使用するための治療化合物を送出するためのキットであって、
a)少なくとも5重量%のアルプラゾラム、エスタゾラム、ミダゾラムおよびトリアゾラムからなる群より選ばれる治療化合物を含む組成物と、
b)前記組成物から、前記治療化合物を含む凝縮エアロゾルを形成する装置と
を具備し、
前記装置が
1)前記治療化合物を含む組成物を被覆した固体サポートを加熱し、前記治療化合物を蒸発させて蒸気を形成する要素と、
2)前記蒸気を冷却して凝縮エアロゾルを形成する要素と、
3)前記エアロゾルを吸入するのを可能にする要素を、
を具備するキット。 - 前記凝縮エアロゾルが、請求項1〜7のいずれか一項に記載の凝縮エアロゾルである、請求項18に記載のキット。
- アルプラゾラムを含む、吸入療法に使用するための凝縮エアロゾルであって、
a)10重量%未満のアルプラゾラムの分解生成物を含む粒子を含有し、
b)5μm未満の空気力学的質量中位径を有し、
ここで前記凝縮エアロゾルは、アルプラゾラムを含む組成物を被覆した固体サポートを加熱し、アルプラゾラムを蒸発させ、そして蒸気を凝縮して粒子を形成することによって形成される、凝縮エアロゾル。 - アルプラゾラムを含む、吸入療法に使用するための凝縮エアロゾルを形成する方法であって、
a)アルプラゾラムの蒸気を形成するのに有効な条件下でアルプラゾラムを蒸発させ、ここで前記蒸発は少なくとも5重量%のアルプラゾラムを含む組成物を加熱することを含む工程と、
b)前記蒸気を凝縮させることにより10重量%未満のアルプラゾラムの分解生成物を含む粒子を含有し、5μm未満の空気力学的質量中位径を有する凝縮エアロゾルを形成する工程と、
を含み、ここで工程a)はアルプラゾラムを含む組成物を被覆した固体サポートを加熱し、アルプラゾラムを蒸発させることを含む、方法。
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2002
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- 2002-05-22 ES ES02737131T patent/ES2316571T3/es not_active Expired - Lifetime
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NZ529417A (en) | 2006-11-30 |
WO2002094218A2 (en) | 2002-11-28 |
CA2641760A1 (en) | 2002-11-28 |
US20030012738A1 (en) | 2003-01-16 |
US7018619B2 (en) | 2006-03-28 |
JP2004531555A (ja) | 2004-10-14 |
EP1392258A2 (en) | 2004-03-03 |
US7060255B2 (en) | 2006-06-13 |
US20040185003A1 (en) | 2004-09-23 |
ATE415155T1 (de) | 2008-12-15 |
US7449173B2 (en) | 2008-11-11 |
AU2002310085B2 (en) | 2008-09-04 |
US20040127490A1 (en) | 2004-07-01 |
EP1392258B1 (en) | 2008-11-26 |
CA2447519A1 (en) | 2002-11-28 |
CA2447519C (en) | 2008-09-16 |
DE60230035D1 (de) | 2009-01-08 |
WO2002094218A3 (en) | 2003-03-06 |
US6737043B2 (en) | 2004-05-18 |
US20060233718A1 (en) | 2006-10-19 |
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