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公开(公告)号:US20060182692A1
公开(公告)日:2006-08-17
申请号:US11344404
申请日:2006-01-30
申请人: C. Fishburn , David Lechuga-Ballesteros , Tacey Viegas , Mei-Chang Kuo , Yuan Song , Hema Gursahani , Chester Leach
发明人: C. Fishburn , David Lechuga-Ballesteros , Tacey Viegas , Mei-Chang Kuo , Yuan Song , Hema Gursahani , Chester Leach
CPC分类号: A61K9/007 , A61K31/167 , A61K31/485 , A61K47/60 , C07C41/24
摘要: Methods of modifying the rate of systemic absorption of a drug administered to a subject by a pulmonary route, the method comprising covalently conjugating a hydrophilic polymer to a drug, wherein the drug has a half-life of elimination from the lung of less than about 180 minutes, to form a drug-polymer conjugate, wherein the drug-polymer conjugate has a net hydrophilic character and a weight average molecular weight of from about 50 to about 20,000 Daltons, and wherein the half-life of elimination from the lung of the drug-polymer conjugate is at least about 1.5-fold greater than the half-life of elimination from the lung of the drug, wherein the half-life of elimination from the lung is measured by bronchoalveolar lavage followed by assaying residual lung material.
摘要翻译: 通过肺途径改变施用于受试者的药物的全身吸收速率的方法,所述方法包括将亲水性聚合物与药物共价共轭,其中所述药物具有从肺中消除的半衰期小于约180 分钟,以形成药物 - 聚合物缀合物,其中药物 - 聚合物缀合物具有净亲水特性和约50至约20,000道尔顿的重均分子量,并且其中从药物的肺中消除的半衰期 - 聚合物缀合物比从药物肺消除的半衰期大至少约1.5倍,其中通过支气管肺泡灌洗测量肺部消除的半衰期,然后测定残留的肺部材料。
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公开(公告)号:US20100210676A1
公开(公告)日:2010-08-19
申请号:US12710167
申请日:2010-02-22
申请人: C. Simone Fishburn , David Lechuga-Ballesteros , Tacey Viegas , Mei-Chang Kuo , Yuan Song , Hema Gursahani , Chester Leach
发明人: C. Simone Fishburn , David Lechuga-Ballesteros , Tacey Viegas , Mei-Chang Kuo , Yuan Song , Hema Gursahani , Chester Leach
IPC分类号: A61K31/485 , A61P25/36
CPC分类号: A61K9/007 , A61K31/167 , A61K31/485 , A61K47/60 , C07C41/24
摘要: Methods of modifying the rate of systemic absorption of a drug administered to a subject by a pulmonary route, the method comprising covalently conjugating a hydrophilic polymer to a drug, wherein the drug has a half-life of elimination from the lung of less than about 180 minutes, to form a drug-polymer conjugate, wherein the drug-polymer conjugate has a net hydrophilic character and a weight average molecular weight of from about 50 to about 20,000 Daltons, and wherein the half-life of elimination from the lung of the drug-polymer conjugate is at least about 1.5-fold greater than the half-life of elimination from the lung of the drug, wherein the half-life of elimination from the lung is measured by bronchoalveolar lavage followed by assaying residual lung material.
摘要翻译: 通过肺途径改变施用于受试者的药物的全身吸收速率的方法,所述方法包括将亲水性聚合物与药物共价共轭,其中所述药物具有从肺中消除的半衰期小于约180 分钟,以形成药物 - 聚合物缀合物,其中药物 - 聚合物缀合物具有净亲水特性和约50至约20,000道尔顿的重均分子量,并且其中从药物的肺中消除的半衰期 - 聚合物缀合物比从药物肺消除的半衰期大至少约1.5倍,其中通过支气管肺泡灌洗测量肺部消除的半衰期,然后测定残留的肺部材料。
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公开(公告)号:US20120088745A1
公开(公告)日:2012-04-12
申请号:US13271158
申请日:2011-10-11
申请人: C. Simone Fishburn , David Lechuga-Ballesteros , Tacey Viegas , Mei-Chang Kuo , Yuan Song , Hema Gursahani , Chester Leach
发明人: C. Simone Fishburn , David Lechuga-Ballesteros , Tacey Viegas , Mei-Chang Kuo , Yuan Song , Hema Gursahani , Chester Leach
IPC分类号: A61K31/16 , C07D489/08 , C07C43/13 , C07J5/00 , A61K31/573 , C07C233/21 , A61K31/485
CPC分类号: A61K9/007 , A61K31/167 , A61K31/485 , A61K47/60 , C07C41/24
摘要: Methods of modifying the rate of systemic absorption of a drug administered to a subject by a pulmonary route, the method comprising covalently conjugating a hydrophilic polymer to a drug, wherein the drug has a half-life of elimination from the lung of less than about 180 minutes, to form a drug-polymer conjugate, wherein the drug-polymer conjugate has a net hydrophilic character and a weight average molecular weight of from about 50 to about 20,000 Daltons, and wherein the half-life of elimination from the lung of the drug-polymer conjugate is at least about 1.5-fold greater than the half-life of elimination from the lung of the drug, wherein the half-life of elimination from the lung is measured by bronchoalveolar lavage followed by assaying residual lung material.
摘要翻译: 通过肺途径改变施用于受试者的药物的全身吸收速率的方法,所述方法包括将亲水性聚合物与药物共价共轭,其中所述药物具有从肺中消除的半衰期小于约180 分钟,以形成药物 - 聚合物缀合物,其中药物 - 聚合物缀合物具有净亲水特性和约50至约20,000道尔顿的重均分子量,并且其中从药物的肺中消除的半衰期 - 聚合物缀合物比从药物肺消除的半衰期大至少约1.5倍,其中通过支气管肺泡灌洗测量肺部消除的半衰期,然后测定残留的肺部材料。
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公开(公告)号:US08067431B2
公开(公告)日:2011-11-29
申请号:US12710167
申请日:2010-02-22
申请人: C. Simone Fishburn , David Lechuga-Ballesteros , Tacey Viegas , Mei-Chang Kuo , Yuan Song , Hema Gursahani , Chester Leach
发明人: C. Simone Fishburn , David Lechuga-Ballesteros , Tacey Viegas , Mei-Chang Kuo , Yuan Song , Hema Gursahani , Chester Leach
IPC分类号: A61K31/485 , C07D489/08
CPC分类号: A61K9/007 , A61K31/167 , A61K31/485 , A61K47/60 , C07C41/24
摘要: Methods of modifying the rate of systemic absorption of a drug administered to a subject by a pulmonary route, the method comprising covalently conjugating a hydrophilic polymer to a drug, wherein the drug has a half-life of elimination from the lung of less than about 180 minutes, to form a drug-polymer conjugate, wherein the drug-polymer conjugate has a net hydrophilic character and a weight average molecular weight of from about 50 to about 20,000 Daltons, and wherein the half-life of elimination from the lung of the drug-polymer conjugate is at least about 1.5-fold greater than the half-life of elimination from the lung of the drug, wherein the half-life of elimination from the lung is measured by bronchoalveolar lavage followed by assaying residual lung material.
摘要翻译: 通过肺途径改变施用于受试者的药物的全身吸收速率的方法,所述方法包括将亲水性聚合物与药物共价共轭,其中所述药物具有从肺中消除的半衰期小于约180 分钟,以形成药物 - 聚合物缀合物,其中药物 - 聚合物缀合物具有净亲水特性和约50至约20,000道尔顿的重均分子量,并且其中从药物的肺中消除的半衰期 - 聚合物缀合物比从药物肺消除的半衰期大至少约1.5倍,其中通过支气管肺泡灌洗测量肺部消除的半衰期,然后测定残留的肺部材料。
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公开(公告)号:US20050152848A1
公开(公告)日:2005-07-14
申请号:US10980652
申请日:2004-11-02
申请人: John Patton , Mei-Chang Kuo , J. Harris , Chester Leach , Kimberly Perkins , Blaine Bueche
发明人: John Patton , Mei-Chang Kuo , J. Harris , Chester Leach , Kimberly Perkins , Blaine Bueche
IPC分类号: A61K9/08 , A61K9/12 , A61K9/19 , A61K9/24 , A61K9/72 , A61K38/00 , A61K38/16 , A61K38/28 , A61K47/34 , A61K47/48 , A61L9/04 , A61P3/10 , C07K14/62 , A61K9/14
摘要: The present invention provides active, hydrophilic polymer-modified derivatives of insulin. The insulin derivatives of the invention are, in one aspect, suitable for delivery to the lung and exhibit pharmakokinetic and/or pharmacodynamic properties that are significantly improved over native insulin.
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公开(公告)号:US06838076B2
公开(公告)日:2005-01-04
申请号:US10154057
申请日:2002-05-21
申请人: John S. Patton , Mei-Chang Kuo , J. Milton Harris , Chester Leach , Kimberly Perkins , Blaine Bueche
发明人: John S. Patton , Mei-Chang Kuo , J. Milton Harris , Chester Leach , Kimberly Perkins , Blaine Bueche
IPC分类号: A61K9/08 , A61K9/12 , A61K9/19 , A61K9/24 , A61K9/72 , A61K38/00 , A61K38/16 , A61K38/28 , A61K47/34 , A61K47/48 , A61L9/04 , A61P3/10 , C07K14/62
摘要: The present invention provides active, hydrophilic polymer-modified derivatives of insulin. The insulin derivatives of the invention are, in one aspect, suitable for delivery to the lung and exhibit pharmakokinetic and/or pharmacodynamic properties that are significantly improved over native insulin.
摘要翻译: 本发明提供胰岛素的活性亲水性聚合物改性衍生物。 在一个方面,本发明的胰岛素衍生物适合于递送至肺并表现出比天然胰岛素明显改善的药物动力学和/或药效学性质。
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公开(公告)号:US06890518B2
公开(公告)日:2005-05-10
申请号:US10405190
申请日:2003-04-01
申请人: John S. Patton , Mei-Chang Kuo , J. Milton Harris , Chester Leach , Kimberly Perkins , Blaine Bueche
发明人: John S. Patton , Mei-Chang Kuo , J. Milton Harris , Chester Leach , Kimberly Perkins , Blaine Bueche
IPC分类号: A61K9/08 , A61K9/12 , A61K9/19 , A61K9/24 , A61K9/72 , A61K38/00 , A61K38/16 , A61K38/28 , A61K47/34 , A61K47/48 , A61L9/04 , A61P3/10 , C07K14/62
摘要: The present invention provides active, hydrophilic polymer-modified derivatives of insulin. The insulin derivatives of the invention are, in one aspect, suitable for delivery to the lung and exhibit pharmakokinetic and/or pharmacodynamic properties that are significantly improved over native insulin.
摘要翻译: 本发明提供胰岛素的活性亲水性聚合物改性衍生物。 在一个方面,本发明的胰岛素衍生物适合于递送至肺并表现出比天然胰岛素明显改善的药物动力学和/或药效学性质。
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