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。

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。

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。