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1. 发明授权

EP0950403B1 Emulsions for in-situ delivery systems 有权
标题翻译：乳液原位药物输送系统
公开(公告)号：EP0950403B1
公开(公告)日：2006-07-05
申请号：EP99107131.7
申请日：1999-04-13
申请人： QLT USA, Inc.
发明人： Dunn, Richard L.
IPC分类号： A61K9/06
CPC分类号： A61K9/0024 , Y02A50/465
摘要： The invention is provides a composition for sustained delivery of a biologically active agent comprising a biologically active mixture and a controlled release formulation. The composition protects the biologically active agent from being destroyed by the controlled release composition. The biologically active mixture includes the biologically active agent and a pharmaceutically acceptable protective carrier. The controlled release formulation includes a pharmaceutically acceptable, biodegradable, matrix forming material that is substantially insoluble in aqueous or body fluids and a pharmaceutically acceptable organic solvent. The biologically active mixture is combined with the controlled release formulation to form an emulsion, the delivery composition, which is then administered to a patient. The protective carrier can be an aqueous substance, a non-aqueous substance or a combination of both. The matrix forming material can be a polymeric material, a non-polymeric material or a combination of both. The organic solvent can have a solubility ranging from a high water solubility to a low water solubility.

2. 发明授权

EP1125577B1 Liquid drug delivery compositions 失效
标题翻译：用于药物递送的液体组合物
公开(公告)号：EP1125577B1
公开(公告)日：2006-02-15
申请号：EP01111735.5
申请日：1995-03-27
申请人： QLT USA, Inc.
发明人： Yewey, Gerald L. , Krinick, Nancy L. , Dunn, Richard L. , Radomsky, Michael L. , Brouwer, Gerbrand , Tipton, Arthur J.
IPC分类号： A61K9/22 , A61K47/48
CPC分类号： A61K9/0024 , A61K9/10 , A61K9/146 , A61K9/5026 , A61K9/5047 , A61K31/4439 , A61K31/485 , A61K31/704 , A61K38/09 , A61K38/27 , A61K47/34 , A61K47/42 , A61K47/58 , A61K47/59 , A61K47/593 , A61K47/6903 , A61K47/6921 , A61K49/0017 , A61K49/0036 , A61K49/0054 , A61K49/0063 , A61K49/0091 , A61L26/0019 , A61L26/0066 , A61L26/0085 , A61L27/18 , A61L27/56 , A61L31/06 , A61L31/146 , A61L31/16 , A61L2300/604 , A61L2300/62 , A61L2400/06 , Y10S514/90 , Y10S525/937 , Y10S977/774 , Y10S977/783 , Y10S977/906 , Y10S977/907 , Y10S977/915 , Y10S977/918 , C08L67/04
摘要： Improved biocompatible liquid delivery compositions, which are useful for the formation of sustained release delivery systems for active agents, are provided. The compositions include liquid formulations of a biocompatible polymer or prepolymer in combination with a controlled release component. The controlled release component includes an active agent. These compositions may be introduced into the body of a subject in liquid form which then solidify or cure in situ to form a gelatinous controlled release implant or a film dressing. The liquid delivery compositions may also be employed ex situ to produce a gelatinous controlled release implant. Methods of forming a gelatinous controlled release implant and employing the liquid formulations in the treatment of a subject are also provided.

3. 发明授权

EP2158900B1 Polymeric delivery formulations of leuprolide with improved efficacy 有权
标题翻译：亮丙瑞林的聚合物制剂具有改善的功效
公开(公告)号：EP2158900B1
公开(公告)日：2013-01-23
申请号：EP09012462.9
申请日：2001-09-21
申请人： QLT USA, Inc.
发明人： Dunn, Richard L. , Garrett, John S. , Ravivarapu, Harish , Chandrashekar, Bhagya L.
IPC分类号： A61K9/00 , A61K38/09 , A61K47/34
CPC分类号： A61K38/09 , A61K9/0019 , A61K9/0024 , A61K9/19 , A61K47/22 , A61K47/34 , B65D81/3205
摘要： The present invention is directed to a flowable composition that is suitable for use as a controlled release implant. The flowable composition includes a biodegradable thermoplastic polyester that is at least substantially insoluble in aqueous medium or body fluid. The flowable composition also includes a biocompatible polar aprotic solvent. The biocompatible polar aprotic solvent is miscible to dispersible in aqueous medium or body fluid. The flowable composition also includes leuprolide acetate. The present invention is also directed to a method for forming the flowable composition. The present invention is also directed to a biodegradable implant formed in situ, in a patient. The biodegradable implant is formed by injecting a flowable composition within the body of the patient and allowing the biocompatible polar aprotic solvent to dissipate to produce a solid biodegradable implant. The present invention is also directed to a method of forming a biodegradable implant in situ, in a living patient. The method includes injecting a flowable composition within the body of a patient and allowing the biocompatible polar aprotic solvent to dissipate to produce a solid biodegradable implant. The present invention is also directed to a method of treating cancer in a patient. The method includes administering to the patient in need of such treatment an effective amount of a flowable composition of the present invention. The present invention is also directed to a method of reducing LHRH levels in a patient. The method includes administering to the patient in need of such LHRH reduction an effective amount of a flowable composition of the present invention. The present invention is also directed to a kit. The kit includes a first container and a second container. The first container includes a composition that includes a biodegradable thermoplastic polyester and a biocompatible polar aprotic solvent. The second container includes leuprolide acetate. The present invention is also directed to a solid implant. The solid implant includes a biocompatible thermoplastic polyester and leuprolide acetate. The solid implant has a solid or gelatinous microporous matrix, wherein the matrix is a core surrounded by a skin. The solid implant can further include a biocompatible organic solvent.

4. 发明公开

EP2158900A1 Polymeric delivery formulations of leuprolide with improved efficacy 有权
标题翻译： Polymere Zubereitungsform von Leuprolid mit verbesserter Wirksamkeit
公开(公告)号：EP2158900A1
公开(公告)日：2010-03-03
申请号：EP09012462.9
申请日：2001-09-21
申请人： QLT USA, Inc.
发明人： Dunn, Richard L. , Garrett, John S. , Ravivarapu, Harish , Chandrashekar, Bhagya L.
IPC分类号： A61K9/00 , A61K38/09 , A61K47/34
CPC分类号： A61K38/09 , A61K9/0019 , A61K9/0024 , A61K9/19 , A61K47/22 , A61K47/34 , B65D81/3205
摘要： The present invention is directed to a flowable composition that is suitable for use as a controlled release implant. The flowable composition includes a biodegradable thermoplastic polyester that is at least substantially insoluble in aqueous medium or body fluid. The flowable composition also includes a biocompatible polar aprotic solvent. The biocompatible polar aprotic solvent is miscible to dispersible in aqueous medium or body fluid. The flowable composition also includes leuprolide acetate. The present invention is also directed to a method for forming the flowable composition. The present invention is also directed to a biodegradable implant formed in situ, in a patient. The biodegradable implant is formed by injecting a flowable composition within the body of the patient and allowing the biocompatible polar aprotic solvent to dissipate to produce a solid biodegradable implant. The present invention is also directed to a method of forming a biodegradable implant in situ, in a living patient. The method includes injecting a flowable composition within the body of a patient and allowing the biocompatible polar aprotic solvent to dissipate to produce a solid biodegradable implant. The present invention is also directed to a method of treating cancer in a patient. The method includes administering to the patient in need of such treatment an effective amount of a flowable composition of the present invention. The present invention is also directed to a method of reducing LHRH levels in a patient. The method includes administering to the patient in need of such LHRH reduction an effective amount of a flowable composition of the present invention. The present invention is also directed to a kit. The kit includes a first container and a second container. The first container includes a composition that includes a biodegradable thermoplastic polyester and a biocompatible polar aprotic solvent. The second container includes leuprolide acetate. The present invention is also directed to a solid implant. The solid implant includes a biocompatible thermoplastic polyester and leuprolide acetate. The solid implant has a solid or gelatinous microporous matrix, wherein the matrix is a core surrounded by a skin. The solid implant can further include a biocompatible organic solvent.
摘要翻译：本发明涉及适合用作控释植入物的可流动组合物。可流动组合物包括至少基本上不溶于水性介质或体液的可生物降解的热塑性聚酯。可流动组合物还包括生物相容的极性非质子传递溶剂。生物相容的极性非质子溶剂可混溶于水性介质或体液中。可流动组合物还包括醋酸亮丙瑞林。本发明还涉及一种形成可流动组合物的方法。本发明还涉及在病人中原位形成的可生物降解植入物。可生物降解的植入物通过在患者体内注射可流动组合物并允许生物相容的极性非质子溶剂消散以产生固体可生物降解的植入物而形成。本发明还涉及一种在活体患者中原位形成生物可降解植入物的方法。该方法包括在患者体内注射可流动的组合物，并允许生物相容的极性非质子溶剂消散以产生固体可生物降解的植入物。本发明还涉及一种在患者体内治疗癌症的方法。该方法包括向需要这种治疗的患者施用有效量的本发明的可流动组合物。本发明还涉及一种降低患者LHRH水平的方法。该方法包括向需要这种LHRH还原的患者施用有效量的本发明的可流动组合物。本发明还涉及一种试剂盒。套件包括第一容器和第二容器。第一容器包括包含可生物降解的热塑性聚酯和生物相容的极性非质子传递溶剂的组合物。第二容器包括醋酸亮丙瑞林。本发明还涉及一种固体植入物。固体植入物包括生物相容性热塑性聚酯和醋酸亮丙瑞林。固体植入物具有固体或凝胶状微孔基质，其中基质是由皮肤包围的核心。固体植入物可进一步包括生物相容性有机溶剂。

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