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1. 发明申请

WO1997015389A1 PREPARATION OF PEPTIDE CONTAINING BIODEGRADABLE MICROSPHERES BY MELT PROCESS 审中-公开
标题翻译：通过熔融法制备含生物可降解微生物的肽
公开(公告)号：WO1997015389A1
公开(公告)日：1997-05-01
申请号：PCT/US1996017237
申请日：1996-10-25
申请人： MACROMED, INC.
发明人： MACROMED, INC. , CHA, Younsik , CHOI, Young, Kweon , PAI, Chaul, Min
IPC分类号： B01J13/02
CPC分类号： A61K38/23 , A61K9/1647 , A61K38/28 , A61K38/38 , B01J13/02
摘要： Peptide/protein biodegradable drug delivery devices are prepared as microspheres without the use of solvents by a polymer melt process. A melt of thermostable polypeptides and an appropriate low melting block copolymer mixture is prepared and dispersed in an appropriate fluid medium such as air, water or an immiscible organic fluid without using any organic solvent to form microdroplets. The fluid medium is cooled to solidify the microdroplets into microspheres and then collected and purified or further processed as drug delivery devices. These biodegradable microspheres are suitable as implantable or injectable pharmaceutical formulations. Following administration as solid microspheres into the body of a warm blooded animal, the formulations absorb water from the body to form a hydrogel from which the polypeptide is released continuously over an extended period of time.
摘要翻译：肽/蛋白质可生物降解的药物递送装置通过聚合物熔融方法制备为不使用溶剂的微球。制备热稳定多肽和合适的低熔点嵌段共聚物混合物的熔体并将其分散在合适的流体介质如空气，水或不混溶的有机流体中，而不使用任何有机溶剂形成微滴。将流体培养基冷却以将微滴固化成微球，然后收集并纯化或进一步加工为药物递送装置。这些可生物降解的微球体适合作为可植入或可注射的药物制剂。在作为固体微球体施用于温血动物的体内后，制剂吸收来自身体的水以形成水凝胶，多肽在延长的时间段内连续释放。

2. 发明申请

WO1997015287A1 THERMOSENSITIVE BIODEGRADABLE POLYMERS BASED ON POLY(ETHER-ESTER) BLOCK COPOLYMERS 审中-公开
标题翻译：基于聚（醚）嵌段共聚物的耐热可生物降解聚合物
公开(公告)号：WO1997015287A1
公开(公告)日：1997-05-01
申请号：PCT/US1996017023
申请日：1996-10-25
申请人： MACROMED, INC.
发明人： MACROMED, INC. , CHA, Younsik , CHOI, Young, Kweon , BAE, You, Han
IPC分类号： A61K09/10
CPC分类号： A61K9/0024 , A61K38/1858 , A61K38/2013 , A61K38/225 , A61K38/28 , A61K47/34
摘要： A system and method for the parenteral delivery of a drug in a biodegradable polymeric matrix to a warm blooded animal as a liquid with the resultant formation of a gel depot for the controlled release of the drug. The system comprises an injectable biodegradable block copolymeric drug delivery liquid having reverse thermal gelation properties. The liquid is an aqueous solution having dissolved or dispersed therein an effective amount of a drug intimately contained in a biodegradable block copolymer matrix. The copolymer has a reverse gelation temperature below the body temperature of the animal to which it is administered and is made up of (i) a hydrophobic A polymer block comprising a member selected from the group consisting of poly( alpha -hydroxy acids) and poly(ethylene carbonates) and (ii) a hydrophobic B polymer block comprising a polyethylene glycol. The liquid is stored below the reverse gelation temperature and is parenterally administered into the animal by intramuscular, intraperitoneal, subcutaneous or similar injection.
摘要翻译：一种用于将可生物降解的聚合物基质中的药物肠胃外递送至温血动物作为液体的系统和方法，其中形成用于控释药物的凝胶储库。该系统包括具有反向热凝胶化特性的可注射的可生物降解的嵌段共聚物药物递送液体。液体是其中溶解或分散有有效量的药物，其密封地包含在可生物降解的嵌段共聚物基质中。该共聚物具有低于其施用的动物的体温的反向凝胶化温度，并且由以下组成：（i）疏水性A聚合物嵌段，其包含选自聚（α-羟基酸）和聚（碳酸亚乙酯）和（ii）包含聚乙二醇的疏水性B聚合物嵌段。将液体储存在反胶凝温度以下，通过肌内，腹膜内，皮下或类似的注射剂肠胃外给药。

3. 发明授权

EP0863745B1 THERMOSENSITIVE BIODEGRADABLE POLYMERS BASED ON POLY(ETHER-ESTER) BLOCK COPOLYMERS 失效
标题翻译：基于聚（酯ESTER）嵌段共聚物热敏生物降解聚合物
公开(公告)号：EP0863745B1
公开(公告)日：2004-05-26
申请号：EP96937727.4
申请日：1996-10-25
申请人： Macromed Inc.
发明人： CHA, Younsik , CHOI, Young Kweon , BAE, You Han
IPC分类号： A61K9/10 , A61K47/34
CPC分类号： A61K9/0024 , A61K38/1858 , A61K38/2013 , A61K38/225 , A61K38/28 , A61K47/34
摘要： A system and method for the parenteral delivery of a drug in a biodegradable polymeric matrix to a warm blooded animal as a liquid with the resultant formation of a gel depot for the controlled release of the drug. The system comprises an injectable biodegradable block copolymeric drug delivery liquid having reverse thermal gelation properties. The liquid is an aqueous solution having dissolved or dispersed therein an effective amount of a drug intimately contained in a biodegradable block copolymer matrix. The copolymer has a reverse gelation temperature below the body temperature of the animal to which it is administered and is made up of (i) a hydrophobic A polymer block comprising a member selected from the group consisting of poly( alpha -hydroxy acids) and poly(ethylene carbonates) and (ii) a hydrophobic B polymer block comprising a polyethylene glycol. The liquid is stored below the reverse gelation temperature and is parenterally administered into the animal by intramuscular, intraperitoneal, subcutaneous or similar injection.

4. 发明公开

EP0863745A1 THERMOSENSITIVE BIODEGRADABLE POLYMERS BASED ON POLY(ETHER-ESTER) BLOCK COPOLYMERS 失效
标题翻译：基于聚（酯ESTER）嵌段共聚物热敏生物降解聚合物
公开(公告)号：EP0863745A1
公开(公告)日：1998-09-16
申请号：EP96937727.0
申请日：1996-10-25
申请人： Macromed Inc.
发明人： CHA, Younsik , CHOI, Young Kweon , BAE, You Han
IPC分类号： A61K9 , A61K38 , A61K47
CPC分类号： A61K9/0024 , A61K38/1858 , A61K38/2013 , A61K38/225 , A61K38/28 , A61K47/34
摘要： A system and method for the parenteral delivery of a drug in a biodegradable polymeric matrix to a warm blooded animal as a liquid with the resultant formation of a gel depot for the controlled release of the drug. The system comprises an injectable biodegradable block copolymeric drug delivery liquid having reverse thermal gelation properties. The liquid is an aqueous solution having dissolved or dispersed therein an effective amount of a drug intimately contained in a biodegradable block copolymer matrix. The copolymer has a reverse gelation temperature below the body temperature of the animal to which it is administered and is made up of (i) a hydrophobic A polymer block comprising a member selected from the group consisting of poly(α-hydroxy acids) and poly(ethylene carbonates) and (ii) a hydrophobic B polymer block comprising a polyethylene glycol. The liquid is stored below the reverse gelation temperature and is parenterally administered into the animal by intramuscular, intraperitoneal, subcutaneous or similar injection.

5. 发明授权

EP0857081B1 PREPARATION OF PEPTIDE CONTAINING BIODEGRADABLE MICROSPHERES BY MELT PROCESS 失效
标题翻译：含肽的生物可降解微球，制造通过熔融
公开(公告)号：EP0857081B1
公开(公告)日：2004-01-07
申请号：EP96937031.1
申请日：1996-10-25
申请人： Macromed Inc.
发明人： CHA, Younsik , CHOI, Young Kweon , PAI, Chaul, Min
IPC分类号： B01J13/02 , B05D7/00 , A61K9/16
CPC分类号： A61K38/23 , A61K9/1647 , A61K38/28 , A61K38/38 , B01J13/02
摘要： Peptide/protein biodegradable drug delivery devices are prepared as microspheres without the use of solvents by a polymer melt process. A melt of thermostable polypeptides and an appropriate low melting block copolymer mixture is prepared and dispersed in an appropriate fluid medium such as air, water or an immiscible organic fluid without using any organic solvent to form microdroplets. The fluid medium is cooled to solidify the microdroplets into microspheres and then collected and purified or further processed as drug delivery devices. These biodegradable microspheres are suitable as implantable or injectable pharmaceutical formulations. Following administration as solid microspheres into the body of a warm blooded animal, the formulations absorb water from the body to form a hydrogel from which the polypeptide is released continuously over an extended period of time.

6. 发明公开

EP0857081A1 PREPARATION OF PEPTIDE CONTAINING BIODEGRADABLE MICROSPHERES BY MELT PROCESS 失效
标题翻译：含肽的生物可降解微球，制造通过熔融
公开(公告)号：EP0857081A1
公开(公告)日：1998-08-12
申请号：EP96937031.0
申请日：1996-10-25
申请人： Macromed Inc.
发明人： CHA, Younsik , CHOI, Young, Kweon , PAI, Chaul, Min
IPC分类号： A61K9 , A61K38 , A61K47 , B01J13
CPC分类号： A61K38/23 , A61K9/1647 , A61K38/28 , A61K38/38 , B01J13/02
摘要： Peptide/protein biodegradable drug delivery devices are prepared as microspheres without the use of solvents by a polymer melt process. A melt of thermostable polypeptides and an appropriate low melting block copolymer mixture is prepared and dispersed in an appropriate fluid medium such as air, water or an immiscible organic fluid without using any organic solvent to form microdroplets. The fluid medium is cooled to solidify the microdroplets into microspheres and then collected and purified or further processed as drug delivery devices. These biodegradable microspheres are suitable as implantable or injectable pharmaceutical formulations. Following administration as solid microspheres into the body of a warm blooded animal, the formulations absorb water from the body to form a hydrogel from which the polypeptide is released continuously over an extended period of time.

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