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1. 发明申请

WO2006023388A2 BIODEGRADABLE DIBLOCK COPOLYMERS HAVING REVERSE THERMAL GELATION PROPERTIES AND METHODS OF USE THEREOF 审中-公开
标题翻译：具有反向热凝性能的可生物降解的二嵌段共聚物及其使用方法
公开(公告)号：WO2006023388A2
公开(公告)日：2006-03-02
申请号：PCT/US2005/028710
申请日：2005-08-11
申请人： MACROMED, INC. , JO. Seongbong , PIAO, Ai-Zhi
发明人： JO. Seongbong , PIAO, Ai-Zhi
IPC分类号： C08F20/00 , A61F2/00
CPC分类号： A61K47/34 , A61K9/0024 , A61L27/54 , A61L27/58 , A61L2300/252 , A61L2300/256 , A61L2300/258 , A61L2300/414 , A61L2300/416 , A61L2300/43 , A61L2300/604 , A61L2300/64 , C08G63/664 , C08G64/183 , C08L53/00 , C08L53/005 , C08L2666/02
摘要： A water soluble, biodegradable AB type diblock copolymer which comprises 61 to 85 by weight of a biodegradable, hydrophobic A block comprising a biodegradable polyester, and 15 to 39 % by weight of a biocompatible, hydrophilic B block comprising a monofunctional polyethylene glycol(PEG) having a number average molecular weight less than 5000, and wherein said diblock copolymer has a number average molecular weight less than 15000 and possesses reverse thermal gelation properties.
摘要翻译：包含61至85重量％的包含可生物降解聚酯的可生物降解的疏水性A嵌段和15至39重量％的包含单官能聚乙二醇（PEG）的生物相容性亲水性B嵌段的水溶性可生物降解AB型二嵌段共聚物，数均分子量小于5000，其中所述二嵌段共聚物的数均分子量小于15000，具有反向热凝胶化特性。

2. 发明申请

WO2006023388A3 BIODEGRADABLE DIBLOCK COPOLYMERS HAVING REVERSE THERMAL GELATION 审中-公开
标题翻译：具有反向热凝胶的生物可降解的二嵌段共聚物
公开(公告)号：WO2006023388A3
公开(公告)日：2006-05-18
申请号：PCT/US2005028710
申请日：2005-08-11
申请人： MACROMED INC , JO SEONGBONG , PIAO AI-ZHI
发明人： JO SEONGBONG , PIAO AI-ZHI
IPC分类号： A61K9/14 , A61F2/00 , A61F13/00
CPC分类号： A61K47/34 , A61K9/0024 , A61L27/54 , A61L27/58 , A61L2300/252 , A61L2300/256 , A61L2300/258 , A61L2300/414 , A61L2300/416 , A61L2300/43 , A61L2300/604 , A61L2300/64 , C08G63/664 , C08G64/183 , C08L53/00 , C08L53/005 , C08L2666/02
摘要： A water soluble, biodegradable AB type diblock copolymer which comprises 61 to 85 by weight of a biodegradable, hydrophobic A block comprising a biodegradable polyester, and 15 to 39 % by weight of a biocompatible, hydrophilic B block comprising a monofunctional polyethylene glycol(PEG) having a number average molecular weight less than 5000, and wherein said diblock copolymer has a number average molecular weight less than 15000 and possesses reverse thermal gelation properties.
摘要翻译：包含61至85重量％的包含可生物降解的聚酯的可生物降解的疏水性A嵌段和15至39重量％的包含单官能聚乙二醇（PEG）的生物相容的亲水性B嵌段的水溶性可生物降解的AB型二嵌段共聚物，数均分子量小于5000，其中所述二嵌段共聚物的数均分子量小于15000，具有反向热凝胶化特性。

3. 发明申请

WO03005961A2 A BIOACTIVE AGENT DELIVERING SYSTEM COMPRISED OF MICROPARTICULES WITHIN A BIODEGRADABLE TO IMPROVE RELEASE PROFILES 审中-公开
标题翻译：包含微生物在生物可扩展以提高释放特性的生物活性剂递送系统
公开(公告)号：WO03005961A2
公开(公告)日：2003-01-23
申请号：PCT/US0222017
申请日：2002-07-12
申请人： MACROMED INC , SHIH CHUNG , ZENTNER GAYLEN
发明人： SHIH CHUNG , ZENTNER GAYLEN
IPC分类号： A61K9/00 , A61K9/06 , A61K9/14 , A61K9/16 , A61K9/50 , A61K9/51 , A61K38/00 , A61K47/30 , A61K47/34 , A61K48/00 , A61P35/00 , A61K
CPC分类号： A61K9/0024 , A61K9/06 , A61K9/1647 , A61K47/34
摘要： A composition and method for releasing a bio-active agent or a drug within a biological environment in a controlled manner is disclosed. The composition is a dual phase polymeric agent- delivery composition comprising a continuous biocompatible gel phase, a discontinuous particulate phase comprising defined microparticles and an agent to be delivered.
摘要翻译：公开了以可控制的方式在生物环境中释放生物活性剂或药物的组合物和方法。组合物是双相聚合物递送组合物，其包含连续的生物相容性凝胶相，包含限定的微粒的不连续颗粒相和待递送的试剂。

4. 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。

5. 发明申请

WO0134677A8 SWELLING AND DESWELLING POLYMER BLENDS 审中-公开
标题翻译：溶胀和脱落聚合物混合物
公开(公告)号：WO0134677A8
公开(公告)日：2001-10-11
申请号：PCT/US0030908
申请日：2000-11-10
申请人： MACROMED INC
发明人： ZENTNER GAYLEN M , BARK JONG-SEOK , LIU FENG
IPC分类号： A61K47/32 , A61K9/20 , A61K47/34 , A61K47/36 , A61K47/38 , C08J3/00 , C08J3/205 , C08L1/12 , C08L5/02 , C08L5/08 , C08L101/00 , C08G63/48 , C08G63/91 , C08H1/06 , C08J5/10
CPC分类号： C08L1/12 , A61K9/2027 , A61K9/2031 , A61K9/205 , A61K9/2054 , C08J3/005 , C08L5/02 , C08L5/08 , C08L2666/02
摘要： A polymer blend is prepared by dissolving chitosan and a second polymer in an acidic aqueous solution to form an aqueous polymer blend, dehydrating said aqueous polymer blend, and recovering said polymer blend. The second polymer may be selected from the group consisting of polyether glycols including polyethylene glycols; cellulose esters including cellulose acetate; poloxamers; polysaccharides including dextran and guar; polyvinylpyrrolidones; polyvinyl alcohols; and mixtures or copolymers thereof. These polymer blends swell in an acidic environment and deswell in a more neutral or basic environment. This technology is valuable for the dispensing of biologically active material or drugs into a surrounding environment, especially the environment as is found in the gastrointestinal tract. Since the various polymer blends of the present invention are not covalently or ionically crosslinked, but are physically combined, each polymer in the physical blend maintains its original chemical structure, and therefore, is safe for oral or other routes of administration.
摘要翻译：通过将壳聚糖和第二聚合物溶解在酸性水溶液中以形成水性聚合物共混物，使所述水性聚合物共混物脱水并回收所述聚合物共混物来制备聚合物共混物。第二聚合物可以选自包括聚乙二醇的聚醚二醇; 包括乙酸纤维素的纤维素酯泊洛沙姆; 包括葡聚糖和瓜尔胶的多糖; 聚乙烯吡咯烷酮; 聚乙烯醇; 及其混合物或共聚物。这些聚合物共混物在酸性环境中溶胀并在更中性或碱性环境中消除。该技术对于将生物活性物质或药物分配到周围环境中是有价值的，尤其是在胃肠道中发现的环境。由于本发明的各种聚合物共混物不是共价或离子交联的，而是物理结合的，物理共混物中的每种聚合物都保持其原始的化学结构，因此对于口服或其他给药途径是安全的。

6. 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。

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