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1. 发明专利

JP2010144178A Biodegradable low molecular weight triblock poly(lactide-co-glycolide)-polyethylene glycol copolymer having reverse thermal gelation property 有权
标题翻译：生物可降解的低分子量TRIBLOCK POLY（LACTIDE-CO-GLYCOLIDE） - 聚乙烯乙二醇共聚物具有反向热凝胶性
公开(公告)号：JP2010144178A
公开(公告)日：2010-07-01
申请号：JP2009297893
申请日：2009-12-28
申请人： Macromed Inc , マクロメド・インコーポレーテッド
发明人： RATHI RAMESH , ZENTNER GAYLEN M , JEONG BYEONGMOON
IPC分类号： C08G63/664 , A61K9/00 , A61K9/08 , A61K9/107 , A61K31/17 , A61K31/282 , A61K31/337 , A61K31/437 , A61K31/519 , A61K31/704 , A61K31/7042 , A61K38/00 , A61K38/04 , A61K38/11 , A61K38/17 , A61K38/21 , A61K38/22 , A61K38/24 , A61K38/26 , A61K38/27 , A61K38/28 , A61K38/43 , A61K39/00 , A61K39/395 , A61K45/00 , A61K47/30 , A61K47/32 , A61K47/34 , A61P35/00 , C08G63/08 , C08G65/329 , C08G81/00 , C08L67/00 , C08L67/04 , C08L71/02 , C08L89/00 , C08L101/16
CPC分类号： A61K9/0024 , A61K9/1075 , A61K47/34 , C08G63/664 , C08L71/02 , C08L2666/18
摘要： PROBLEM TO BE SOLVED: To provide low molecular weight triblock copolymer drug delivery systems that are biodegradable, exhibit reverse thermal gelation behavior, namely, are a liquid solution at low temperatures, reversibly form gels at physiologically relevant temperatures, and provide good drug release characteristics. SOLUTION: A biodegradable BAB-type triblock polymer comprises a hydrophobic A block comprising poly(lactide-co-glycolide) and a hydrophilic B block comprising a hydrophilic polyethylene glycol polymer, wherein when formed as an aqueous polymer solution, the block copolymer possesses reverse thermal gelation characteristics, and the hydrophobic A block comprises 51-83 wt.% of the polymer and the hydrophilic B block comprises 17-49 wt.% of the polymer. Further, a composition includes the biodegradable BAB-type triblock polymer and an effective amount of a drug. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：要解决的问题：为了提供可生物降解的低分子量三嵌段共聚物药物递送系统，表现出反向热凝胶化行为，即在低温下为液体溶液，在生理相关温度下可逆形成凝胶，并提供良好的药物释放特性。解决方案：可生物降解的BAB型三嵌段聚合物包含包含聚（丙交酯 - 共 - 乙交酯）的疏水性A嵌段和包含亲水性聚乙二醇聚合物的亲水性B嵌段，其中当形成为聚合物水溶液时，嵌段共聚物具有反向热凝胶化特性，并且疏水性A嵌段包含51-83重量％的聚合物，并且亲水性B嵌段包含17-49重量％的聚合物。此外，组合物包括可生物降解的BAB型三嵌段聚合物和有效量的药物。版权所有（C）2010，JPO＆INPIT

2. 发明专利

JP2009280600A Biodegradable block copolymer composition for medicine delivery 有权
标题翻译：用于药物递送的生物可降解嵌段共聚物组合物
公开(公告)号：JP2009280600A
公开(公告)日：2009-12-03
申请号：JP2009171750
申请日：2009-07-23
申请人： Macromed Inc , マクロメド・インコーポレーテッド
发明人： SHIH CHUNG , ZENTNER GAYLEN M
IPC分类号： A61K9/00 , A61K47/34 , A61K9/08 , A61K9/10 , A61K31/337 , A61K31/765 , A61K31/77 , A61K38/28 , A61P3/10 , A61P35/00 , C08G63/664 , C08L67/00 , C08L71/02 , C08L101/16
CPC分类号： A61K47/34 , A61K9/0024 , A61K31/765 , A61K31/77 , A61K47/10 , C08G2261/126 , C08L71/02 , C08L2666/18 , C08L2666/02
摘要： PROBLEM TO BE SOLVED: To provide an improved composition and a method for medicine delivery.
SOLUTION: The composition comprises one or more agent carriers made of a biodegradable block copolymer; and an agent that comprises polyethylene glycol (PEG), a PEG derivative or a mixture of PEG and a PEG derivative and raises and enables reconstitution. The composition is administered as it is, or is dissolved to an aqueous vehicle or forms a homogeneous solution or a uniform colloid system that is administered after quick reconstitution.
COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：待解决的问题：提供改进的组合物和药物递送方法。组合物包含一种或多种由可生物降解的嵌段共聚物制成的试剂载体; 以及包含聚乙二醇（PEG），PEG衍生物或PEG和PEG衍生物的混合物并提高并使得能够重构的试剂。组合物原样施用，或溶解于水性载体中，或形成均匀溶液或均匀胶体体系，其在快速重构后施用。版权所有（C）2010，JPO＆INPIT

3. 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。

4. 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。

5. 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。

6. 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。

7. 发明专利

TW574253B 在酸性環境中膨脹而在鹼性環境中去膨脹之聚體攙合物有权
简体标题：在酸性环境中膨胀而在碱性环境中去膨胀之聚体搀合物
公开(公告)号：TW574253B
公开(公告)日：2004-02-01
申请号：TW089124007
申请日：2000-11-13
申请人：麥克羅麥德公司 MACROMED,INC.
发明人：蓋倫增納 ZENTNER, GAYLEN M. , 卜忠三 PARK, JONG SANG , 劉豐 LIU, FENG
IPC分类号： C08G
CPC分类号： C08L1/12 , A61K9/2027 , A61K9/2031 , A61K9/205 , A61K9/2054 , C08J3/005 , C08L5/02 , C08L5/08 , C08L2666/02
摘要：一種聚體攙合物，係將去乙醯殼多醣及一第二聚合物溶於酸性水液中形成水性聚體攙合物，將所述水性聚體攙合物脫水，及回收所述聚體攙合物予以製備。該第二聚合物可由聚醚二醇類包括聚乙二醇；纖維素酯包括乙酸纖維素；聚氧體(poloxamer)；多醣類包括葡聚糖及食糖；聚乙烯基咯酮；聚乙烯醇；及其等之混合物或共聚物所組成集團中選出。此等聚體攙合物在酸性環境中膨脹而在更中性或鹼性環境中去膨脹。此技藝有用於將生物活性物質或藥物分配於周圍環境，尤其腸胃道內所見環境。由於本發明之各種聚體攙合物非以共價或離子方式交聯，而係物理結合，故該物理攙合物內之每一聚合物保持其原始化學結構，因而對經口腔或其他投施路徑具有安全性。
简体摘要：一种聚体搀合物，系将去乙酰壳多糖及一第二聚合物溶于酸性水液中形成水性聚体搀合物，将所述水性聚体搀合物脱水，及回收所述聚体搀合物予以制备。该第二聚合物可由聚醚二醇类包括聚乙二醇；纤维素酯包括乙酸纤维素；聚氧体(poloxamer)；多糖类包括葡聚糖及食糖；聚乙烯基咯酮；聚乙烯醇；及其等之混合物或共聚物所组成集团中选出。此等聚体搀合物在酸性环境中膨胀而在更中性或碱性环境中去膨胀。此技艺有用于将生物活性物质或药物分配于周围环境，尤其肠胃道内所见环境。由于本发明之各种聚体搀合物非以共价或离子方式交联，而系物理结合，故该物理搀合物内之每一聚合物保持其原始化学结构，因而对经口腔或其他投施路径具有安全性。

8. 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。

9. 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。

10. 发明公开

EP1240230A4 SWELLING AND DESWELLING POLYMER BLENDS 有权
标题翻译： AN- UND ABSCHWELLENDE POLYMERBLENDS
公开(公告)号：EP1240230A4
公开(公告)日：2004-12-01
申请号：EP00980328
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 , C08B37/08
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; 纤维素酯，包括乙酸纤维素; 泊洛沙姆; 多糖包括葡聚糖和瓜尔胶; 聚乙烯吡咯烷酮; 聚乙烯醇; 及其混合物或共聚物。这些聚合物混合物在酸性环境中溶胀并在较中性或碱性环境中溶解。该技术对于将生物活性物质或药物分配到周围环境，特别是在胃肠道中发现的环境是有价值的。由于本发明的各种聚合物共混物不共价或离子交联，而是物理组合，物理混合物中的每种聚合物保持其原始化学结构，因此对于口服给药是安全的。

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