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11. 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。

12. 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。

13. 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。

14. 发明公开

EP1034207A1 BIODEGRADABLE LOW MOLECULAR WEIGHT TRIBLOCK POLY(LACTIDE-co-GLYCOLIDE) POLYETHYLENE GLYCOL COPOLYMERS HAVING REVERSE THERMAL GELATION PROPERTIES 有权
标题翻译：可生物降解的三嵌段 - 聚（丙交酯 - 共 - 乙）-POLYETHYLENGLYCOL共聚物REVERSE热凝胶化
公开(公告)号：EP1034207A1
公开(公告)日：2000-09-13
申请号：EP98950839.5
申请日：1998-10-02
申请人： Macromed Inc.
发明人： RATHI, Ramesh , ZENTNER, Gaylen, M. , JEONG, Byeongmoon
IPC分类号： C08G65/32 , C08G63/91 , A61K47/30 , A61K47/32 , A61K47/34
CPC分类号： A61K9/0024 , A61K9/1075 , A61K47/34 , C08G63/664 , C08L71/02 , C08L2666/18
摘要： A water soluble biodegradable ABA- or BAB- type triblock polymer is disclosed that is made up of a major amount of a hydrophobic polymer made up of a poly(lactide-co-glycolide) copolymer or poly(lactide) polymer as the A-blocks and a minor amount of hydrophilic polyethylene glycol polymer B-block, having an overall weight average molecular weight of between about 2000 and 4990, and that possesses reverse thermal gelation properties. Effective concentrations of the triblock polymer and a drug may be uniformly contained in an aqueous phase to form a drug delivery composition. The release rate of the drug may be adjusted by changing various parameters such as hydrophobic/hydrophilic component content, polymer concentration, molecular weight and polydispersity of the triblock polymer. Because the triblock polymer is amphiphilic, it functions to increase the solubility and/or stability of drugs in the composition, as demonstrated by a phase diagram illustrating the gelation behaviour of aqueous solutions of a PLGA-PEG-PLGA triblock copolymer studied at different concentrations and temperatures.

15. 发明公开

EP1141079A4 BIODEGRADABLE LOW MOLECULAR WEIGHT TRIBLOCK POLYESTER POLYETHYLENE GLYCOL COPOLYMERS HAVING REVERSE THERMAL GELATION PROPERTIES 有权
标题翻译：具有反向热凝胶可生物降解的低分子三嵌段聚酯聚乙二醇共聚物
公开(公告)号：EP1141079A4
公开(公告)日：2004-03-24
申请号：EP99954698
申请日：1999-09-30
申请人： MACROMED INC
发明人： RATHI RAMESH C , ZENTNER GAYLEN M , JEONG BYEONGMOON
IPC分类号： C08G81/00 , A61K9/00 , A61K9/10 , 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 , C08G63/66 , C08G63/664 , C08G63/91 , C08G65/329 , C08L67/00 , C08L67/04 , C08L71/02 , C08L101/16 , C08G65/32
CPC分类号： C08G63/664 , A61K9/0024 , A61K9/1075 , A61K47/34 , C08L71/02 , C08L2666/18

16. 发明公开

EP1141079A1 BIODEGRADABLE LOW MOLECULAR WEIGHT TRIBLOCK POLYESTER POLYETHYLENE GLYCOL COPOLYMERS HAVING REVERSE THERMAL GELATION PROPERTIES 有权
标题翻译：具有反向热凝胶可生物降解的低分子三嵌段聚酯聚乙二醇共聚物
公开(公告)号：EP1141079A1
公开(公告)日：2001-10-10
申请号：EP99954698.9
申请日：1999-09-30
申请人： Macromed Inc.
发明人： RATHI, Ramesh, C. , ZENTNER, Gaylen, M. , JEONG, Byeongmoon
IPC分类号： C08G63/91 , C08L67/00
CPC分类号： C08G63/664 , A61K9/0024 , A61K9/1075 , A61K47/34 , C08L71/02 , C08L2666/18
摘要： A water soluble, biodegradable ABA- or BAB-type tri-block polymer is disclosed that is made up of a major amount of a hydrophobic A polymer block made of a biodegradable polyester and a minor amount of a hydrophilic polyethylene glycol(PEG) B polymer block, having an overall average molecular weight of between about 2000 and 4990, and that possesses reverse thermal gelation properties. Effective concentrations of the tri-block polymer and a drug may be uniformly contained in an aqueous phase to form a drug delivery composition. At temperatures below the gelation temperature of the tri-block polymer the composition is a liquid and at temperatures at or above the gelation temperature the composition is a gel or semi-solid. The composition may be administered to a warm-blooded animal as a liquid by parenteral, ocular, topical, inhalation, transdermal, vaginal, transurethral, rectal, nasal, oral, pulmonary or aural delivery means and is a gel at body temperature. The composition may also be administered as a gel. The drug is released at a controlled rate from the gel which biodegrades into non-toxic products. The release rate of the drug may be adjusted by changing various parameters such as hydrophobic/hydrophilic component content, polymer concentration, molecular weight and polydispersity of the tri-block polymer. Because the tri-block polymer is amphiphilic, it functions to increase the solubility and/or stability of drugs in the composition.

17. 发明专利

CA2672551C BIODEGRADABLE BLOCK COPOLYMERIC COMPOSITIONS FOR DRUG DELIVERY 未知
公开(公告)号：CA2672551C
公开(公告)日：2013-02-05
申请号：CA2672551
申请日：2003-05-29
申请人： MACROMED INC
发明人： SHIH CHUNG , ZENTNER GAYLEN M
IPC分类号： A61K47/34 , A61K9/10 , A61K31/765 , A61K31/77 , A61K38/28 , C08L67/00 , C08L71/02 , C08L101/16
摘要： An improved drug delivery composition and method of use is disclosed. The composition comprises one or more biodegradable block copolymer drug carriers; and a reconstitution enhancing and enabling agent comprising polyethylene glycol (PEG), a PEG derivative or a mixture of PEG and a PEG derivative. The composition can be administered as is or after being be dissolved or rapidly reconstituted in an aqueous vehicle to afford a homogeneous solution or uniform colloidal system.

18. 发明专利

HK1052713B 溶脹和消溶脹聚合物共混物未知
公开(公告)号：HK1052713B
公开(公告)日：2005-08-19
申请号：HK03104609
申请日：2003-06-27
申请人： MACROMED INC
发明人： GAYLEN M ZENTNER , JONG-SEOK BARK , FENG LIU
IPC分类号： A61K20060101 , A61K9/20 , A61K47/32 , A61K47/34 , A61K47/36 , A61K47/38 , C08B20060101 , C08J20060101 , C08J3/00 , C08J3/205 , C08L20060101 , C08L1/12 , C08L5/02 , C08L5/08 , C08L101/00

19. 发明专利

DE69631290D1 未知
公开(公告)号：DE69631290D1
公开(公告)日：2004-02-12
申请号：DE69631290
申请日：1996-10-25
申请人： MACROMED INC
发明人： CHA YOUNSIK , CHOI YOUNG KWEON , PAI MIN
IPC分类号： A61K9/50 , A61K9/16 , A61K38/00 , A61K38/23 , A61K38/28 , A61K38/38 , A61K47/48 , B01J13/02 , B05D7/00
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.

20. 发明专利

ZA200203164B Swelling and deswelling polymer blends. 未知
公开(公告)号：ZA200203164B
公开(公告)日：2003-06-25
申请号：ZA200203164
申请日：2002-04-22
申请人： MACROMED INC
发明人： ZENTNER GAYLEN M , BARK JONG-SEOK , LIU FENG
IPC分类号： A61K9/20 , A61K47/34 , A61K47/36 , A61K47/32 , A61K47/38 , C08J3/00 , C08J3/205 , C08L1/12 , C08L5/02 , C08L5/08 , C08L101/00 , C08G , C08H , C08J
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 administration.

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