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31. 发明申请

US20080317666A1 Colonic Delivery of Active Agents 审中-公开
标题翻译：活性剂的结肠递送
公开(公告)号：US20080317666A1
公开(公告)日：2008-12-25
申请号：US11628832
申请日：2006-02-09
申请人： Elias Fattal , Antoine Andremont , Patrick Couvreur , Sandrine Bourgeois
发明人： Elias Fattal , Antoine Andremont , Patrick Couvreur , Sandrine Bourgeois
IPC分类号： A61K9/00 , A61K49/00 , A61K51/12 , A61P1/00
CPC分类号： A61K9/1652 , A61K9/1682 , A61K31/155 , A61K38/465 , A61K38/47 , C12Y305/02006 , G01N2800/065
摘要： Drug delivery devices that are orally administered, and that release active ingredients in the colon, are disclosed. In one embodiment, the active ingredients are those that inactivate antibiotics, such as macrolides, quinolones and beta-lactam containing antibiotics. One example of a suitable active agent is an enzyme such as beta-lactamases. In another embodiment, the active agents are those that specifically treat colonic disorders, such as Chrohn's Disease, irritable bowel syndrome, ulcerative colitis, colorectal cancer or constipation. The drug delivery devices are in the form of beads of pectin, crosslinked with calcium and reticulated with polyethyleneimine. The high crosslink density of the polyethyleneimine is believed to stabilize the pectin beads for a sufficient amount of time such that a substantial amount of the active ingredients can be administered directly to the colon. Advantageously, the amount of polyethyleneimine is sufficient to allow a substantial portion of the pectin beads to pass through the gastrointestinal tract to the colon without releasing the active agent, and is also sufficient such that the pectin beads are sufficiently degraded in the colon to release an effective amount of the active agent.
摘要翻译：公开了口服给药并且释放结肠中活性成分的药物输送装置。在一个实施方案中，活性成分是使抗生素失活的成分，例如大环内酯类，喹诺酮类和含β-内酰胺类的抗生素。合适的活性剂的一个实例是酶如β-内酰胺酶。在另一个实施方案中，活性剂是特异性治疗结肠疾病如克罗恩病，肠易激综合征，溃疡性结肠炎，结肠直肠癌或便秘的那些。药物递送装置是果胶珠的形式，与钙交联并用聚乙烯亚胺网化。据信聚乙烯亚胺的高交联密度使果胶珠稳定足够的时间，使得大量的活性成分可以直接施用于结肠。有利地，聚乙烯亚胺的量足以允许大部分果胶珠通过胃肠道至结肠而不释放活性剂，并且也足够使得果胶珠在结肠中充分降解以释放有效量的活性剂。

32. 发明申请

US20050043481A1 Material consisting of at least a biodegradable polymer and cyclodextrins 审中-公开
标题翻译：由至少可生物降解的聚合物和环糊精组成的材料
公开(公告)号：US20050043481A1
公开(公告)日：2005-02-24
申请号：US10490417
申请日：2002-09-27
申请人： Ruxandra Gref , Patrick Couvreur
发明人： Ruxandra Gref , Patrick Couvreur
IPC分类号： A61K9/14 , A61K9/16 , A61K9/48 , A61K9/51 , A61K9/52 , A61K31/138 , A61K31/683 , A61K31/70 , A61K31/7032 , A61K31/7088 , A61K31/715 , A61K38/00 , A61K39/395 , A61K47/30 , A61K47/32 , A61K47/34 , A61K47/36 , A61K47/40 , A61K47/48 , A61P35/00 , C08F2/00 , C08G81/00 , C08L101/16
CPC分类号： A61K9/5153 , A61K9/1652 , A61K47/593 , A61K47/6951 , B82Y5/00 , C08G81/00
摘要： The invention concerns a material consisting of at least a biodegradable polymer and a cyclic oligosaccharide, characterized in that at least one molecule of the oligosaccharide is grafted via a covalent bond to at least a molecule of the biodegradable polymer. The invention also concerns a method for preparing the material, the nanoparticles and microparticles derived from the material and uses thereof as biological vectors for active substances.
摘要翻译：本发明涉及由至少一种可生物降解的聚合物和环状低聚糖组成的材料，其特征在于至少一个寡糖分子通过共价键接枝至至少一个分子的可生物降解的聚合物。本发明还涉及一种制备材料的方法，从该材料衍生的纳米颗粒和微粒以及其作为活性物质的生物载体的用途。

33. 发明授权

US06211273B1 Method for preparing malonate methylidene nanoparticles, nanoparticles optionally containing one or several biologically active molecules 有权
标题翻译：制备丙二酸亚甲基纳米颗粒的方法，任选含有一种或几种生物活性分子的纳米颗粒
公开(公告)号：US06211273B1
公开(公告)日：2001-04-03
申请号：US09284455
申请日：1999-04-16
申请人： Nicole Bru-Magniez , Xavier Guillon , Pascal Breton , Patrick Couvreur , François Lescure , Claude Roques-Carmes , Gérard Riess
发明人： Nicole Bru-Magniez , Xavier Guillon , Pascal Breton , Patrick Couvreur , François Lescure , Claude Roques-Carmes , Gérard Riess
IPC分类号： C08K507
CPC分类号： A61K9/5138 , C08F22/14
摘要： The invention relates to a method for the preparation of nanoparticles formed from a random polymer of at least one compound of formula (I) in which A represents a group or a group; R1 and R2, identical or different, represents a linear or branched C1-C6 alkyl group; n=1, 2, 3, 4 or 5, characterised in that the monomer is dissolved beforehand in a water-miscible aprotic organic solvent forming, with the polymerisation medium, a non-solvent mixture of the polymer formed.
摘要翻译：本发明涉及一种由至少一种式（I）化合物的无规聚合物制备的纳米颗粒的制备方法，其中A代表基团; R 1和R 2相同或不同，表示直链或支链C1- C6烷基; n = 1,2,3,4或5，其特征在于，所述单体预先溶解在与水混溶的非质子有机溶剂中，所述聚合介质形成所形成的聚合物的非溶剂混合物。

34. 发明授权

US4489055A Process for preparing biodegradable submicroscopic particles containing a biologically active substance and their use 失效
标题翻译：用于制备含有生物活性物质的可生物降解的亚显微粒子及其用途的方法
公开(公告)号：US4489055A
公开(公告)日：1984-12-18
申请号：US349545
申请日：1982-02-17
申请人： Patrick Couvreur , Michel Roland , Peter Speiser
发明人： Patrick Couvreur , Michel Roland , Peter Speiser
IPC分类号： A61K9/51 , C08F22/32 , G01N33/48 , A61J3/00 , A61K49/00 , B01J13/02
CPC分类号： A61K9/5138 , A61K9/5192 , C08F22/32 , Y10T428/2989
摘要： Biodegradable particles, with a diameter smaller than 500 nanometers, formed by the micellar polymerization of an alkyl-cyano-acrylate where the term "alkyl" means a lower alkyl radical having 1 to 4 carbon atoms and containing a biologically active substance. Also provided are processes for making pharmaceutical compositions containing the biodegradable particles and using the particles in pharmaceutical and diagnostic applications.
摘要翻译：通过氰基 - 丙烯酸烷基酯的胶束聚合形成直径小于500纳米的生物可降解颗粒，其中术语“烷基”是指具有1至4个碳原子并含有生物活性物质的低级烷基。还提供了制备含有可生物降解的颗粒并在药物和诊断应用中使用该颗粒的药物组合物的方法。

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