公开(公告)号：US06699505B2

公开(公告)日：2004-03-02

申请号：US09981655

申请日：2001-10-17

申请人： Venkatram R. Shastri ,  Isaac Yue ,  Patrice Hildgen ,  Ruben Dario Sinisterra ,  Robert Langer

发明人： Venkatram R. Shastri ,  Isaac Yue ,  Patrice Hildgen ,  Ruben Dario Sinisterra ,  Robert Langer

IPC分类号： A61K914

CPC分类号： A61K31/155 ,  A61K31/65 ,  A61K31/7036 ,  A61K47/6951 ,  B82Y5/00

摘要： The present invention provides methods of increasing the biological activity of a bioactive agent by complexing the bioactive agent with a complexing agent. In one preferred embodiment, the bioactive agent is an antibiotic and the complexing agent is a cyclodextrin. However, the invention may be extended to include any drugs as bioactive agents. In certain preferred embodiments, the bioactive agent fits into a hydrophobic core of a complexing agent.

摘要翻译： 本发明提供了通过使生物活性剂与络合剂络合来增加生物活性剂的生物活性的方法。 在一个优选的实施方案中，生物活性剂是抗生素，并且络合剂是环糊精。 然而，本发明可以扩展到包括任何药物作为生物活性剂。 在某些优选的实施方案中，生物活性剂适合于络合剂的疏水核心。

公开(公告)号：US20060165987A1

公开(公告)日：2006-07-27

申请号：US10510319

申请日：2003-04-04

申请人： Patrice Hildgen ,  Avedis Panoyan ,  Francois-Xavier Lacasse ,  Richard Quesnel ,  Nevine Rizkalla

发明人： Patrice Hildgen ,  Avedis Panoyan ,  Francois-Xavier Lacasse ,  Richard Quesnel ,  Nevine Rizkalla

IPC分类号： B32B9/02

CPC分类号： A61K9/5153 ,  A61K9/5192 ,  A61K47/34 ,  C08G63/668 ,  C08G63/672 ,  Y10T428/2984

摘要： Disclosed herein are stealthy polymeric biodegradable nanospheres each comprising: (i) a polyester-polyethylene multiblock copolymer; (ii) optionally a polyester entangled with the multiblock copolymer to give rigidity to the nanospheres; and (iii) optionally a pharmaceutical compound incorporated therein. Also disclosed is the use of such nanospheres for the preparation of a medicament having a long-term and non-toxic release of a pharmaceutical compound into a mammal, and the method for preparing a stealthy polymeric biodegradable nanospheres.

摘要翻译： 本文公开了隐形聚合物可生物降解的纳米球，其包含：（i）聚酯 - 聚乙烯多嵌段共聚物; （ii）任选地与多嵌段共聚物缠结的聚酯以赋予纳米球的刚性; 和（iii）任选地掺入其中的药物化合物。 还公开了这样的纳米球用于制备将药物化合物长期和无毒释放到哺乳动物中的药物的用途，以及制备隐形聚合物可生物降解纳米球的方法。

公开(公告)号：US20050203270A1

公开(公告)日：2005-09-15

申请号：US10510407

申请日：2003-04-03

申请人： Patrice Hildgen ,  Gregoire Leclair ,  Richard Quesnel

发明人： Patrice Hildgen ,  Gregoire Leclair ,  Richard Quesnel

IPC分类号： A61K9/16 ,  C08G63/08 ,  C08G63/91 ,  C08G65/22 ,  C08L71/02

CPC分类号： C08G65/22 ,  A61K9/1647 ,  C08G63/912 ,  C08L71/02 ,  C08L2203/02 ,  C08L2205/05 ,  C08L2666/18

摘要： Disclosed is a polymer of the formula I: wherein: Z is —O— or —NH—; R1 represents a non-functional backbone of a hydroxy acid or amino acid derived from a cyclic ester or diester or cyclic amide or diamide monomer (A); R2 represents a non-functional chain derived from an epoxide monomer (B), said chain ending with a graftable hydroxy or carboxylic group; n is the number of units derived from the monomers (A); m is the number of units derived from the monomers (B); and x is equal to n+m, the ratio m/x ranging from 0.005 to 0.30. Also disclosed is a process of preparing this functionalizable polymer to the hydroxy or carboxylic groups of which can be grafted a compound selected from the group consisting of: ligands specific to cellular receptors, such as Selectine E; lipids; peptides; polyethers; polyacrylates; natural polymers; polyosides; antigens or antibodies; salen; and cyclodextrins. The so grafted polymer can be used as carried or excipient in the biomedical and pharmaceutical fields.

摘要翻译： 公开了式I的聚合物：其中：Z是-O-或-NH-; R 1代表衍生自环酯或二酯或环酰胺或二酰胺单体（A）的羟基酸或氨基酸的非官能主链; R 2表示衍生自环氧化物单体（B）的非官能链，所述链以可接枝的羟基或羧基为末端; n是衍生自单体（A）的单元数; m是衍生自单体（B）的单元数; x等于n + m，m / x的比例范围为0.005〜0.30。 还公开了将该可官能化聚合物制备成羟基或羧基的方法，其可以接枝选自以下的化合物：对细胞受体特异性的配体，例如Selectine E; 脂质 肽类 聚醚 聚丙烯酸酯; 天然聚合物; 多糖苷 抗原或抗体; 萨伦 和环糊精。 所述接枝聚合物可用作生物医药领域的载体或赋形剂。