ALPHA-AMINOAMIDINE POLYMERS AND USES THEREOF
    44.
    发明公开
    ALPHA-AMINOAMIDINE POLYMERS AND USES THEREOF 审中-公开
    α-氨基酰胺聚合物及其用途

    公开(公告)号:EP2791210A1

    公开(公告)日:2014-10-22

    申请号:EP12809954.6

    申请日:2012-12-15

    摘要: α-Aminoamidine polymers and methods of preparing a-aminoamidine polymers by reacting by reacting one or more amines with one or more isocyanides and one or more aldehydes are described. Methods of preparing a-aminoamidine polymers from commercially available starting materials are also provided, wherein the starting materials are racemic or stereochemically pure. a-Aminoamidine polymers or salt forms thereof are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems and for other purposes as well such as, for example, coatings, additives, excipients, plastics, and materials, etc. Given the amino moiety of these α-aminoamidine polymers, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive α-aminoamidine polymers and polynucleotides can be prepared. The inventive α-aminoamidine polymers may also be used in preparing microparticles for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.

    摘要翻译: 描述了α-氨基脒聚合物和通过使一种或多种胺与一种或多种异氰化物和一种或多种醛反应来制备α-氨基脒聚合物的方法。 还提供了由市售原料制备α-氨基脒聚合物的方法,其中原料是外消旋或立体化学纯的。 α-氨基脒聚合物或其盐形式优选是可生物降解的和生物相容的,并且可以用于多种药物递送系统中以及用于其他目的,例如涂料,添加剂,赋形剂,塑料和材料等。给定的 这些α-氨基脒聚合物的氨基部分,它们特别适合于递送多核苷酸。 可以制备含有本发明的α-氨基脒聚合物和多核苷酸的复合物,胶束,脂质体或颗粒。 本发明的α-氨基脒聚合物也可以用于制备用于药物递送的微粒。 考虑到它们缓冲周围环境pH的能力,它们在提供不稳定剂方面特别有用。

    MICROCHIP DEVICES FOR DELIVERY OF MOLECULES AND METHODS OF FABRICATION THEREOF
    46.
    发明授权
    MICROCHIP DEVICES FOR DELIVERY OF MOLECULES AND METHODS OF FABRICATION THEREOF 有权
    MICROCHIP药品管理体系和方法。

    公开(公告)号:EP1235560B1

    公开(公告)日:2006-04-19

    申请号:EP00992588.4

    申请日:2000-12-01

    IPC分类号: A61K9/20 A61K9/00

    摘要: Methods of manufacturing microchip devices are provided for controlled release of molecules, such as drugs. Methods include compression molding and casting, alone or in combination with microfabrication techniques. In preferred embodiments, devices are made by (1) filling a die with a polymer powder; (2) compressing the powder to form a polymer preform; (3) thermal compression molding the preform to form a substrate in a mold having a plurality of protrusions that form reservoirs in the substrate; and (4) filling the reservoirs with a release system comprising the molecules to be released. Alternatively, ceramic devices are formed by casting the substrate from a ceramic powder or a slurry using a mold having protrusions that form reservoirs in the substrate. Control over the release rate and time of the molecules from the reservoirs of the microchip device is provided by incorporating release systems and/or reservoir caps.

    BIODEGRADABLE POLYMER NETWORKS FOR USE IN ORTHOPEDIC AND DENTAL APPLICATIONS
    49.
    发明授权
    BIODEGRADABLE POLYMER NETWORKS FOR USE IN ORTHOPEDIC AND DENTAL APPLICATIONS 失效
    可生物降解聚合物联网骨科和牙科的

    公开(公告)号:EP0882085B1

    公开(公告)日:2002-07-24

    申请号:EP97906686.7

    申请日:1997-02-19

    摘要: Biodegradable polymer networks are provided which are useful in a variety of dental and orthopedic applications. The biodegradable polymer networks can be formed in one embodiment by polymerizing anhydride prepolymers including cross-linkable groups, such as unsaturated moieties. The anhydride prepolymers can be cross-linked, for example in a photopolymerization reaction by irradiation of the prepolymer with light in the presence of a free radical initiator. Suitable anhydride prepolymers include dianhydrides of a dicarboxylic acid and a carboxylic acid molecule comprising a cross-linkable group. For example, methacrylic acid dianhydrides of monomers or oligomers of a diacid such as sebacic acid or 1,3-bis(p-carboxyphenoxy)-hexane can be used. The anhydride prepolymers can be applied in vivo to a site where an orthopedic implant is needed, and then may be cross-linked, for example, by irradiation with UV light, to form a biodegradable implant such as a rod, pin or plate. The implants advantageously provide mechanical support and also are capable of slow surface degradation to permit bone ingrowth.

    MICROCHIP DRUG DELIVERY DEVICES
    50.
    发明授权
    MICROCHIP DRUG DELIVERY DEVICES 失效
    MIKROCHIP-ARZNEISTOFFVERABREICHNUNGSSYSTEME

    公开(公告)号:EP0914092B1

    公开(公告)日:2002-04-17

    申请号:EP97936950.1

    申请日:1997-07-02

    IPC分类号: A61K9/00

    摘要: Microchips are provided, which control both the rate and time of release of multiple chemical substances and which allow for the release of a wide variety of molecules in either a continuous or pulsatile manner. In all of the preferred embodiments, a material that is impermeable to the drugs or other molecules to be delivered and the surrounding fluids is used as the substrate. Reservoirs are etched into the substrate using either chemical (wet) etching or ion beam (dry) etching techniques well-known in the field of microfabrication. Hundreds to thousands of reservoirs can be fabricated on a single microchip using these techniques. A release system, which includes the molecules to be delivered, is inserted into the reservoirs by injection, inkjet printing or spin coating methods. Exemplary release systems include polymers and polymeric matrices, non-polymeric matrices, and other excipients or diluents. The physical properties of the release system control the rate of release of the molecules. The reservoirs can contain multiple drugs or other molecules in variable dosages. The filled reservoirs can be capped with materials that either degrade, dissolve, or allow the molecules to diffuse passively out of the reservoir over time or materials that, upon application of an electric potential, oxidize to form soluble compounds or ions that dissolve into the surrounding fluids. Release from an active device can be controlled by a preprogrammed microprocessor, remote control, or by biosensors.

    摘要翻译: 为微芯片提供制造方法,其控制多种化学物质的释放速率和时间,并允许以连续或脉动方式释放多种分子。 在所有优选的实施方案中,将待递送的药物或其它分子和周围的流体不可渗透的材料用作基底。 使用在微细加工领域中熟知的化学(湿)蚀刻或等离子(干)蚀刻技术将储层蚀刻到基底中。 使用这些技术可以在单个微芯片上制造数百到数千个储层。 包括待输送分子的释放系统通过注射,喷墨印刷或旋涂方法插入储存器中。 示例性的释放系统包括聚合物和聚合物基质,非聚合物基质和其它赋形剂或稀释剂。 释放系统的物理性质控制分子的释放速率。 储层可以含有多种药物或其他可变剂量的分子。 填充的储存器可以用被动分解的材料封盖,允许分子随时间被动地扩散到储存器中的材料,或在施加电势时分解的材料。 从有源设备释放可以由预编程的微处理器,遥控器或生物传感器控制。