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    Ph-selective delivery system using crosslinked polymeric resins as vehicles
    1.
    发明授权
    Ph-selective delivery system using crosslinked polymeric resins as vehicles 失效
    使用交联聚合物树脂作为载体的选择性递送系统

    公开(公告)号：US06471955B1

    公开(公告)日：2002-10-29

    申请号：US09050042

    申请日：1998-03-30

    申请人： Samuel J. Tremont ,  Denis Forster ,  Ricky L. Fenton ,  Yinong Ma

    发明人： Samuel J. Tremont ,  Denis Forster ,  Ricky L. Fenton ,  Yinong Ma

    IPC分类号： A61K3175

    CPC分类号： A61K31/5575 ,  A61K47/58 ,  A61K47/6927 ,  Y10S514/926 ,  Y10S514/927

    摘要： This invention provides a method of preparing a polymeric delivery system for active ingredients having enhanced site specific release performance characteristics. The delivery system is formed either by attaching the active ingredient to a linker through an acid-sensitive covalent bond, then forming a covalent bond between the linker and a portion of the subunits of a crosslinked polystyrene polymer, or by attaching a linker to a portion of the subunits of a crosslinked polystyrene polymer, then attaching the active ingredient to the polymer-linker combination through an acid-sensitive covalent bond. The invention also provides a delivery system comprising an active ingredient covalently bonded through an acid-sensitive covalent bond to a linker, which is in turn covalently bonded to a portion of subunits of a crosslinked polystyrene polymer. The invention further provides a method for treatment or prevention of gastric ulcers using a delivery system capable of delivering prostaglandin or prostacyclin drugs, especially misoprostol.

    摘要翻译： 本发明提供了制备具有增强的位点特异性释放性能特征的活性成分的聚合物递送系统的方法。 递送系统通过将活性成分通过酸敏感共价键连接到接头上，然后在接头与交联聚苯乙烯聚合物的一部分亚单位之间形成共价键，或通过将接头连接到部分 的交联聚苯乙烯聚合物的亚基，然后通过酸敏感共价键将活性成分连接到聚合物 - 连接体组合。 本发明还提供了一种递送系统，其包含通过酸敏感共价键共价结合至接头的活性成分，其接触共价键合到交联聚苯乙烯聚合物的一部分亚单位。 本发明还提供了使用能够递送前列腺素或前列环素药物，特别是米索前列醇的递送系统来治疗或预防胃溃疡的方法。

    Gastro-specific prodrugs
    2.
    发明授权
    Gastro-specific prodrugs 失效
    胃特异性前药

    公开(公告)号：US06413945B1

    公开(公告)日：2002-07-02

    申请号：US09514819

    申请日：2000-02-28

    申请人： Samuel J. Tremont ,  Paul W. Collins ,  Ricky L. Fenton

    发明人： Samuel J. Tremont ,  Paul W. Collins ,  Ricky L. Fenton

    IPC分类号： C07F710

    CPC分类号： A61K47/60 ,  C07F7/1804

    摘要： A compound is disclosed havin the formula AW—SiR1R2R3 wherein R1 and R2 are independently alkyl, cycloalkyl, alkenyl, alkynyl, aryl, aralkyl, alkaryl, or a hydrophilic group; R3 is a hydrophilic group; and AW is the covalently bonded form of a drug AWH, wherein W is O, NH, S, or an enolate group. The hydrophilic group may be either non-neutral, or may be a polyol. This compound serves as a prodrug for the drug AWH. A method for preparing these compounds is also disclosed. Also disclosed is a method of treatment or prevention of gastric ulcers by administering the prodrug compounds.

    摘要翻译： 公开了化合物，其中R 1和R 2独立地为烷基，环烷基，烯基，炔基，芳基，芳烷基，烷芳基或亲水基团; R3是亲水基团; AW是药物AWH的共价键合形式，其中W是O，NH，S或烯醇化物基团。 亲水基团可以是非中性的，也可以是多元醇。 该化合物用作药物AWH的前药。 还公开了制备这些化合物的方法。 还公开了通过施用前药化合物治疗或预防胃溃疡的方法。