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    Process for the preparation of immobilized and activity-stabilized complexes of LHRH antagonists
    4.
    发明授权
    Process for the preparation of immobilized and activity-stabilized complexes of LHRH antagonists 失效
    制备LHRH拮抗剂的固定和活性稳定复合物的方法

    公开(公告)号：US6054555A

    公开(公告)日：2000-04-25

    申请号：US422990

    申请日：1999-10-22

    申请人： Jurgen Engel ,  Wolfgang Deger ,  Thomas Reissmann ,  Gunter Losse ,  Wolfgang Naumann ,  Sandra Murgas

    发明人： Jurgen Engel ,  Wolfgang Deger ,  Thomas Reissmann ,  Gunter Losse ,  Wolfgang Naumann ,  Sandra Murgas

    IPC分类号： A61K47/48 ,  A61K38/09 ,  A61K38/24 ,  A61K45/00 ,  A61P35/00 ,  C07K14/59

    CPC分类号： A61K47/48315 ,  A61K38/09 ,  Y10S514/841 ,  Y10S514/951

    摘要： In this invention, a release-delaying system is to be developed for LHRH antagonists, in particular for cetrorelix, which allows the active compound to be released in a controlled manner over several weeks by complexation with suitable biophilic carriers. The acidic polyamino acids polyglutamic acid and polyaspartic acid were selected for complexation with cetrorelix. The cetrorelix polyamino acid complexes are prepared from aqueous solutions by combination of the solutions and precipitation of the complexes, which are subsequently centrifuged off and dried over P.sub.2 O.sub.5 in vacuo. If complexes having a defined composition are to be obtained, lyophilization proves to be a suitable method. The cetrorelix-carboxylic acid complexes were also prepared from the aqueous solutions. In the random liberation system, the acidic polyamino acids poly-Glu and poly-Asp showed good release-delaying properties as a function of the hydrophobicity and the molecular mass of the polyamino acid. In animal experiments, it was possible to confirm the activity of the cetrorelix-polyamino acid complexes as a depot system in principle. It is thus possible by complexation of cetrorelix with polyamino acids to achieve testosterone suppression in male rats over 600 hours. The release of active compound here can be controlled by the nature and the molecular mass of the polymers.

    摘要翻译： 在本发明中，将开发用于LHRH拮抗剂，特别是西曲瑞克的释放延迟系统，其允许活性化合物在几周内以适当的生物亲和载体络合以受控的方式释放。 选择酸性聚氨基酸聚谷氨酸和聚天冬氨酸与西曲瑞克络合。 由溶液的组合和络合物的沉淀通过水溶液制备西曲瑞克聚氨基酸复合物，随后将其离心并真空干燥P2O5。 如果要获得具有限定组成的复合物，则冻干证明是合适的方法。 也由水溶液制备西曲瑞克 - 羧酸络合物。 在随机释放系统中，酸性聚氨基酸poly-Glu和poly-Asp显示出作为聚氨基酸的疏水性和分子量的函数的良好的释放延迟性质。 在动物实验中，原则上可以确认西曲瑞克 - 聚氨基酸复合物作为贮库系统的活性。 因此，通过将西曲瑞克与聚氨基酸络合，可以在600小时内在雄性大鼠中实现睾酮抑制。 这里的活性化合物的释放可以通过聚合物的性质和分子量来控制。

    Immobilized and activity-stabilized complexes of LHRH antagonists and processes for their preparation
    5.
    发明授权
    Immobilized and activity-stabilized complexes of LHRH antagonists and processes for their preparation 失效
    LHRH拮抗剂的固定和活性稳定复合物及其制备方法

    公开(公告)号：US6022860A

    公开(公告)日：2000-02-08

    申请号：US48244

    申请日：1998-03-26

    申请人： Jurgen Engel ,  Wolfgang Deger ,  Thomas Reissmann ,  Gunter Losse ,  Wolfgang Naumann ,  Sandra Murgas

    发明人： Jurgen Engel ,  Wolfgang Deger ,  Thomas Reissmann ,  Gunter Losse ,  Wolfgang Naumann ,  Sandra Murgas

    IPC分类号： A61K47/48 ,  A61K38/09 ,  A61K38/24 ,  A61K45/00 ,  A61P35/00 ,  A61K38/00

    CPC分类号： A61K47/48315 ,  A61K38/09 ,  Y10S514/841 ,  Y10S514/951

    摘要： In this invention, a release-delaying system is to be developed for LHRH antagonists, in particular for cetrorelix, which allows the active compound to be released in a controlled manner over several weeks by complexation with suitable biophilic carriers.The acidic polyamino acids polyglutamic acid and polyaspartic acid were selected for complexation with cetrorelix. The cetrorelix polyamino acid complexes are prepared from aqueous solutions by combination of the solutions and precipitation of the complexes, which are subsequently centrifuged off and dried over P.sub.2 O.sub.5 in vacuo. If complexes having a defined composition are to be obtained, lyophilization proves to be a suitable method. The cetrorelix-carboxylic acid complexes were also prepared from the aqueous solutions.In the random liberation system, the acidic polyamino acids poly-Glu and poly-Asp showed good release-delaying properties as a function of the hydrophobicity and the molecular mass of the polyamino acid.In animal experiments, it was possible to confirm the activity of the cetrorelix-polyamino acid complexes as a depot system in principle. It is thus possible by complexation of cetrorelix with polyamino acids to achieve testosterone suppression in male rats over 600 hours. The release of active compound here can be controlled by the nature and the molecular mass of the polymers.

    摘要翻译： 在本发明中，将开发用于LHRH拮抗剂，特别是西曲瑞克的释放延迟系统，其允许活性化合物在几周内以适当的生物亲和载体络合以受控的方式释放。 选择酸性聚氨基酸聚谷氨酸和聚天冬氨酸与西曲瑞克络合。 由溶液的组合和络合物的沉淀通过水溶液制备西曲瑞克聚氨基酸复合物，随后将其离心并真空干燥P2O5。 如果要获得具有限定组成的复合物，则冻干证明是合适的方法。 也由水溶液制备西曲瑞克 - 羧酸络合物。 在随机释放系统中，酸性聚氨基酸poly-Glu和poly-Asp显示出作为聚氨基酸的疏水性和分子量的函数的良好的释放延迟性质。 在动物实验中，原则上可以确认西曲瑞克 - 聚氨基酸复合物作为贮库系统的活性。 因此，通过将西曲瑞克与聚氨基酸络合，可以在600小时内在雄性大鼠中实现睾酮抑制。 这里的活性化合物的释放可以通过聚合物的性质和分子量来控制。