发明授权
US6022860A 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
- 专利标题: Immobilized and activity-stabilized complexes of LHRH antagonists and processes for their preparation
- 专利标题(中): LHRH拮抗剂的固定和活性稳定复合物及其制备方法
-
申请号: US48244申请日: 1998-03-26
-
公开(公告)号: US6022860A公开(公告)日: 2000-02-08
- 发明人: Jurgen Engel , Wolfgang Deger , Thomas Reissmann , Gunter Losse , Wolfgang Naumann , Sandra Murgas
- 申请人: Jurgen Engel , Wolfgang Deger , Thomas Reissmann , Gunter Losse , Wolfgang Naumann , Sandra Murgas
- 申请人地址: DEX Dresden
- 专利权人: Asta Medica Aktiengesellschaft
- 当前专利权人: Asta Medica Aktiengesellschaft
- 当前专利权人地址: DEX Dresden
- 优先权: DEX19712718 19970326
- 主分类号: A61K47/48
- IPC分类号: A61K47/48 ; A61K38/09 ; A61K38/24 ; A61K45/00 ; A61P35/00 ; A61K38/00
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.
公开/授权文献
- USD376896S Repeat pattern of a shoe sole 公开/授权日:1996-12-31
信息查询