COMPLEXES OF THE LHRH CETRORELIX ANTAGONIST WITH POLYAMINO ACIDS, AS WELL AS PROCEDURE FOR PREPARATION.

摘要

The invention relates to a delay system for LHRH antagonists, especially cetrorelix, based on complexation with suitable biophilic excipients that makes possible a specific release for a target of the active substance over a period of several weeks. For complexation with cetrorelix, acidic polyamino acids, polyasparaginic acids and polyglutamine acids are selected. Cetrorelix polyamino acid complexes are produced from aqueous solutions by combining the solutions and precipitating the complexes that are subsequently centrifuged and dried under vacuum by P {sub, 2} O {sub, 5}, lyophilization has been shown to be a proper procedure Acidic, polyglutamic and polyasparagine polyamino acids show delay properties in static release systems depending on the hydrophobicity and molar mass of polyamine acids. Animal tests have demonstrated the main efficacy of cetrorelix polyamine acid complexes as a deposition system. By complexing cetrorelix with polyamine acids, testosterone suppression can be achieved in female rats over a period of 600 hours. In this way, the release of the active substance can be controlled according to the type of polymer and the molar mass.