The present invention provides a composition comprising an opioid agonist, and a polymer-antagonist conjugate. The polymer-antagonist conjugate preferably does not hydrolyze upon administration to a patient, and does not bind to the opioid receptors. The covalent bond between the polymer and the antagonist in the conjugate is broken over a defined period of time to release the antagonist into the formulation. The released antagonist attenuates the liking of the agonist, thereby eliminating the incentive to the diversion of the medicines.
本发明提供了一种由阿片激动剂和聚合物-拮抗剂共轭物组成的组合物。聚合物-拮抗剂共轭物在给患者用药时最好不会
水解,也不会与阿片受体结合。聚合物与拮抗剂共轭物之间的共价键会在一定时间内断裂,从而将拮抗剂释放到制剂中。释放出的拮抗剂会减弱激动剂的药效,从而消除药物转移的诱因。