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Use of a conjugate of polyethylene glycol with a local anesthetic in non-narcotic analgesia

机译:在非麻醉镇痛中使用聚乙二醇的缀合物与局部麻醉剂

摘要

The invention discloses use of a conjugate of polyethylene glycol and a local anesthetic in non-anesthetic analgesia. A local anesthetic is prepared into a prodrug or a sustained release preparation, wherein a high molecular polymer such as polyethylene glycol in the prodrug is covalently bonded with a local anesthetic, and auxiliary materials with a sustained release effect in the sustained release preparation are non-covalently bonded to the local anesthetic. After administration, there is no anesthesia and analgesic effect before the release of the free local anesthetic. After the free local anesthetic is released, an analgesic effect is achieved. And the prodrug or the sustained-release preparation of the local anesthetic of the present invention releases the drug slowly, and renders the drug concentration kept stable and long-lasting in the effective concentration range of non-narcotic analgesia, and the long-acting non-anesthetic analgesic effect can be achieved while significantly reducing the clinical adverse reactions of local anesthetics and reducing the number of administrations. The effectiveness of the drug is greatly enhanced and the clinical application range of local anesthetics is expanded.
机译:本发明公开了使用聚乙二醇和局部麻醉剂在非麻醉镇痛中的用途。将局部麻醉剂制备成前药或持续释放制剂,其中前药中的高分子聚合物如聚乙二醇与局部麻醉剂共价键合,并且在持续释放制剂中具有持续释放效果的辅助材料是非的与局部麻醉剂共价键合。在给药后,在自由局部麻醉剂释放之前没有麻醉和镇痛作用。释放自由局部麻醉后,实现镇痛作用。和本发明局部麻醉剂的前药或持续释放制剂缓慢释放出来,并且呈现出在非麻醉镇痛的有效浓度范围内的药物浓度保持稳定和持久,以及长效的非 - 致癌镇痛效果可以实现,同时显着降低局部麻醉剂的临床不良反应并减少施用的次数。药物的有效性大大提高,扩大了局部麻醉剂的临床应用范围。

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