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AMINO ACID AND PEPTIDE PRODRUGS OF OPIOID ANALGESICS WITH REDUCED GI SIDE-EFFECTS

机译:减轻胃肠道副作用的阿片类药物的氨基酸和肽类产品

摘要

The present invention relates to methods for reducing gastrointestinal side effects in a subject, the gastrointestinal side effects being associated with the administration of an opioid analgesic. The methods comprise orally administering an opioid prodrug or pharmaceutically acceptable salt thereof to a subject, wherein the opioid prodrug is comprised of an opioid analgesic covalently bonded through a carbamate linkage to a peptide of 1-5 amino acids in length, and wherein upon oral administration, the prodrug or pharmaceutically acceptable salt minimizes at least one gastrointestinal side effect associated with oral administration of the opioid analgesic alone. Compositions for use with the method are also provided.
机译:本发明涉及用于减轻受试者的胃肠道副作用的方法,该胃肠道副作用与阿片类镇痛药的施用有关。所述方法包括向受试者口服给予阿片样物质前药或其药学上可接受的盐,其中所述阿片样药物前体由通过氨基甲酸酯键共价键合至长度为1-5个氨基酸的肽的阿片样镇痛剂组成,并且其中在口服时,前药或药学上可接受的盐使与单独口服阿片类镇痛药有关的至少一种胃肠道副作用减至最小。还提供了与该方法一起使用的组合物。

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