COMPOSITIONS COMPRISING ENZYME-CLEAVABLE OPIOID PRODRUGS AND INHIBITORS THEREOF

摘要

PROBLEM TO BE SOLVED: To provide a pharmaceutical composition which can properly administer an opioid which is susceptible to misuse, abuse, or overdose without controlling the use and possession.SOLUTION: The invention relates to a pharmaceutical composition containing: an opioid prodrug in which an opioid is covalently bound to a promoiety (protecting group) comprising a gastrointestinal (GI) enzyme-cleavable moiety, and enzymatically-controlled release of opioid is mediated by cleavage of the enzyme-cleavable moiety by the GI enzyme; and a GI enzyme inhibitor which interacts with the GI enzyme which mediates enzymatically-controlled release of the opioid after ingestion.