To provide a compound and composition stable before exposing to a biological fluid such as plasma, etc., relatively insoluble in the biological fluid such as plasma, etc., and returning to at least one kind of analgesic compounds or compositions in dissolving into the biological fluid such as plasma, etc.
The pharmaceutically active compound comprises two independently active analgesic moieties covalently joined through a physiologically labile linker. A preferred embodiment comprises an opioid, such as morphine, covalently linked to at least one analgesic compound selected from the group consisting of an opioid or a non-opioid compound through a physiologically labile linker. Suitable covalent linkers are covalently bonded to the two independently active analgesic compounds through one or more lactone, lactam, or sulfonamide linkages. Suitable linkers include endogenous carboxylate, amide, or sulfonamide moieties, and exogenous moieties that form the lactone, lactam or sulfonamide linkages.
COPYRIGHT: (C)2010,JPO&INPIT
SMITH THOMAS J
CYNKOWSKI TADEUSZ
CYNKOWSKA GRAZYNA
MICKUNAS EDMUND
