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Details for Patent: 8,133,881

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Details for Patent: 8,133,881

Title:Carbohydrate conjugates to prevent abuse of controlled substances
Abstract: The invention provides a "street-safe" version of a controlled substance that permits the therapeutically beneficial effects of the substance while reducing or eliminating the euphoric effects that lead to substance abuse. The invention provides pharmaceutical compositions comprising a controlled substance and a carbohydrate covalently bound to said controlled substance in a manner that renders said controlled substance pharmacologically inactive or substantially diminishes its activity and methods of using the same.
Inventor(s): Mickle; Travis (Coralville, IA), Piccariello; Thomas (Blacksburg, VA), Moncrief; James Scott (Christiansburg, VA), Boerth; Nancy Johnston (Blacksburg, VA), Bishop; Barney (Annandale, VA)
Assignee: Shire LLC (Florence, KY)
Filing Date:Jul 13, 2005
Application Number:11/179,801
Claims:1. An oral pharmaceutical composition comprising: hydrocodone; and a disaccharide covalently bound to the hydrocodone via an ester or carbonate bond through a hydroxyl group of the disaccharide and an oxygen atom in the hydrocodone in a manner that renders the hydrocodone pharmacologically inactive or substantially diminishes its activity until unbound hydrocodone is released.

2. An oral pharmaceutical composition comprising a disaccharide covalently bound to hydrocodone via an ester or carbonate group through a hydroxyl group of the disaccharide and an oxygen atom in the hydrocodone in a manner that renders the hydrocodone pharmacologically inactive or substantially diminishes its activity until the unbound hydrocodone is released, wherein the hydrocodone covalently bound to the carbohydrate has the formula: ##STR00012##

3. A compound of the formula: ##STR00013##
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