Patent ID: 6096834
Filing Date: 2000-08-01
Classification: A61K,C08F

Abstract:
A method for preparing a crosslinked polymeric selectively hydrolyzable delivery system for an active ingredient, said active ingredient containing a moiety, selected from the group consisting of hydroxyl, carboxyl, amino, mercapto and enolizable carbonyl moiety; said method comprising the steps of(a) providing (i) the active ingredient, (ii) a linker, and (iii) a crosslinked polymer;(b) forming:(1) a combination of (i) and (ii) by attaching the active ingredient to the linker through a hydrolyzable covalent bond formed with the hydroxyl, carboxyl, amino, mercapto or enolizable carbonyl moiety of the active ingredient to form an ester, carboxylic acid anhydride, amide, thioester or enol ester or(2) a combination of (ii) and (iii) by forming a linker-polymer covalent bond selected from the group consisting of a nitrogen-carbon bond and a phosphorus-carbon bond between the linker and subunits of the crosslinked polymer; and(c) forming the delivery system by(1) forming the linker-polymer covalent bond between the combination of (I) and (ii) and subunits of the crosslinked polymer; or(2) attaching the active ingredient to the combination of (ii) and (iii) through the hydrolyzable covalent bond.