Patent ID: 7163698
Filing Date: 2007-01-16
Classification: A61K,B82Y

Abstract:
1. A sustained controlled release system consisting of a drug molecule to be released directly conjugated to a biodegradable polyester polymer via a covalent bond, wherein the conjugation is carried out after activating the biodegradable polyester polymer by mixing with coupling agents, bases and optionally additives, wherein the coupling agents are selected from the group comprising bis(2-oxo-3-oxazolydinyl)phosphonic chloride (BOP-Cl), bromo-tris-pyrrolidino-phosphonium hexafluorophosphate (PyBroP), benzotriazol-1-yl-oxy-tris-pyrrolidino-phosphonium hexafluorophosphate (PyBOP), 2-(1H-benzotriazol-1-yl)-1,1,3,3-tetramethyl-uronium hexafluorophosphate (HBTU), dicyclohexyl carbodiimide, disuccinimidyl carbonate, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide (EDC), bis(2-oxo-3-oxazolydinyl)phosphin, diisopropyl carbodiimde (DIPC), 2-(1H-benzotrioxazolyl)-1,1,3,3-tetramethyl-uronium tetrafluoroborate (TBTU), 2-(5-norboren)-2,3-dicarboxyimido)-1,1,3,3-tetramethyluronium tetrafluoroborate (TNTU), para-nitrophenylchloroformate, and O-(N-succinimidyl)-1,1,3,3-tetramethyluronium tetrafluoroborate (TSTU), and wherein the bases are selected from the group consisting of triethylamine, N-methylmorpholine, pyridine, 1,8-diazabicyclo[5,4,0]-undec-7-ene, N,N-dimethyl aminopyridine, and N,N-diisopropyl ethylamine.