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Controlled drug delivery system using the conjugation of drug to biodegradable polyester

  • US 6,589,548 B1
  • Filed: 11/14/2000
  • Issued: 07/08/2003
  • Est. Priority Date: 05/16/1998
  • Status: Expired due to Fees
First Claim
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1. A method for manufacturing a sustained controlled release system wherein a drug molecule to be released is directly conjugated to a biodegradable polyester polymer via a covalent bond, comprising the steps of:

  • 1) forming an activated polymer solution by activating a biodegradable polyester polymer by mixing with coupling agents selected from the group consisting of 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-tetramethyluronium hexafluorophosphate (HBTU), dicyclohexyl carbodiimide, disuccinimidyl carbonate, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimde (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), bases, and optionally additives;

    2) directly conjugating a drug molecule with said polymer by adding said drug molecule to the activated polymer solution of step 1, and 3) purifying the polymer-molecule conjugate resulting from step 2.

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