Biocompatible polymeric delivery systems for sustained release of quinazolinones.


The present invention relates to biocompatible polymeric delivery systems for controlled or sustained release of quinazolinone derivs.(I; n = 1-2; R1 = H, halo, NO2, benzo, alkyl, Ph, alkoxy; R2 = OH, acetoxy, alkoxy; R3 = H, alkenoxy carbonyl), including the compd. halofuginone. In particular the invention relates to a polymeric delivery system comprising biocompatible polymeric beads having a two-phase core and shell structure, or polymeric films, beads or complexes that provide local sustained release of the pharmacol. agent. For example, polymeric emulsion beads with core/shell structure were prepd. for controlled release of halofuginone. A water-in-oil emulsion was prepd., in which the 20% wt. internal phase contained 50 mg halofuginone HBr/mL and the oil was sunflower oil. The emulsion was prepd. by adding the aq. halofuginone soln. in to the oil which contains 2.7% wt. span 80, and homogenized. Beads were formed by a core-shell double nozzle Innotek. The shell soln. was 2.5% sodium alginate and 2.5% silica in aq. soln. [on SciFinder(R)]


CAPLUS AN 2005:961994(Patent)