A preparation
system of the
palonosetron sustained-release microspheres comprises
palonosetron or salt derivatives thereof, an
organic solvent, a
polymer sustained-release material, an emulsifier, a pH
regulator and a freeze-
drying protective additive, and the
palonosetron sustained-release microspheres are characterized in that D90 of the palonosetron sustained-release microspheres is 15-40 [mu] m, the
polymer sustained-release material is a
lactide-glycolide
copolymer, and D90 of the palonosetron sustained-release microspheres is 1-10 [mu] m. The
molar ratio of
polylactic acid to polyglycolic acid in the
lactide-glycolide
copolymer is (40-60): (40-60), and the weight-average molecular weight of the
lactide-glycolide
copolymer is 7-38 kDa. The palonosetron sustained-release
microsphere provided by the invention is high in
drug loading capacity and encapsulation efficiency, good in 7-day sustained-release effect, obvious in
vomiting stopping effect and high in
bioavailability.