| 摘要 |
Production of microsphere composition for sustained release of water-soluble drug (I) involves: (a) emulsifying aqueous solution of (I) in solution of d,l-lactide-co-glycolide matrix copolymer (II) in chlorinated hydrocarbon; (b) emulsifying obtained fine, homogeneous first emulsion in aqueous external phase containing surfactant, thickener and osmotic agent; and (c) extracting/evaporating solvent. Production of a microsphere composition for sustained release of a water-soluble drug (I) involves: (a) emulsifying an aqueous solution of (I) in a solution of d,l-lactide-co-glycolide matrix copolymer (II) (average molecular weight 40-80 kDa; lactic/glycolic acid ratio 50/50 to 80/20) in a chlorinated hydrocarbon; (b) emulsifying the obtained fine, homogeneous first emulsion in an aqueous external phase containing surfactant, thickener and osmotic agent; and (c) extracting/evaporating the solvent to give microspheres, which are filtered off, washed and dried. An Independent claim is included for microspheres obtained by the process, which release (I) continuously over a period of more than 2 (preferably at least 3) months. |
