Preparation and Quality Control of Aspirin-β-cyclodextrin-PLGA Microspheres / 中国药房

ABSTRACT

OBJECTIVE:To prepare aspirin-β-cyclodextrin-PLGA microspheres,and control its quality. METHODS:Aspirin-β-cy-clodextrin inclusion complexes were firstly prepared,and then aspirin-β-cyclodextrin-PLGA microspheres were prepared by emul-sion-solvent evaporation method. The morphology and particle size of microspheres were detected,and entrapment efficiency and accu-mulative release rate were calculated. With entrapment efficiency as index,orthogonal test was adopted to optimize stirring speed,PVA concentration,PVA volume and feed ratio. RESULTS:The optimal formulation was as follows as stirring speed of 4 000 r/min,PVA concentration of 3%(g/100 ml),PVA volume of 30 ml,feed ratio of 1∶10. Prepared microspheres were round and smooth in appear-ance. Entrapment efficiency of the microspheres was (41.79 ± 1.09)%. The diameter were regular and ranged 0.5-127.5 μm. As drug-loaded microspheres degraded,the release of aspirin was slow and its accumulative release rate was 83%within 600 h. CONCLU-SIONSAspirin-β-cyclodextrin-PLGA microspheres are prepared successfully with regular morphology and good sustained-release.