阿司匹林-β-环糊精包合物PLGA微球的制备及其质量控制

Preparation and Quality Control of Aspirin-β-cyclodextrin-PLGA Microspheres

目的：制备阿司匹林-β-环糊精包合物聚乳酸-羟基乙酸共聚物（PLGA）微球,并进行质量控制。方法：首先制备阿司匹林-β-环糊精包合物,再通过乳化溶剂挥发法制备阿司匹林-β-环糊精包合物PLGA微球,检测载药微球的形态和粒径,计算包封率和累积释放度。以包封率为指标,采用正交试验优化搅拌速度、聚乙烯醇（PVA）浓度、PVA体积、投料比。结果：最优处方工艺为搅拌速度4 000 r/min、PVA浓度3%（g/100 ml）、PVA体积30 ml、投药比1∶10。所制微球为圆球形,表面光滑,包封率为（41.79±1.09）%,粒径较为均一,粒径范围为0.5～127.5μm;随着载药微球的降解,阿司匹林的释放速度较平缓,600 h内累积释放度为83%。结论：成功制得形态规则且具有缓释作用的阿司匹林-β-环糊精包合物PLGA微球。

OBJECTIVE：To prepare aspirin-β-cyclodextrin-PLGA microspheres,and control its quality.METHODS：Aspirin-β-cyclodextrin inclusion complexes were firstly prepared,and then aspirin-β-cyclodextrin-PLGA microspheres were prepared by emulsion-solvent evaporation method.The morphology and particle size of microspheres were detected,and entrapment efficiency and accumulative 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 appearance.Entrapment efficiency of the microspheres was（41.79 ± 1.09）%.The diameter were regular and ranged 0.5-127.5 μ m.As drug-loaded microspheres degraded,the release of aspirin was slow and its accumulative release rate was 83% within 600 h.CONCLUSIONS：Aspirin-β-cyclodextrin-PLGA microspheres are prepared successfully with regular morphology and good sustained-release.