阿苯达唑-聚乙二醇6000固体分散体壳聚糖微球的制备与药剂学性质研究

目的:制备阿苯达唑-聚乙二醇6000(PEG)固体分散体壳聚糖微球并评价其性质。方法:以阿苯达唑-PEG固体分散体(ASD)为主体,壳聚糖为载体,采用乳化交联法制备ASD壳聚糖微球;采用电镜、红外光谱、X衍射分析法等对微球进行表征并考察其药剂学性质;动态透析法研究微球的体外释放特性。结果:所制得微球形态圆整,粒径分布均匀,平均粒径约(210±3.8)μm,载药量(6.42±0.32)%,包封率(57.86±0.74)%;红外光谱、X衍射分析法证明药物成功包载于微球中;微球在醋酸盐溶液(pH3.5)介质中的释放情况遵循Higuchi方程,可持续释放400h以上。结论:本法制备微球工艺稳定,所制微球具有显著的缓释效果。

Study on Preparation and Pharmaceutical Characteristics of Albendazole-PEG6000 Solid Dispersions-chitosan Microspheres

OBJECTIVE:To prepare Albendazole-PEG6000 solid dispersions(ASD)-chitosan microspheres,and to evaluate the property of it.METHODS:ASD chitosan microspheres were prepared by emulsion cross-linking technique using ASD as main component and chitosan as carrier.Superficial characteristics and pharmaceutical property of microspheres were investigated by electronic microscope,IR-spectrum and X-ray diffraction.Dynamic dialysis system was adopted to study the drug release in vitro.RESULTS:The microspheres were spherical in shape and even in particle size.The mean diameter was(210±3.8) μm.The drug-loading amount and encapsulated efficiency of microspheres were(6.42±0.32)% and(57.86±0.74)%.IR-spectrum and X-ray diffraction indicated drug had been included in microspheres successfully.The release behavior of ABZ-PEG6000-CS-MS in acetate was in line with Higuchi model lasting for more than 400 h.CONCLUSION:The optimized technology presents good stability and excellent effect of sustained drug release.