壳寡糖修饰的盐酸川芎嗪mPEG-PLGA微球的制备及体外释放特性  

Preparation and in vitro release characteristics of tetramethylpyrazine hydrochloride-loaded mPEG-PLGA microspheres modified with chitosan oligosaccharide

作　　者：吴铄珺 刘文雅[2] 王曙东[2] WU Shuo-jun;LIU Wen-ya;WANG Shu-dong(Pharmacy Department,Nanjing University of Chinese Medicine,Nanjing 210046,Jiangsu,China;Departmentof Pharmaceutical Preparation,General Hospital of Eastern Theater Command,PLA,Nangjing 210002,Jiangsu,China)

机构地区：[1]南京中医药大学药学院,南京210046 [2]东部战区总医院(原南京军区南京总医院)制剂科,南京210002

出　　处：《东南国防医药》2019年第3期267-272,共6页Military Medical Journal of Southeast China

摘　　要：目的以单甲氧基聚乙二醇-聚乳酸羟基乙酸共聚物(mPEG-PLGA)为载体制备盐酸川芎嗪(TMPH)微球,用壳寡糖(COS)对微球进行修饰,并对其包封前后的体外药物释放行为进行考察。方法采用复乳-溶剂挥发法制备壳寡糖修饰的盐酸川芎嗪缓释微球,通过单因素试验,以包封率为评价指标,考察影响微球质量的因素,采用正交试验进行优化,筛选出最佳的处方,并进行体外释药性能的考察。结果mPEG-PLGA浓度为50g/L,药物浓度为30g/L,内水相/油相比为1∶10,外水相油相比为4∶1,最佳处方制备的盐酸川芎嗪微球表面光滑圆整,包封率在60%以上。经壳寡糖修饰后微球突释效应减少。结论以mPEG-PLGA为载体材料,采用复乳-溶剂挥发法可以制备包封率较高的盐酸川芎嗪微球,壳寡糖修饰有减小突释效应的作用。Objective To prepare tetramethylpyrazine hydrochloride microspheres with methoxy poly(ethylene glycol)-poly (lactide-co-glycolide)copolymer(mPEG-PLGA).Microspheres were modified with chitosan oligosaccharide(COS).The in vitro drug release behavior were investigated before and after the modification.Methods Tetramethylpyrazine hydrochloride microspheres modified with COS were prepared by emulsion-solvent evaporation method.The influence of formulation and manufacture was studied by the single factor experiments.The optimal formulation was verified by Orthogonal experimental.The characteristics of drug release were determined in vitro.Results The optimum prescription was 50 g/L mPEG-PLGA,30 g/L Ligustrazine,internal water phase∶oil phase=1∶10,external water phase∶oil phase=4∶1.The surface of Ligustrazine microspheres prepared with optimal prescription was with a good appearance without adhesions.The encapsulation efficiency was over 60%.The burst effect of microspheres modi- fied with COS was decreased.Conclusion Emulsion-solvent evaporation method was developed to prepare mPEG-PLGA tet- ramethylpyrazine microspheres with higher entrapment efficiency.The microspheres modified with COS could decrease burst ef- fect.

关 键 词：盐酸川芎嗪 壳寡糖 单甲氧基聚乙二醇-聚乳酸羟基乙酸共聚物 微球 体外释放 

分 类 号：R944.9[医药卫生—药剂学]