正丁苯酞-聚乳酸聚羟基乙酸微球的制备及性能评价  

Preparation and properties evaluation of N-butylphthalide-PLGA microspheres

作　　者：米雷[1] 袁志根[1] 谭赞[1] 艾缘[1] 付三清[1] 刘益锋 MI Lei;YUAN Zhigen;TAN Zan;AI Yuan;FU Sanqing;LIU Yifeng(Department of Orthopedics Trauma, The Second People’s Hospital of Hunan Province, Changsha 410007, China)

机构地区：[1]湖南省第二人民医院创伤骨科

出　　处：《西部医学》2019年第8期1170-1173,1177,共5页Medical Journal of West China

基　　金：湖南省自然科学基金青年基金(2018JJ3283)

摘　　要：目的优选正丁苯酞-聚乳酸聚羟基乙酸(PLGA)微球的制备工艺,并对制备微球的性能进行检测。方法使用O/W型乳化溶剂挥发法制备正丁苯酞-PLGA微球,以载药量、包封率为观察指标,通过单因素实验优选制备工艺,并观察体外释药性能。采用生物显微镜观察微球的表面形态并测量粒径。结果最佳制备工艺为投药量15mg,PLGA 50mg,聚乙烯醇质量分数为2%,搅拌转速为700rpm。正丁苯酞的载药量(14.49±0.56),包封率(82.89±1.46)。所制备的微球光滑圆整、粒径均一,平均粒径约为(23.6±0.87)nm。体外释药实验表现为突释。结论采用O/W型乳化溶剂挥发法初步制备了正丁苯酞-PLGA微球,优选的制备工艺条件稳定,制备方法重现性良好。ObjectiveTo select the best technology for the preparation of N-butylphthalide (NBP)-Poly (polylactic acid) polyglycolic acid copolymer (PLGA) microspheres and evaluate its properties. MethodsO/W emulsified solvent evaporation method was used to prepare the microspheres. Drug loading and encapsulation efficiency were the indexes. The signal factor tests were used to optimize processes of preparation, and in vitro release was investigated. Biomicroscope was used to observe the surface and measure particle size of microspheres. ResultsOptimum processes of preparation were determined, N-butylphthalide dosage of 15mg, PLGA50/50 amount of 50mg, polyvinyl alcohol(PVA) amount of 2.0%, stirring speed of 700rpm. The drug loading and encapsulation efficiency were 14.49±0.56 and 82.89 ± 1.46. The microspheres were smooth and round, uniform-sized. Average particle size was 23.6±0.87nm. The release of drug in vitro was sudden release. ConclusionNBP-PLGA microspheres can be prepared by O/W emulsified solvent evaporation method. This optimized process is conditionally stable, and the reproducibility of the preparation method is good.

关 键 词：正丁苯酞 PLGA 微球 制备 性能 

分 类 号：R944.9[医药卫生—药剂学]