摘要
该文研究了青蒿琥酯聚乳酸微球的制备工艺及体外释放行为,以制备一种适合肝动脉栓塞的青蒿琥酯给药方式。以聚乳酸为材料,聚乙烯醇为乳化剂,采用O/W乳化-溶剂挥发法制备青蒿琥酯聚乳酸微球,并对制备工艺进行优化。以载药量、包封率、粒径为指标,对聚乳酸浓度、聚乙烯醇浓度、药载比、搅拌速度等进行单因素考察,通过正交试验,确定了最佳工艺条件为聚乳酸质量分数9.0%,聚乙烯醇质量分数0.9%,药载比1∶2,搅拌速度1 000 r·min-1。并对最佳工艺进行了验证,微球粒径为(101.7±0.37)μm,载药量和包封率分别为(30.8±0.84)%,(53.6±0.62)%。研究表明该工艺合理,稳定性好,为进一步研究奠定了基础。
This study aims to investigate the preparation process and in vitro release behavior of artesunate polylactic acid mi- crospheres, in order to prepare an artesunate polylactic acid （PLA） administration method suitable for hepatic arterial embolization. With PLA as the material and polyvinyl alcohol （PVA） as the emulsifier, O/W emulsion/solvent evaporation method was adopted to prepare artesunate polylactic acid microspheres, and optimize the preparation process. With drug loading capacity, encapsulation effi- ciency and particle size as indexes, a single factor analysis was made on PLA concentration, PVA concentration, drug loading ratio and stirring velocity. Through an orthogonal experiment, the optimal processing conditions were determined as follows： PLA concentration was 9.0%, PVA concentration was 0.9% , drug loading ratio was 1：2 and stirring velocity was 1 000 r · min-1. According to the veri- fication of the optimal process, microsphere size, drug loading and entrapment rate of artesunate polylactic acid microspheres were （ 101.7 ±0. 37） μm, （30. 8 ±0. 84） %, （53.6 ±0. 62） % , respectively. The results showed that the optimal process was so reasona- ble and stable that it could lay foundation for further studies.
出处
《中国中药杂志》
CAS
CSCD
北大核心
2013年第23期4071-4075,共5页
China Journal of Chinese Materia Medica
基金
杭州市医疗科研及重点专科专病项目(20110733Q20)
关键词
青蒿琥酯
聚乳酸微球
制备工艺
正交设计
体外释放
artesunate
polylactic acid microsphere
preparation process
orthogonal design
release in vitro
