摘要
目的优选制备PDLLA-PEG-PDLLA丹参酮ⅡA微球的处方和工艺条件。方法以PDLLA-PEG-PDLLA为载体材料,单因素与正交试验设计相结合,采用乳化溶剂挥发法制备丹参酮ⅡA微球,紫外分光光度法测定丹参酮ⅡA的含量,以载药量、包封率及收率为主要评价指标,进行综合加权评分,确定最佳制备处方工艺,并用扫描电镜(SEM)、激光粒度仪、傅里叶变换红外光谱扫描(FT-IR)、X射线衍射(XRD)进行表征。结果最佳处方工艺制备所得微球圆整、无粘连,结构呈片层状,平均粒径为103.5μm,跨度为0.862,载药量为(27.84±0.36)%,包封率为(77.33±2.82)%,收率为(92.59±2.22)%。FT-IR,XRD等结果表明,丹参酮ⅡA制备成微球后药物仍有晶型存在。结论采用O/W型乳化溶剂挥发法成功制备得到丹参酮ⅡA微球,所得微球具有较高的载药量和包封率。该方法简便易行,工艺稳定。
Objective To select the process conditions for preparation of PDLLA-PEG-PDLLA tanshinone ⅡA microspheres.Methods PDLLA-PEG-PDLLA as carrier material,by single factor test and orthogonal design,the microspheres were prepared by emulsion solvent evaporation method. The content of tanshinone Ⅱ A was determined by UV spectrophotometric method. The optimum preparation process were clarified by the comprehensive weighted score which was evaluated with the the drug loading,encapsulation efficiency,and yield. The quality characterization of the tanshinone ⅡA microspheres were assayed by SEM,laser particle size analyzer,FT-IR,and XRD. Results The PDLLA-PEG-PDLLA microspheres were regularly shaped and spherical,while the surface had a flakily structure. The mean particle size was 103. 5 μm,span was 0. 862,the drug loading was（ 27. 84 ± 0. 36） %,the encapsulation efficiency was（ 77. 33 ± 2. 82） % and the yield was（ 92. 59 ± 2. 22） %. The drug crystal form was still in the microspheres from FT-IR and XRD results which maybe produce a novel crystal form. Conclusion Microspheres of TA were successfully prepared by emulsion solvent evaporation method. The TA microspheres had significantly high drug loading and encapsulation efficiency. And the optimal process was simple and reasonable,which is base for further research.
出处
《时珍国医国药》
CAS
CSCD
北大核心
2017年第10期2413-2416,共4页
Lishizhen Medicine and Materia Medica Research
基金
贵州省科技计划项目(黔科合SY字[2015]3032)
贵州省科学技术基金项目(黔科合J字[2013]2039号)
高等学校大学生创新创业训练计划(No.201510660020)
贵州省普通高等学校创新团队项目(黔教合人才团队字[2014]31)
贵州省高层次创新型人才培养项目(黔科合人才[2015]4029号)
贵州省科技创新人才团队建设项目(黔科合人才团队[2015]4025号)
作者简介
徐旖旎（1983-），女（汉族），山东青岛人，贵州医科大学在读博士研究生，主要从事心血管药理研究工作．;通讯作者简介：陶玲（1975-），女（汉族），贵州贵阳人，贵州医科大学教授，硕士学位，主要从事中药药剂学研究工作．;通讯作者简介：沈祥春（1973-），男（汉族），山东临沂人，贵州医科大学教授，博士研究生导师，博士学位，主要从事中药民族药活性及效应机制、心血管系统药物药理研究工作．
