天麻苷元脂质体制备及药剂学性能研究  

Study on preparing technology of Gastrodigenin liposome

作　　者：邱红燕 刘学[1] 周雪 吴林菁[1] 肖婷[1] 茅向军 沈祥春 陶玲[1] QIU Hongyan;LIU Xue;ZHOU Xue;WU Linjing;XIAO Ting;MAO Xiangjun;SHEN Xiangchun;TAO Ling(The High Efficacy Application Engineering Center of Natural Medicinal Resources of Guizhou Province&Guiyang Joint Key Lab of Guizhou Medical University&The Higher Education Key Lab of Natural Medicinal Pharmacology and Patent Medicinal Evaluation&The Key Lab of Optimal Utilization of Natural Medicine Resources,Guiyang 550025,Guizhou,China;Guizhou Institute for Food And Drug Control,Guiyang 550004,Guizhou,China)

机构地区：[1]贵州医科大学贵州省天然药物资源高效利用工程中心&贵州医科大学-贵阳市联合重点实验室&贵州省高等学校天然药物药理与成药性评价特色重点实验室&天然药物资源优效利用重点实验室,贵州贵阳550025 [2]贵州省食品药品检验所,贵州贵阳550004 [3]贵州医科大学

出　　处：《贵州医科大学学报》2021年第10期1151-1155,1168,共6页Journal of Guizhou Medical University

基　　金：贵州医科大学药学国际科技合作基地[黔科合平台人才(2017)5802];贵州省科技厅联合学术新苗项目[黔科合平台人才(2017)5718];贵阳市科技局联合基金项目[筑科合同(2017)30-16号];贵州医科大学博士启动基金(YJ2017-30);贵州省高层次创新型人才百层次人才项目[贵州省科技厅黔科合人才(2015)4029号];贵州省科技创新团队项目[黔科合人才团队(2015)4025号];贵州省科学技术厅学术新苗培养及创新探索[黔科合平台人才(2017)5718]。

摘　　要：目的建立天麻苷元脂质体的含量测定方法并优化制备工艺。方法采用高效液相色谱法(HPLC)建立测定天麻苷元脂质体含量的方法,以包封率(EE)、平均粒径、粒径范围和多分散指数(PDI)作为评价指标,通过单因素考察,薄膜分散法制备天麻苷元脂质体,优化天麻苷元脂质体的制备工艺。结果天麻苷元脂质体最佳处方为天麻苷元-大豆磷脂-胆固醇(1∶3∶1);最佳制备工艺为40℃旋转蒸发回收有机溶剂,超纯水10 mL,40℃水合30 min,50℃超声10 min,10000 r/min高速剪切3 min,采用脂质体挤出器0.8、0.4μm滤膜分别挤出3次、0.1μm滤膜挤出7次;采用最优制备工艺即得平均粒径为150.39 nm,EE为21%,外观为微带淡蓝色乳光的半透明乳白混悬液。结论HPLC适用于天麻苷元脂质体的定量测定,单因素实验优选的制备工艺简单、可行、稳定可靠,最佳处方和工艺制备所得天麻苷元脂质体外观形态良好、粒径适中。Objective To optimize the formulation and preparation technology of Gastrodigenin liposomes and establish a method for the determination of Gastrodigenin.Methods HPLC method was used to determine the content of Gastrodigenin.Gastrodigenin liposomes were prepared by thin-film dispersion method and the preparation technology was optimized by single factor test and encapsulation efficiency(EE),average particle size,particle size range and polydispersity index(PDI)were used as evaluation indexes.Results The optimal formulation of Gastrodigenin liposomes was 1(Gastrodigenin)∶3(soybean phospholipid)∶1(cholesterol).The optimal process was as follows:forming membrane at 40℃,washing membrane with 10 mL ultra pure water,hydration at 40℃for 30 min,ultrasonic at 50℃for 10 min,high speed shearing at 10000 r/min for 3 min,filtering with 0.8,0.4μm membrane for 3 times separately,and 0.1μm membrane for 7 times by liposome extrude.The average particle size of liposomes prepared by the optimal process was 150.39 nm,the particle size distribution was single peak and narrow,and the EE was 21%.The appearance of the liposomes was milky white,translucent and with light blue opalescence.Conclusion HPLC method is suitable for the quantitative determination of Gastrodigenin.The preparation process optimized by single factor experiment is simple,feasible,stable,and reliable.The obtained Gastrodigenin liposomes have small particle size and good appearance.

关 键 词：色谱法 高压液相 脂质体 天麻苷元 包封率 制备工艺 薄膜分散法 

分 类 号：R943[医药卫生—药剂学]