毛兰素TPGS/F68混合胶束的制备及质量评价  

Preparation and quality evaluation of Erianin TPGS/F68 mixed micelles

作　　者：张艺雯 宋宗辉 王诗华 于波涛 ZHANG Yiwen;SONG Zonghui;WANG Shihua;YU Botao(College of Medicine,Southwest Jiaotong University,Chengdu,Sichuan,610031 P.R China;Department of Pharmacy,General Hospital of Western Theater Command,Chengdu,Sichuan,610083 P.R China)

机构地区：[1]西南交通大学医学院,四川成都610031 [2]西部战区总医院药剂科,四川成都610083

出　　处：《华西药学杂志》2021年第2期154-158,共5页West China Journal of Pharmaceutical Sciences

摘　　要：目的制备毛兰素混合胶束,评价该胶束的质量,并考察其体外释药特性。方法采用薄膜分散法,以聚乙二醇1000维生素E琥珀酸酯、泊洛沙姆188为载体,制备毛兰素混合胶束。采用正交试验,以包封率为指标优化制备工艺;以临界胶束浓度、粒径等作指标对混合胶束的表征;考察混合胶束的体外释药特性。结果毛兰素混合胶束的最佳处方为:毛兰素10 mg、聚乙二醇1000维生素E琥珀酸酯30 mg、泊洛沙姆18810 mg、乙醇10 m L、超纯水10 m L,水化温度35℃、60 r·min-1搅拌20 min;所制胶束的粒径为53.92±1.65 nm,包封率为84.97%±1.52%,载药量为16.52%±0.88%,临界胶束浓度为33.92 mg·L^(-1)。结论采用薄膜分散法制备的毛兰素混合胶束溶液各项参数符合要求,且体外释药速度较毛兰素原料药溶液更平稳。OBJECTIVE To prepare Erianin(Er)TPGS/F68 mixed micelles,and to evaluate the quality and drug release in vitro of the mixed micelles.METHODS Er mixed micelles were prepared by a film-thin hydration method with D-α-tocopherol polyethyleneglycol 1000 succinate and poloxamer188 as the carriers,the preparation technology was optimized by orthogonal test with the entrapment efficiency as the index.The characterizations of the micelles were measured by critical micelle concentration,diameter of particles,the drug release in vitro of the mixed micelles was evaluated.RESULTS The optimized preparation of the mixed micelles was as follow:Er of 30 mg,D-α-tocopherol polyethyleneglycol 1000 succinate of 30 mg,poloxamer 188 of 10 mg,ethanol of 10 m L,ultrapure water of 10 m L,hydration temperature of 35℃,stirring rate of 60 r·min^(-1),and stirring time of 20 min.The average particle size of micelles was 53.92±1.65 nm,the average entrapment efficiency was84.97%±1.52%,the average drug loading efficiency was 16.52%±0.88%,and the critical micelle concentration was 33.92 mg·L-1.CONCLUSION The characterizations of the Er mixed micelles were up to the standard,and the rate of drug release in vitro was gentler than Er solution.

关 键 词：毛兰素 混合胶束 聚乙二醇1000维生素E琥珀酸酯 处方工艺 薄膜分散法 质量评价 临界胶束浓度 体外释药特性 

分 类 号：R94[医药卫生—药剂学]