毛蕊花苷固体脂质纳米粒的处方优选及其质量评价  

Preparation Optimization and Quality Evaluation of Verbascoside Solid Lipid Nanoparticles

作　　者：丁立新[1] 杨珊珊[1] 张楠楠[1] 李焕[1] 李冬阳[1] 王丽红[1] 

机构地区：[1]佳木斯大学药学院黑龙江省生物药制剂重点实验室,黑龙江佳木斯154007

出　　处：《中国药房》2014年第3期231-234,共4页China Pharmacy

基　　金：黑龙江省教育厅科学技术研究项目(No.12521559);佳木斯大学大学生科技创新项目(No.xs2013-127);佳木斯大学科学技术重点项目(No.Sjz2012-24)

摘　　要：目的:优选毛蕊花苷(VER)固体脂质纳米粒(SLN)的处方,并对VER-SLN质量进行评价。方法:采用乳化超声分散法制备VER-SLN,以包封率为评价指标,以药脂质量比、单硬脂酸甘油脂用量、泊洛沙姆188用量、豆磷脂用量为考察因素,通过正交试验对处方进行优化,同时以载药量、粒径、Zeta电位、包封率、稳定性及体外累积释放度为指标评价其质量。结果:最佳制备处方为药脂质量比为1∶75,单硬脂酸甘油脂的用量为0.6 g,泊洛沙姆188用量为0.5 g,豆磷脂用量为0.2 g。所制得的VER-SLN外观形态圆整,粒度分布均匀,平均粒径为(109±17)nm,Zeta电位为(-23±0.91)mV,平均包封率为96.66%,平均载药量为2.27%。体外释放结果表明,VER原料药体外8 h累积释放完全,VER-SLN体外4 h累积释放率为47.2%,48 h可达到92.9%。结论:该制剂处方设计合理,制备工艺稳定,乳化超声分散法制备的VER-SLN质量符合要求,可达到使药物缓慢释放的效果。OBJECTIVE： To optimize the prescription of Verbascoside solid lipid nanoparticles （VER-SLN） and to evaluate the quality of it. METHODS： VER-SLN was prepared by emulsion ultrasound dispersing method. The formulation of VER-SLN was op- timized by orthogonal design with the entrapment efficacy as index using the ratio of drug to lipid, amount of glyceryl monostea- rate, poloxamer 188 and fabaceous lecithin as factors. The quality of preparation was evaluated with drug-loading amount, particle size, Zeta potential, entrapment efficiency, stability and in vitro drug release rate as index. RESULTS： The optimal formulation was as follows： drugtolipid ratio of 1：75 （m/m）, the amount of glycerol glyceryl monostearate of 0.6 g, the amount of poloxamer 188 of 0.5 g and the amount of fabaceous lecithin of 0.2 g. The obtained VER-SLN was round and smooth particles with average size of （109 ± 17） nm, Zeta potential of （- 23 ± 0.91） mV, average entrapment efficiency of 96.66%, and average drug-loading amount of 2.27%. VER solution was released completely within 8 h, and accumulative release rate of VER-SLN was 47.2% at 4 h and reached 92.9% at 48 h. CONCLUSIONS： The formulation is reasonable and stable. VER-SLN prepared by emulsification ultrasonic dispersion method is up to quality standard and can reach sustained-release effects.

关 键 词：毛蕊花苷 固体脂质纳米粒 质量研究 体外累积释放度 

分 类 号：R284.2[医药卫生—中药学] R283[医药卫生—中医学]