依维莫司自微乳化释药系统的制备及质量评价  

Preparation and Quality Evaluation of Everolimus Self-Microemulsifying Drug Delivery System

作　　者：陈吼[1] 

机构地区：[1]陕西省杨凌职业技术学院药物与化工学院,杨凌712100

出　　处：《医药导报》2017年第5期544-548,共5页Herald of Medicine

摘　　要：目的制备依维莫司自微乳化释药系统,并评价其理化性质。方法通过考察依维莫司在不同辅料中的溶解度和辅料配伍实验,采用伪三元相图法最终确定依维莫司自微乳化释药系统的最优处方;考察依维莫司自微乳化释药系统经水稀释后形成微乳的外观、微观形态、粒径分布、Zeta电位及体外释放行为。结果依维莫司自微乳化释药系统处方组成为:油酸乙酯(油相),Solutol HS 15(乳化剂),1,2-丙二醇(助乳化剂),最佳配比为8∶1∶1。依维莫司自微乳化释药系统经水稀释后形成的微乳外观呈微泛蓝光的澄清、透明状液体;透射电镜下显示其成圆整、规则球状分布;平均粒径(48.7±25.1)nm,Zeta电位(-14.2±2.5)mV;依维莫司自微乳化释药系统在30 min内药物释放完全。结论将依维莫司制备成自微乳化释药系统可显著提高药物的体外溶出速度,为依维莫司的新剂型开发提供了理论基础。Objective To prepare everolimus self-microemulsifying drug delivery systems （Everolimus-SMEDDS） and evaluate its physicochemical properties.Methods Everolimus-SMEDDS were developed by using rational blends of components with good solubilizing ability for everolimus which were selected based on solubility investigation.Then, pseudo-ternary phase diagram was constructed to determine the self-emulsifying region.The appearance, morphology, particle size distribution, Zeta potential and in vitro drug release behavior of Everolimus-SMEDDS were investigated after being diluted by water.Results An optimal Everolimus-SMEDDS consisting of ethylis oleas, Solutol HS 15 and propylene glycol were identified, and the optimum proportion was 8∶1∶1.Upon mixing with water, Everolimus-SMEDDS formed a clear and transparent microemulsion solution with homogeneous small spherical as seen in transmission electron microscopy.Particle size and Zeta potential of Everolimus-SMEDDS were found to be （48.7±25.1） nm and （-14.2±2.5） mV, respectively.The in vitro release profile indicated that the accumulated release of everolimus in SMEDDS reached up to nearly 100% within 30 min.Conclusion The in vitro dissolution of everolimus was remarkably improved by SMEDDS.It can provide reference for the new dosage form of everolimus.

关 键 词：依维莫司 自微乳化释药系统 伪三元相图 溶出度 

分 类 号：R979.5[医药卫生—药品] TQ460.6[医药卫生—药学]