摘要
目的制备蛇床子素自乳化释药并评价其质量。方法通过溶解度和伪三元相图实验确定蛇床子素自乳化释药系统所用油相、表面活性剂和助表面活性剂的种类和用量范围,通过D-最优混合实验设计优化蛇床子素自乳化释药系统的处方;评价了蛇床子素自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电位以及体外溶出情况。结果蛇床子素自乳化释药系统的处方组成为:Capmul MCM C8作为油相、Tween 20作为表面活性剂,PEG400作为助表面活性剂,最优比例为:46.9∶29.9∶23.2。加水稀释蛇床子素自乳化释药可快速形成澄清、透明状微泛蓝光液体;透射电镜下可观察到其为圆整、规则球状;平均粒径为(31.8±1.6)nm,多分散指数为(0.164±0.014),zeta电位为-(26.1±1.4)m V;自乳化释药系统中蛇床子素释放迅速,在45 min内药物可到90%以上。结论制备的自乳化释药系统可以显著提高蛇床子素的体外溶出速度,有望成为蛇床子素的新型给药制剂。
Objective To prepare osthole self-emulsifying drug and evaluate its quality. Methods Solubility and pseudo-ternary phase diagram experiment were used to determine the types and dosage of oily phase, surfactant and co-surfactant used in osthole self-emulsifying drug delivery system. The formulation of osthole self- emulsifying drug delivery system was optimized by D-optimal mixture experimental design. The appearance, microscopic morphology, particle size distribution, zeta potential and dissolution in vitro of osthole self- emulsifying drug delivery system after dilution with water were evaluated. Results The formulation of osthole self-emulsifying drug delivery system consisted of Capmul MCM C8 （the oil phase）, Tween 20 （the surfactant）, and Polyethylene glycol 400 （the co-surfactant） at the optimal ratio of 46.9 ： 29.9 ： 23.2. The osthole self- emulsifying drug delivery rapidly formed a clear and transparent blue liquid, which the transmission electron microscopy showed was round and regular sphere with an average diameter of （31.8±1.6） nm, polydispersity index （PDI） of （0.164±0.014）, and zeta potential of -（26.1±1.4） inV. The osthole was released rapidly in the self-emulsifying drug delivery system and completely dissolved within 45 min. Conclusion The prepared self- emulsifying drug delivery system can significantly improve the osthole dissolution rate, which is expected to be a new drug delivery system of osthole.
作者
果秋婷
李昱
冯华
王芳
GUO Qiu-ting, LI Yu, FENG Hua, WANG Fang(Xianyang Vocational Technical College, Shaanxi Xianyang 71200)
出处
《中南药学》
CAS
2018年第7期958-962,共5页
Central South Pharmacy
基金
咸阳职业技术学院项目(No.2017KYC01)
2017年陕西省中医药管理局项目(No.JCPT056)
关键词
蛇床子素
自微乳化释药系统
D-最优混合实验设计
osthole
self-emulsifying drug delivery system
D-optimal mixture experimental design
