基于“药辅合一”的紫杉醇-薏苡仁油微乳的制备及含量测定  

Preparation and Detemination of Paclitaxel-Coix Seed Oil Microemulsion Based on the Unity of Medicine and Adjuvant

作　　者：陈云艳 马睿 卜晓阳 周凌云 钱智磊 CHEN Yunyan;MA Rui;BU Xiaoyang;ZHOU Lingyun;QIAN Zhilei(School of Pharmacy,Wannan Medical College,Wuhu 241002,China;The Affiliated Brain Hospital of Nanjing Medical University,Nanjing 210029,China)

机构地区：[1]皖南医学院药学院,芜湖241002 [2]南京医科大学附属脑科医院,南京210029

出　　处：《中国现代应用药学》2023年第8期1064-1069,共6页Chinese Journal of Modern Applied Pharmacy

基　　金：安徽省自然科学基金(2108085QH370);安徽省高等学校自然科学研究项目(KJ2020A0596,KJ2020A0608);皖南医学院校中青年科研基金(wk202008)。

摘　　要：目的采用以薏苡仁油替代微乳的油相制备紫杉醇-薏苡仁油微乳,筛选紫杉醇-薏苡仁油微乳制备的最佳处方,并进行紫杉醇含量测定的方法学考察。方法选用不同的乳化剂和助乳化剂,采用水滴定法绘制出伪三元相图,筛选出最佳乳化剂和助乳化剂,通过观察成乳状态,并以包封率和载药量为指标,筛选出最佳处方制备得到紫杉醇-薏苡仁油微乳,并测定其zeta电位以及粒度分布。结果紫杉醇-薏苡仁油微乳处方为紫杉醇10 mg,HS 15600 mg,PEG400200 mg,薏苡仁油200 mg,包封率为(98.9±1.26)%,载药量为(0.56±0.05)%,紫杉醇-薏苡仁油微乳粒径为(35.23±1.20)nm,zeta电位为(–2.93±0.69)mV。结论本研究成功制备得到了紫杉醇-薏苡仁油微乳,所得微乳外观完整均一,粒径较小,包封率高,具有一定的药物缓释功能。OBJECTIVE To prepare paclitaxel-Coix seed oil microemulsion using oil phase replacing microemulsion with Coix seed oil,to screening the optimal formula for the preparation of paclitaxel-Coix seed oil microemulsion and to conduct methodological studies on the determination of paclitaxel content.METHODS Different emulsifiers and auxiliary emulsifiers were selected,and water titration method was used to draw the pseudo ternary phase diagram,and the best emulsifier and auxiliary emulsifier were selected.By observing the milk formation,and the encapsulation efficiency and loading efficiency were selected as the indexes,the optimal formula to obtain paclitaxel-Coix oil microemulsion,and the zeta potential and particle size distribution were determined.RESULTS The formulation of paclitaxel-Coix seed oil microemulsion was paclitaxel(10 mg),HS 15600 mg and polyethylene glycol 400200 mg,Coix seed oil 200 mg and respectively.The encapsulation efficiency and drug loading efficiency of paclitaxel-Coix seed oil microemulsion were(98.9±1.26)%and(0.56±0.05)%,respectively.The paclitaxel-Coix seed oil microemulsion particle size was(35.23±1.20)nm and zeta potential was(–2.93±0.69)mV.CONCLUSION Paclitaxel-Coix seed oil microemulsion is successfully prepared in this study,which has a complete and uniform appearance,small particle size,high encapsulation efficiency,and certain drug sustained-release function.

关 键 词：紫杉醇 薏苡仁油 微乳 含量测定 

分 类 号：R944[医药卫生—药剂学]