基于“药辅合一”的辛夷油亚微乳的制备及评价  

Preparation and evaluation of Magnolia Flos oil-loaded sub-micron emulsion based on the unification of drugs and excipients

作　　者：孟扬 徐丽芝 王欣茹 冯向阳 刘彤 叶田田 杨瑞[6] 王淑君 MENG Yang;XU Li-zhi;WANG Xin-ru;FENG Xiang-yang;LIU Tong;YE Tian-tian;YANG Rui;WANG Shu-jun(School of Pharmacy,Jiangxi University of Chinese Medicine,Nanchang 330004;Yangtze Delta Drug Advanced Research Institute,Nantong Jiangsu 226133;Jiangsu Aidinami Biopharmaceutical Co.,Ltd.,Nantong Jiangsu 226100;School of Pharmacy,Anhui University of Chinese Medicine,Hefei 230012;Shenyang Pharmaceutical University,Shenyang 110016;The Second Affiliated Hospital of Liaoning University of Traditional Chinese Medicine,Shenyang 110034;Liaoning Institute for Drug Control,Shenyang 110032)

机构地区：[1]江西中医药大学药学院,南昌330004 [2]长三角药物高等研究院,江苏南通226133 [3]江苏艾迪纳米生物医药有限公司,江苏南通226100 [4]安徽中医药大学药学院,合肥230012 [5]沈阳药科大学,沈阳110016 [6]辽宁中医药大学附属第二医院,沈阳110034 [7]辽宁省药品检验检测院,沈阳110032

出　　处：《中南药学》2024年第5期1213-1219,共7页Central South Pharmacy

基　　金：国家自然科学基金项目(No.81973494)。

摘　　要：目的 基于“药辅合一”理念优化辛夷油亚微乳的处方与制备工艺,并对其进行表征和体外释放动力学研究。方法 以离心稳定性常数Ke、粒径、ζ电位的综合评分为指标,采用Box-Behnken效应面法优化辛夷油亚微乳处方工艺,透析法研究其体外释放桉油精的情况。结果 辛夷油亚微乳的最优处方:辛夷油5%、大豆磷脂1.2%、泊洛沙姆188 1.8%、油酸1.3%,最佳制备工艺条件:乳化时间10 min,乳化温度60℃,超声时间10 min。辛夷油亚微乳的桉油精含量为(2.43±0.04)mg·mL^(-1),粒径为(156.93±1.53)nm,多分散指数(PDI)为(0.16±0.02),ζ电位为(-24.87±1.67)mV,体外释放符合一级动力学方程特征,释放机制为Fick扩散。结论 成功制备辛夷油亚微乳并优化了处方工艺,所得制剂的稳定性良好,并且具有缓释作用。Objective To optimize the prescription and preparation of Magnolia Flos oil-loaded sub-micro emulsion based on unification of drugs and excipients,characterize its preparation and determine the vitro release kinetics.Methods Box-Behnken response surface method was used to optimize the formulation and process variables of Magnolia Flos oil-loaded sub-micro emulsion using the comprehensive score of Ke,particle size,and zeta potential as indexes.The dialysis method was used to determine the in vitro release of eucalyptol.Results The optimal formulation of Magnolia Flos oil-loaded sub-micro emulsion was as follows:5%Magnolia Flos oil,1.2%soybean lecithin,1.8%poloxamer 188,and 1.3%oleic acid.The optimal preparation conditions:emulsification for 10 min,at 60℃,ultrasonic time of 10 min.The content of eucalyptol in the Magnolia Flos oil-loaded sub-micro-emulsion was(2.43±0.04)mg·mL^(-1),mean particle size was(156.93±1.53)nm,polymer dispersity index(PDI)was(0.16±0.02)and zeta potential was(-24.87±1.67)mV.The in vitro release study exhibited the characteristics of the first-order kinetic equation,and the release mechanism was Fick diffusion.Conclusion Magnolia Flos oil-loaded sub-micro emulsion is successfully prepared and the formulation is optimized.The preparation has good stability and sustained release effect.

关 键 词：辛夷油 药辅合一 响应面法 亚微乳 体外释药 

分 类 号：R944[医药卫生—药剂学] R286[医药卫生—药学]