响应面法优化草乌甲素纳米乳的制备工艺  

Optimization of the preparation process of bulleyaconitine A nanoemulsion by response surface methodology

作　　者：何雨晓 李丽云 孙文强 丁江生 周云龙 HE Yuxiao;LI Liyun;SUN Wenqiang;DING Jiangsheng;ZHOU Yunlong(Yunnan University of Traditional Chinese Medicine,Kunming 650500,China;Yunnan Institute of Materia Medica,Kunming 650111,China;Key Laboratory of Traditional Chinese Medicine and Ethnic Medicine New Drug Creation Enterprises in Yunnan Province,Kunming 650111,China)

机构地区：[1]云南中医药大学,昆明650500 [2]云南省药物研究所,昆明650111 [3]云南省中药和民族药新药创制企业重点实验室,昆明650111

出　　处：《西北药学杂志》2023年第6期105-112,共8页Northwest Pharmaceutical Journal

基　　金：云南省科技厅科技计划项目(编号:2019DC008)。

摘　　要：目的研究草乌甲素纳米乳的处方和制备工艺,并对其质量进行评价。方法用加水滴定法和微流化均质制备草乌甲素纳米乳,用伪三元相图法结合Box-Behnken响应面法优化草乌甲素纳米乳的处方,并对其粒径分布、稳定性进行考察。结果草乌甲素纳米乳的最优处方和工艺为乳化剂与助乳化剂的质量比为1∶1、油相的比例为8%、乳化剂的比例为11%、均质压力为28000 psi,平均粒径的预测值为60.25 nm,用激光粒度仪测得的粒径为(60.55±0.88)nm,多分散指数为(0.233±0.220),Zeta电位为(-28.5±0.34)mV。纳米乳在低温条件下保存较稳定。草乌甲素纳米乳体外透皮实验结果显示,纳米乳中草乌甲素的24 h累积透皮量为(260.8512±7.7639)μg·cm^(-2),24 h内的释药数据符合一级方程。结论所优化的处方工艺稳定,模型预测功能良好,制备的草乌甲素纳米乳外观圆整,粒径均一且稳定,体外透皮性能良好。Objective To study the formulation and preparation process of bulleyaconitine A nanoemulsion(BANE),and to evaluate its quality.Methods Aqueous titration method and micro fluidization homogenization were used to prepare the BANE.The formulation of the BANE was optimized by pseudo-ternary phase diagram method combined with Box-Behnken response surface methodology,and its particle size distribution and stability were investigated.Results The optimal formulation and preparation conditions of the BANE were as follows:the mass ratio of emulsifier to co-emulsifier 1∶1,the proportion of oil phase 8%,the proportion of emulsifier 11%,and the homogenization pressure 28000 psi.The average particle sizes of predicted result and the result determined by using laser particle size analyzer were 60.25 nm and(60.55±0.88)nm respectively.The polydispersity index was(0.233±0.220),and the Zeta potential was(-28.5±0.34)mV.The nanoemulsion observed by transmission electron microscope showed a round appearance,and uniform and stable size.The BANE was relatively stable in cryopreservation.The cumulative transdermal amount of bulleyaconitine A in vitro in 24 hours was(260.8512±7.7639)μg·cm^(-2),conforming to the first-order equation.Conclusion The optimized formulation process is stable,the model prediction function is good,and the prepared BANE has a round appearance,uniform and stable particle size.

关 键 词：草乌甲素 纳米乳 微射流均质 响应面分析 

分 类 号：R94[医药卫生—药剂学]