白鲜皮-地肤子药对醇质体的制备及处方优化  

Preparation and Prescription Optimization of Alcoholsome by Cortex Dictamni-Fructus Kochiae

作　　者：姜京京 吕江维[1] 杨硕[1] 陈泳霖 夏江 王昊 张文君[1,3,4] JIANG Jingjing;LYU Jiangwei;YANG Shuo;CHEN Yonglin;XIA Jiang;WANG Hao;ZHANG Wenjun(School of Pharmacy,Harbin University of Commerce,Harbin 150076,China;Jiangsu Hengrui Pharmaceutical Co.,LTD,Lianyungang 222002,China;Engineering Research Center of Ministry of Education of Natural Antitumor Drugs,Harbin 150076,China;Heilongjiang Provincial Key Laboratory of Drugs for the Prevention and Treatment of Senile Diseases,Harbin 150076,China)

机构地区：[1]哈尔滨商业大学药学院,哈尔滨150076 [2]江苏恒瑞医药股份有限公司,连云港222002 [3]抗肿瘤天然药物教育部工程研究中心,哈尔滨150076 [4]黑龙江省预防与治疗老年性疾病药物研究重点实验室,哈尔滨150076

出　　处：《医药导报》2025年第4期639-647,共9页Herald of Medicine

基　　金：2023年度新一轮黑龙江“双一流”学科协同创新成果项目(LJGXCG2023-101);2024年黑龙江省中医药经典普及化专项课题项目(ZYW2024-025;ZYW2024-076)。

摘　　要：目的制备白鲜皮-地肤子药对醇质体,筛选最佳处方工艺,对其进行处方验证及性能研究。方法采用乙醇注入法制备白鲜皮-地肤子醇质体,以包封率为评价指标,通过单因素考察和响应面试验优化处方,并对其外观形态、粒径大小、Zeta电位及稳定性进行考察。结果白鲜皮-地肤子药对醇质体最佳制备工艺:冻干粉用量为409.06 mg、大豆卵磷脂用量为258.07 mg、胆固醇用量为90.87 mg、乙醇体积分数为22.76%,50℃水浴温度下以700 r·min^(-1)搅拌2 h,制备的醇质体混悬液外观呈淡黄色,透射电镜测得形状规则近似球形;平均粒径为(103.1±0.78)nm,电位为(-36.0±3.65)mV,黄柏酮、梣酮和地肤子皂苷Ic的平均包封率分别为(89.25±0.91)%、(80.16±1.52)%、(86.59±0.58)%,室温下放置14 d后,醇质体仍是淡黄色的均一稳定液体,且无分层析出现象。结论乙醇注入法制备的白鲜皮-地肤子药对醇质体操作易行,包封率较高,稳定性良好,为进一步探讨该制剂的皮肤给药奠定了基础。Objective The optimum formulation process was selected to prepare the ethosomes of Cortex Dictamni-Fructus Kochiae,and its prescription was verified and its properties were studied.Methods The formulation was optimized by single factor and response surface test.The appearance,particle size,Zeta potential and stability were investigated.The encapsulation rate was used as the evaluation index.Results The optimum preparation process of ethosomes of Cortex Dictamni-Fructus Kochiae is as follows:Using the dosage of lyophilized powder 409.06 mg,soybean lecithin 258.07 mg,cholesterol 90.87 mg,ethanol volume fraction 22.76%,stirred for 2 hours at 700 r·min^(-1) at 50℃water bath temperature,The appearance of the prepared ethosomes suspension was light yellow,and the particles were nearly spherical in shape.The average particle size was(103.1±0.78)nm,the Zeta potential was(-36.0±3.65)mV,and the average encapsulation rates of Xibutanone,ash,and saponin Ic were(89.25±0.91)%,(80.16±1.52)%,(86.59±0.58)%,respectively.After 14 days of storage at room temperature,the results showed that:The ethosomal suspension is still a light yellow,uniform,and stable liquid,and there is no stratified precipitation phenomenon.Conclusion The method of ethanol injection is easy to operate,high encapsulation rate and good stability,which lays a foundation for further study on the skin administration of this preparation.

关 键 词：白鲜皮 地肤子 醇质体 处方优化 

分 类 号：R971[医药卫生—药品]