延胡索乙素纳米乳制备工艺优化及其性质研究  

Preparation Process Optimization and Properties of Nanoemulsions of Tetrahydropalmatine

作　　者：陈子龙 吕倩 孙鑫 刘思美 赵鹏[2] CHEN Zilong;LYU Qian;SUN Xin;LIU Simei;ZHAO Peng(Weinan Inspection and Research Institute,Weinan,Shaanxi,China 714000;College of Pharmacy,Shaanxi University of Chinese Medicine,Xi′an,Shaanxi,China 712046)

机构地区：[1]陕西省渭南市检验检测研究院,陕西渭南714000 [2]陕西中医药大学药学院,陕西西安712046

出　　处：《中国药业》2025年第1期47-53,共7页China Pharmaceuticals

基　　金：陕西省重点研发计划项目[2022SF-389];陕西省教育厅重点科学研究计划项目[21JS008];陕西省渭南市科技计划项目[2022ZDYFJH-168]。

摘　　要：目的优选延胡索乙素纳米乳制备工艺,并考察其稳定性和理化性质。方法采用亲水亲油平衡(HLB)法制备延胡索乙素纳米乳,以粒径和聚合物分散性指数为评价指标,在单因素试验基础上,采用Box-BehnkenDesign响应面法筛选最优制备工艺,并考察优选工艺制得样品的稳定性和理化性质。结果最优工艺为聚氧乙烯蓖麻油-油酸乙酯质量比19.514∶1,无水乙醇用量1.2 g,去离子水用量6.48 g。以优选工艺制得延胡索乙素纳米乳为无色透明液体,外观均匀,易于涂布,呈球形或近球形,平均粒径为16.3 nm,聚合物分散性指数为0.306,在40℃条件下的物理稳定性良好,24 h累积透过量为1100.92μg/cm^(2),纳米乳中延胡索乙素的透皮吸收过程与质量浓度无关,且为扩散过程。结论制备的延胡索乙素纳米乳的稳定性、物理性质和透皮吸收性均较好,可为延胡索乙素新剂型的研发提供参考。Objective To optimize the preparation process of nanoemulsions of tetrahydropalmatine,and to investigate their stability and physicochemical properties.Methods Hydrophilic lipophilic balance(HLB)method was used to prepare nanoemulsions of tetrahydropalmatine.With particle size and polymer dispersibility index(PDI)as evaluation indicators,the Box-Behnken design response surface methodology was used to screen the optimal preparation process based on the single factor test,and the stability and physicochemical properties of the samples prepared by the optimized process were investigated.Results The optimal process was as follows:the mass ratio of polyoxyethylene castor oil-ethyl oleate was 19.514∶1,with anhydrous ethanol dosage of 1.2 g,and deionized water dosage of 6.48 g.The nanoemulsions of tetrahydropalmatine prepared by the optimal process were colorless and transparent liquid with uniform appearance,easy to apply,spherical or nearly spherical shape,with an average particle size of 16.3 nm,PDI of 0.306,good physical stability at 40℃,and 24 h cumulative transmittance of 1100.92μg/cm^(2).The transdermal absorption process of tetrahydropalmatine in nanoemulsion was independent of concentration and exhibited a diffusion process.Conclusion The stability,physical properties,and transdermal absorption of the prepared nanoemulsions of tetrahydropalmatine are good,which can provide a reference for the development of new formulations of tetrahydropalmatine.

关 键 词：延胡索乙素 纳米乳 Box-Behnken Design响应面法 工艺优选 体外性质研究 

分 类 号：R932[医药卫生—生药学] TQ460.6[医药卫生—药学]