辣椒碱微乳的制备及其质量评价  

Preparation and quality evaluation of capsaicin microemulsion

作　　者：郭晔 陈建平 成日青 徐长进 高鑫 齐和日玛 白文明 王来兵 于姝燕 郭慧卿 GUO Ye;CHEN Jian-ping;CHENG Ri-qing;XU Chang-jin;GAO Xin;Qiherima;BAI Wen-ming;WANG Lai-bing;YU Shu-yan;GUO Hui-qing(School of Pharmacy,Inner Mongolia Medical University,Hohhot 010110,China)

机构地区：[1]内蒙古医科大学药学院,内蒙古呼和浩特010110

出　　处：《化学研究与应用》2024年第9期2119-2126,共8页Chemical Research and Application

基　　金：内蒙古医科大学面上项目(YKD2023MS084)资助;内蒙古自治区卫生健康科技计划项目(202201235)资助。

摘　　要：为了提高辣椒碱溶解度和生物利用度将其制备成微乳,经溶解度实验和伪三元相图确定微乳处方组成和表面活性剂与助表面活性剂的最佳质量比(Km);以粒径和载药量为考察指标,采用星点设计-响应面法优化辣椒碱微乳处方;并对最优处方制备的辣椒碱微乳进行质量评价。辣椒碱微乳最优处方为辣椒碱5.12%,油酸乙酯5.82%,曲拉通X-100和无水乙醇(K_(m)=3∶1)28.54%,加纯化水至5.0 g;制得的微乳为O/W型澄清透明的均一液体,其形态为表面光滑的球形;CAP微乳粒径为16.5±0.17 nm,多分散指数为0.387±0.02,Zeta电位为-12.1±0.12 m V,粘度为33±1.73 m Pa·s;冻融稳定性和离心稳定性良好;红外光谱和差示扫描量热分析表明辣椒碱被包裹在微乳中。将辣椒碱制备成辣椒碱微乳,溶解度得以提高,解决了其水溶性低的问题,为辣椒碱的开发与应用提供一定的参考。To improve the solubility and bioavailability of capsaicin,it was prepared into microemulsion.The composition of microe-mulsion prescription and the optimal mass ratio(Km)of surfactant and co-surfactant were determined by solubility experiments and pseudo-ternary phase diagrams.The central composite design method was used to optimize the prescription of capsaicin microemul-sion by the particle size and the drug loading capacity as the indexes,and its quality was evaluated.The optimal prescription of cap-saicin microemulsion was capsaicin 5.12%,ethyl oleate 5.82%,triton X-100 and anhydrous ethanol(K_(m)=3:1)28.54%,and adding purified water to 5.0 g.The CAP microemulsion was a clear and transparent homogeneous liquid of O/W type,which was in the form of a smooth spherical surface.Its particle size was 16.5±0.17 nm,the polydispersity index was 0.387±0.17,Zeta potential was-12.1+0.12 mV,and viscosity was 33±1.73 mPa·s;freeze-thaw and centrifugal stability were good;Infrared spectroscopy and diferential scanning calorimetry(DSC)showed that capsaicin was encapsulated in the microemulsion.Capsaicin was prepared into its microemulsion,and the solubility of capsaicin was improved.The problem of low water solubility was solved,which provideda certain reference for the development and application of capsaicin.

关 键 词：辣椒碱 微乳 伪三元相图 星点设计-响应面法 质量评价 

分 类 号：O647[理学—物理化学]