基于基准关联度与信息熵权法优选桂枝配方颗粒中挥发性成分的β-环糊精包合工艺  

Optimization of β-cyclodextrin Inclusion Process of Cinnamomi Ramulus Formula Granules Volatile Constituents Based on Standard Relation and Information Entropy Method

作　　者：陈雅茜 李卓远 陶琳 陈娜娜 柯益鑫 沈雯 谢薇 张雯[1,2] 李俊松 CHEN Yaxi;LI Zhuoyuan;TAO Lin;CHEN Nana;KE Yixin;SHEN Wen;XIE Wei;ZHANG Wen;LI Junsong(School of Pharmacy,Nanjing University of Chinese Medicine,Nanjing 210023,China;Jiangsu Engineering Research Center for Efficient Delivery System of TCM,Nanjing 210023,China)

机构地区：[1]南京中医药大学药学院,江苏南京210023 [2]江苏省中药高效给药系统工程技术研究中心,江苏南京210023

出　　处：《南京中医药大学学报》2024年第6期582-588,共7页Journal of Nanjing University of Traditional Chinese Medicine

基　　金：江苏省自然科学基金(BK20190800);南京中医药大学自然科学基金(XPT82104688)。

摘　　要：目的结合基准关联度与信息熵权法,采用正交试验对β-环糊精(β-Cyclodextrin,β-CD)与桂枝配方颗粒中挥发性成分的包合工艺进行优化。方法在单因素考察的基础上,选择β-CD与桂枝芳香水的投料比、包合温度、包合时间为主要影响因素,以包合物中桂皮醛的包合率、载药量及基准关联度为评价指标,采用信息熵权法计算各评价指标的权重系数,进行综合评价和优化正交试验包合工艺。通过薄层色谱法、紫外可见吸收光谱、傅里叶红外光谱、X射线衍射等方法对包合物进行表征。结果优选的最佳包合工艺为β-CD与芳香水的投料比3∶100(g·mL^(-1)),包合温度50℃,包合时间1 h。经验证,桂皮醛包合率为80.48%,载药量为8.63%,基准关联度为0.91。薄层、紫外、红外等表征实验表明芳香水中挥发性成分成功进入β-CD空腔,包合物制备成功。结论优选的包合工艺稳定可行,可为桂枝配方颗粒的制剂工艺研究提供参考。OBJECTIVE To optimize β-cyclodextrin(β-CD)inclusion process of Cinnamomi Ramulus Formula Granules volatile constituents by orthogonal test,based on standard relation and information entropy method.METHODS On the basis of single factor experiments,the ratio of β-CD to aromatic aqueous solution,the inclusion temperature,and the inclusion time were selected as the investigating factors;the inclusion rate,drug loading,and standard relation of cinnamic aldehyde in inclusion complex were used as the evaluation index.The information entropy method was used to determine the weight coefficient of each index,then the comprehensive score was calculated,the inclusion process conditions were optimized by orthogonal experiment.The inclusion complex was characterized by thin layer chromatography,ultraviolet absorption spectroscopy,Fourier infrared spectroscopy,and X-ray diffraction.RESULTS The best inclusion process was that the ratio of β-CD to aromatic aqueous solution was 3∶100(g·mL^(-1)),the inclusion temperature was 50℃,and the inclusion time was 1 h.The average inclusion rate of the obtained inclusion compound was 80.84%,the drug loading was 8.63%,and the standard relation was 0.91.The results of thin-layer chromatography,ultraviolet,infrared spectroscopy and other characterization experiments showed that the volatile components in the aromatic aqueous solution successfully entered the β-CD cavity,and the inclusion complex was successfully prepared.CONCLUSION The optimum inclusion process is stable and feasible,which can provide references for the preparation process of Cinnamomi Ramulus Formula Granules.

关 键 词：桂枝配方颗粒 芳香水 Β-环糊精 信息熵权法 基准关联度 正交试验 包合工艺 

分 类 号：R284[医药卫生—中药学]