几种常用辅料与中药提取物原料的相容性探索研究

Exploratory study on the compatibility of several commonly used excipients with raw material of traditional Chinese medicine extract

关键词:  二至方  药物辅料相容性  理论预测  高效液相色谱法  差示扫描量热法  傅里叶变换红外光谱法  X射线粉末衍射法

Key words:  Erzhi Formula  compatibility of drug and excipients  theoretical prediction  high performance liquid chromatography  differential scanning calorimetry  fourier transform infrared spectroscopy  X-ray powder diffraction

摘要:

[目的] 开展中药制剂当中的几种常用辅料（三氯蔗糖、枸橼酸、二氧化硅、麦芽糊精、糊精）与经典名方二至方提取物原料的相容性研究，探索当前常规方法对中药相容性研究的适用性，为中药制剂处方辅料筛选提供参考。[方法] 以二至方提取物中的特女贞苷为指标性成分。首先采用PharmDE平台预测上述辅料与特女贞苷成分的相容性风险，然后用高效液相色谱法（HPLC）、差示扫描量热法（DSC）、傅里叶变换红外光谱法（FTIR）和X射线粉末衍射法（XRPD）从多角度考察了这些辅料与原料的相容性。[结果] 理论预测显示枸橼酸与提取物原料中特女贞苷配伍风险较高；HPLC含量测定结果显示，所有辅料与特女贞苷的光照相容性较好，枸橼酸与特女贞苷的高温相容性较差，三氯蔗糖、糊精与特女贞苷的高温、高湿相容性均较差；而通过DSC、FTIR和XRPD表明辅料与提取物原料间没有发生明显相互作用。[结论] 在高温、高湿的环境下，某些辅料对提取物原料中的特女贞苷成分有一定的影响。

Abstract:

[Objective] To study the compatibility between several commonly used excipients（sucralose，citric acid，silica，maltodextrin，dextrin） in traditional Chinese medicine preparations and the raw material of Erzhi Formula extract，to explore the applicability of current conventional methods for compatibility studies of traditional Chinese medicine，and provide reference for the screening of excipients in traditional Chinese medicine preparations. [Methods] Specnuezhenide from Erzhi Formula extract was used as the indicator component. Firstly，the PharmDE platform was used to predict the compatibility risk between above mentioned excipients and specnuezhenide. Then，the compatibility of these excipients with specnuezhenide was investigated from multiple perspectives using high performance liquid chromatography（HPLC），differential scanning calorimetry（DSC），fourier transform infrared spectroscopy（FTIR），and X-ray powder diffraction（XRPD）. [Results] Theoretical predictions indicated that there was a high risk of compatibility between citric acid and specnuezhenide. The content determination results by HPLC showed that all excipients had good compatibility with specnuezhenide under lighting condition，compatibility between citric acid and specnuezhenide was poor under high temperature condition，and compatibility between sucralose，dextrin，and specnuezhenide was poor under high temperature and high humidity. DSC，FTIR，and XRPD indicated that there was no significant interaction between excipients and the extract. [Conclusion] In high temperature and high humidity environments，certain excipients have a certain impact on specnuezhenide of Erzhi Formula extract.