| 引用本文： |
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陈新科,李静萍,刘亚男,蒋才武.两种二氢杨梅素-酚酸共晶的制备、表征和性质研究[J].广西科学院学报,2026,42(2):240-248. [点击复制]
- CHEN Xinke,LI Jingping,LIU Ya'nan,JIANG Caiwu.Preparation,Characterization and Properties of Two Dihydromyricetin-Phenolic Acid Cocrystals[J].Journal of Guangxi Academy of Sciences,2026,42(2):240-248. [点击复制]
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| 摘要: |
| 为改善二氢杨梅素(Dihydromyricetin，DHM)低溶解性导致的低生物利用度，本研究选用DHM作为药物活性成分，大黄酸(RH)、香草酸(VA)作为共晶形成剂，利用冷却结晶、溶剂挥发技术成功制备出两种新型药物共晶，并采用粉末X射线衍射(PXRD)、傅里叶变换红外光谱(FT-IR)、差示扫描量热(DSC)、热重(TG)和核磁共振氢谱(1H-NMR)对其进行表征,同时考察了药物共晶的溶解度。结果表明，两种药物共晶在PXRD图谱中有新的衍射峰生成，在FT-IR图谱中有特征官能团偏移；在DSC曲线中，药物共晶吸热峰不同于DHM的吸热峰；1H-NMR结果显示DHM-RH共晶、DHM-VA共晶的化学计量比分别为1∶2、1∶1；在体外溶出实验研究中，与DHM相比，两种药物共晶的溶出速率均有明显提升。本研究中的药物共晶合成策略可为中药制剂开发提供参考。 |
| 关键词: 药物共晶 二氢杨梅素 大黄酸 香草酸 溶解度 |
| DOI：10.13657/j.cnki.gxkxyxb.20260105.001 |
| 投稿时间：2025-07-30修订日期：2025-09-26 |
| 基金项目:国家自然科学基金项目(20662002)，广西自然科学基金面上项目(2023GXNSFAA026292)和广西壮瑶药重点实验室开放课题(桂科基字〔2014〕32号)资助。 |
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| Preparation,Characterization and Properties of Two Dihydromyricetin-Phenolic Acid Cocrystals |
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CHEN Xinke, LI Jingping, LIU Ya'nan, JIANG Caiwu
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| (Guangxi Key Laboratory of Zhuang and Yao Ethnic Medicine, Guangxi University of Chinese Medicine, Nanning, Guangxi, 530200, China) |
| Abstract: |
| To improve the low bioavailability caused by the low solubility of dihydromyricetin (DHM),DHM was selected as the active component of the drug,and rhein (RH) and Vanillic Acid (VA) were used as the cocrystal forming agents in this study.Two new types of drug cocrystals were successfully prepared using cooling crystallization and solvent evaporation techniques.The obtained cocrystals were characterized by Powder X-ray Diffraction (PXRD),Fourier Transform Infrared spectroscopy (FT-IR),Differential Scanning Calorimetry (DSC),Thermogravimetric (TG) and proton Nuclear Magnetic Rresonance spectra (1H-NMR),and the solubility of the drug cocrystals was investigated simultaneously.The results showed that new diffraction peaks appeared in the PXRD patterns of the two pharmaceutical cocrystals,and characteristic functional group shifts were observed in their FT-IR spectra.In the DSC curve,the endothermic peak of the drug cocrystal was different from that of DHM.The results of 1H-NMR showed that the stoichiometric ratios of DHM-RH cocrystal and DHM-VA cocrystal were 1∶2 and 1∶1,respectively.In the in vitro dissolution experiment study,compared with DHM,the dissolution rates of the two drug cocrystals were significantly improved.The drug cocrystal synthesis strategy in this study can provide a reference for the development of traditional Chinese medicine preparations. |
| Key words: drug cocrystal dihydromyricetin rhein vanillic acid solubility |
