白藜芦醇-牛磺脱氧胆酸钠共无定形体系改善溶解度和物理稳定性  

Resveratrol-sodium taurodeoxycholate coamorphous system improves solubility and physical stability

作　　者：李珏 姜飞 李慧丽 沈祥春 贺智勇 易媛丹 刘文 陶玲 LI Jue;JIANG Fei;LI Huili;SHENG Xiangchun;HE Zhiyong;YI Yuandan;LIU Wen;TAO Ling(Guizhou Province Specialized Natural Medicine Resource Efficient Utilization Engineering Center,Specialized Key Laboratory of Pharmacology and Pharmacological Evaluation of Natural Medicines in Guizhou Higher Education Institutions,Guizhou Medical University Guiyang Joint Key Laboratory,Key Laboratory of Optimal Utilization of Natural Medicine Resources,School of Pharmaceutical Sciences,Guizhou Medical University,Guiyang 550006,China;Guizhou Maternal and Child Health Care Hospital,Guiyang 550000,China)

机构地区：[1]贵州医科大学药学院,贵州省特色天然药物资源高效利用工程中心,贵州省高等学校天然药物药理与成药性评价特色重点实验室,贵州医科大学-贵阳市联合重点实验室,天然药物资源优效利用重点实验室,贵州贵阳550006 [2]贵州省妇幼保健院,贵州贵阳550000

出　　处：《中草药》2024年第21期7248-7256,共9页Chinese Traditional and Herbal Drugs

基　　金：国家自然科学基金资助项目(82260827);国家自然科学基金资助项目(U1812403-4-4);贵州省自然科学基金资助项目([2020]1Z069);贵州省科技计划项目(黔科合支撑[2020]4Y240号);贵州省高层次创新型人才十层次人才项目(黔科合平台人才-GCC [2023]048);贵州省科技创新基地(黔科合中引地[2023]003)。

摘　　要：目的 通过共无定形体系(coamorphous system,CAS)来改善和提升白藜芦醇(resveratrol,Res)的溶解度和物理稳定性。方法 通过溶剂挥发法进行白藜芦醇-牛磺脱氧胆酸钠(sodium taurodeoxycholate,STD)共无定形体系(Res-STDCAS)制备研究,考察了最佳物质的量比;利用粉末X射线衍射、傅里叶变换红外光谱、拉曼光谱、固态核磁、差示扫描量热分析和扫描电子显微镜等技术表征其固态特征,并考察其在不同pH值缓冲液中的溶解度,进一步研究其吸湿性和物理稳定性。结果 固态表征结果显示,白藜芦醇与STD形成了具有单一玻璃化转变温度的CAS,且存在分子间氢键作用;溶解度结果显示,在Res-STD-CAS物质的量比为1∶1、1∶2、1∶3的CAS中,白藜芦醇的溶解度均高于其原料药及其物理混合物;在40℃、75%相对湿度条件下,其稳定性高达3个月。结论 Res-STD-CAS大幅提高了白藜芦醇的溶解度,并具有良好的物理稳定性。Objective The solubility and physical stability of resveratrol(Res)are improved and promoted through coamorphous system(CAS).Methods Resveratrol-sodium taurodeoxycholate coamorphous system(Res-STD-CAS)was prepared by solvent volatilization method and the optimal molar ratio was investigated.Powder X-ray diffraction,Fourier transform infrared spectroscopy,raman spectroscopy,solid state nuclear magnetism,differential scanning calorimetry and scanning electron microscope were used to racterise the solid state properties,and its solubility in buffers with different pH values was investigated,and its hygroscopicity and physical stability were further study.Results The solid-state characterization results showed that resveratrol and STD formed a CAS with a single glass transition temperature,and there was intermolecular hydrogen bonding.The solubility results showed that the solubility of resveratrol was higher than that of its raw material and its physical mixture in the CAS with the molar ratios of Res-STD-CAS of 1:1,1:2 and 1:3.It is stable for up to three months at 40℃ and 75%relative humidity.Conclusion Res-STD-CAS greatly improves the solubility of resveratrol and has good physical stability.

关 键 词：白藜芦醇 牛磺脱氧胆酸钠 共无定形体系 增溶 溶解度 稳定性 溶剂挥发法 吸湿性 

分 类 号：R283.6[医药卫生—中药学]