质量权重系数法整体表征雪菊黄酮提取物性质及其磷脂复合物的制备研究  

Study on Propertie of Coreopsis tinctoria Flavonoid and Preparation of Phospholipid Complex with Mass Weight Coefficient Method

作　　者：王开暄 陈新梅[1] WANG Kaixuan;CHEN Xinmei(School of Pharmacy,Shandong University of Traditional Chinese Medicine,Jinan 250355,China)

机构地区：[1]山东中医药大学药学院,山东济南250355

出　　处：《现代中药研究与实践》2024年第3期79-85,共7页Research and Practice on Chinese Medicines

基　　金：教育部产学合作协同育人项目(230805236011230,220805236310802);山东省中医药科技重点项目(Z-2023070);山东省研究生优质教育教学资源项目(SDYKC2023043);山东中医药大学药学院“药苑育研”优秀研究生创新基金(2023-0018)。

摘　　要：目的 研究雪菊黄酮理化性质,优化雪菊黄酮磷脂复合物制备工艺。方法 以马里苷、木犀草素、槲皮万寿菊苷为指标成分,测定雪菊黄酮的平衡溶解度和油水分配系数,并通过质量权重系数整体表征药物性质;采用层次分析法(AHP)对雪菊黄酮磷脂复合物复合率赋权,设计Box-Behnken响应面试验,优化制备工艺。结果 雪菊黄酮在pH 1.0 ~ 8.0缓冲液和水中的平衡溶解度为0.056 6 ~ 1.861 5 mg/mL,为低溶解性药物,在pH 1.0 ~ 6.0溶液中LogP > 0,易透过胃和十二指肠等上消化道,为高渗透性药物;雪菊黄酮磷脂复合物最优工艺中无水乙醇为反应溶剂,脂药比为3∶1,药物浓度为0.5 mg/mL,反应温度为40 ℃,反应时间为2.0 h,复合率为(96.26±2.71)%,与预测值相比偏差< 3.00%。结论 雪菊黄酮为BCSⅡ类药物,制备为磷脂复合物,工艺稳定可行,可为BCSⅡ类药物设计提供参考。Objective To explore the properties of Coreopsis tinctoria flavonoid and optimize the preparation process of phospholipid complex.Methods The equilibrium solubility and oil-water partition coefficient of Coreopsis tinctoria flavonoid were determined by using marein,luteolin and quercetagitrin as index components,and the properties of Coreopsis tinctoria flavonoid were further characterized with mass weight coefficient method.The complexing rate of Coreopsis tinctoria flavonoid phospholipid complex was weighted by the analytic hierarchy process (AHP).Box-Behnken response surface test was designed to optimize the preparation process.Results The equilibrium solubility of Coreopsis tinctoria flavonoid in pH 1.0-8.0 buffer solution and water was 0.056 6-1.861 5 mg/mL,which was a low solubility drug.The LogP of Coreopsis tinctoria flavonoid in pH 1.0-6.0 buffer solution was more than 0.It was easy to penetrate the upper digestive tract such as the stomach and duodenum,which was a high-permeability drug.The optimal process of Coreopsis tinctoria flavonoid phospholipid complex was anhydrous ethanol as the reaction solvent,the ratio of lipid-drug was 3:1,the drug concentration was 0.5 mg/mL,the reaction temperature was 40°C,and the reaction time was 2.0 h.The complexing rate was (96.26±2.71)%.Compared with the predicted value,the deviation was less than 3.00%.Conclusion The Coreopsis tinctoria flavonoid belongs to BCSII drugs.It is prepared as a phospholipid complex,and the process is stable and feasible.It hopes to provide a reference for the design of BCSII drugs.

关 键 词：雪菊黄酮 平衡溶解度 油水分配系数 磷脂复合物 质量权重系数 

分 类 号：R283.2[医药卫生—中药学]