苦参总黄酮磷脂复合物的制备及优化  

Preparation and Characterization of TotaL Flavonoids Phospholipid Complex from Sophora flavenscens

作　　者：杨志欣[1] 程静 张文君[2] 王鑫[1] 张蕾[1] 侯立强[3] YANG Zhixin;CHENG Jing;ZHANG Wenjun;WANG Xin;ZHANG Lei;HOU Liqiang(College of Pharmacy, Heilongjiang University of Chinese Medicine, Harbin 150040 Heilongjiang, China;School of Pharmacy, Harbin University of Commerce, Harbin 150076 Heilongjiang, China;The Second Affiliated Hospital of Heilongjiang University of Chinese Medicine, Harbin 150001 Heilongjiang, China)

机构地区：[1]黑龙江中医药大学药学院,黑龙江哈尔滨150040 [2]哈尔滨商业大学药学院,黑龙江哈尔滨150076 [3]黑龙江中医药大学附属第二医院,黑龙江哈尔滨150001

出　　处：《中药新药与临床药理》2018年第3期342-346,共5页Traditional Chinese Drug Research and Clinical Pharmacology

基　　金：黑龙江省自然科学基金(H2016057;H2017066);黑龙江中医药大学"优秀创新人才支持计划"项目(2012);国家教育部春晖计划(Z2008-1-15016);黑龙江省教育厅骨干教师基金(1251 G058)

摘　　要：目的制备苦参总黄酮组分磷脂复合物,并研究复合物的理化性质。方法采用溶剂挥发法制备苦参总黄酮磷脂复合物,采用单因素考察和正交试验,以复合率为指标,优化工艺条件;采用差示扫描量热分析(DSC)和傅里叶变换红外光谱法(FTIR)、紫外吸收光谱(UV)等对复合物的形成进行验证。结果最佳工艺条件是二氯甲烷︰甲醇(1∶1)为反应溶剂,反应物浓度为2 g·L^(-1),药物与磷脂投料质量比为1∶1.5,在40℃下反应1.5 h;在此条件下复合率为95.57%。与原提取物比较,磷脂复合物中总黄酮的水溶性得到提高;苦参总黄酮与磷脂形成了一种新的物相,但其自身的化学性质并未改变。结论所建立的苦参总黄酮磷脂复合物的制备工艺简单、稳定可靠、可操作性强,易于工业生产。Objective To prepare flavonids phospholipids complex and investigate its physicochemical properties.Methods Using complex rate as index,phospholipids complex was prepared and optimized by solvent evaporation method and orthogonal design; physicochemical characteristics of the complex were investigated by apparent solubility studies, fourier transform infrared spectroscopy（FTIR）, differential scanning calorimetry（DSC）and ultraviolet spectrum（UV）. Results The optimal formulation protocol were as follows：dichloromethane：methanol（1∶1）were taken as the reaction solvent,the reactant concentration was 2 g·L^-1,the mass ratio of total flavonoids from Sophora flavescens and phospholipid was 1︰1.5（w/w）,and the reaction temperature and time were 40 ℃ and 1.5 h,respectively. The complex rate was 95.57 %. Compared with the original extract,the water solubility of the total flavonoids in phospholipid complex was improved;IR,UV and DSC analysis indicated that total flavonoids might interact with phospholipids by apolar interactions. Conclusion Total flavonoids phospholipids complex was successfully developed using the optimized protocol,possessing high complex rate and enhanced water solubility,which was a fundamental formulation for the further research of total flavonoids.

关 键 词：苦参总黄酮 磷脂复合物 差示扫描量热分析(DSC) 红外光谱法(FTIR) 正交设计 

分 类 号：R284.2[医药卫生—中药学]