摘要
采用溶剂挥发法制备柚皮素磷脂复合物,利用紫外光谱法、傅里叶变换红外光谱法、X射线衍射法对柚皮素磷脂复合物的结构进行表征,用差示扫描量热法对复合物的热特性进行分析,利用气相色谱法测定磷脂复合物的溶剂残留量,利用高效液相色谱法测定其在水、正辛醇、磷酸盐缓冲液(PBS)(pH值分别为2.5、5.0、6.5、7.0、7.8~8.0)中的平衡溶解度、油水分配系数以及体外溶出度。结果显示,在柚皮素质量浓度5g/L、柚皮素与磷脂质量比1∶1.5、反应时间2h、反应温度40℃的条件下,柚皮素磷脂复合物载药量为31.79%±0.99%。柚皮素磷脂复合物中二氯甲烷残留量为0.0163%±0.0025%,乙酸乙酯残留量为0.0408%±0.0019%,均符合药典标准。柚皮素磷脂复合物可显著提高柚皮素在水、正辛醇及不同pH下PBS中的平衡溶解度,其油水分配系数对数值(logP)为1.11±0.09。体外溶出试验结果显示,柚皮素磷脂复合物溶出度明显增加,较易被人体吸收利用。
The naringenin phospholipid complex was prepared by solvent evaporation method.The structure of naringenin phospholipid complex was characterized by ultraviolet spectroscopy,Fourier transform infrared spectroscopy,and X-ray diffraction.The thermal properties of the complex were analyzed by differential scanning calorimetry.The solvent residues in phospholipid complex were determined by gas chromatography.The equilibrium solubility in water,n-octanol and PBS (pH 2.5,pH 5.0,pH 6.5,pH 7.0,pH 7.8-8.0),oil/water partition coefficient and in vitro dissolution were determined by high performance liquid chromatography.The results showed that the drug loading efficiency of naringenin phospholipid complex was 31.79%±0.99% under the condition of naringenin mass fraction 5 g/L,naringenin and phospholipid mass ratio 1∶1.5,reaction time 2 h and reaction temperature 40 ℃.The residual amounts of methylene chloride and ethyl acetate in the naringenin phospholipid complex were 0.016 3%±0.002 5% and 0.040 8%±0.001 9%,respectively,which all met the standard of Chinese Pharmacopoeia.The equilibrium solubility of the naringenin phospholipid complex was significantly higher than that of naringenin in water,n-octanoland and PBS with different pHs.The logarithmic value of oil-water partition coefficient of naringenin phospholipid complex was 1.11±0.09.The in vitro dissolution of naringenin phospholipid complex was significantly higher than that of naringenin,and easier to be absorbed and utilized by human.
作者
何小燕
彭颖
何婉莺
潘思轶
HE Xiaoyan;PENG Ying;HE Wanying;PAN Siyi(College of Food Science and Technology,Huazhong Agricultural University,Wuhan 430070,China)
出处
《华中农业大学学报》
CAS
CSCD
北大核心
2019年第5期137-142,共6页
Journal of Huazhong Agricultural University
基金
国家自然科学基金面上项目(31571847)
关键词
柚皮素
磷脂复合物
结构特征
载药量
平衡溶解度
油水分配系数
体外溶出度
naringenin
phospholipid complex
structural characteristics
drug loading efficiency
equilibrium solubility
oil/water partition coefficient
in vitro dissolution
