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- 2019
柚皮素磷脂复合物的制备及其理化性质的研究
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Abstract:
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5 g/L、柚皮素与磷脂质量比1∶1.5、反应时间2 h、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0.016 3%±0.002 5%，乙酸乙酯残留量为0.040 8%±0.001 9%，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
