柚皮素磷脂复合物的制备及其理化性质的研究
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国家自然科学基金面上项目( 31571847)


Preparation and physicochemical properties of naringenin phospholipid complex
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    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(logP)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。

    Abstract:

    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.

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何小燕,彭颖,何婉莺,潘思轶.柚皮素磷脂复合物的制备及其理化性质的研究[J].华中农业大学学报,2019,38(5):137-142

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  • 收稿日期:2019-04-28
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  • 在线发布日期: 2019-08-14
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