红花提取物磷脂复合物的制备及其透膜性研究

Preparation and membrane permeability of phospholipid complex from extract of Carthamus tinctorius

目的优化红花提取物磷脂复合物的制备工艺并研究其透膜性能。方法在单因素实验基础上,利用响应曲面分析法,以红花提取物与磷脂形成的磷脂复合物的复合率为指标,优化制备工艺。利用紫外-可见吸收光谱和红外光谱方法进行表征。采用改良Franz扩散池,评价红花提取物及不同药脂比的磷脂复合物的体外透膜性能。结果红花提取物磷脂复合物的最佳制备工艺为以甲醇为复合溶剂,红花提取物的质量浓度为5.0mg/m L,与磷脂质量比为1∶1,反应时间为1.5h,反应温度为55℃。透膜实验结果显示,红花提取物及药脂比分别为2、1、0.5的磷脂复合物24h累积渗透量(Q24)分别为(15.07±1.24)、(15.61±0.92)、(21.94±1.54)、(21.05±1.39)μg/cm2。结论优选的制备工艺合理可行,红花提取物磷脂复合物能明显改善其透膜性能。

Objective To optimize the preparation technology of phospholipid complex of Carthamus tinctorius(safflower)extract and investigate its permeability.Methods On the basis of single factor experiment,the preparation process was optimized by using the response surface analysis method,taking the compound rate of phospholipid complex of safflower extract as the index.It was characterized by UV-vis absorption spectrum and infrared spectrum.The modified Franz diffusion cell was used to evaluate the membrane permeability of safflower extract and phospholipid complex of safflower extract with different drug-lipid ratios in vitro.Results The optimum preparation technology of phospholipid complex of safflower extract was as follows:methanol was used as compound solvent,the concentration of safflower extract was 5.0 mg/mL,and the mass ratio of phospholipid to phospholipid was 1∶1,the reaction time was 1.5 h,and the reaction temperature was 55℃.The results of transmembrane experiment showed that the 24-hour cumulative permeability(Q24)of safflower extract phospholipid complex with drug-fat ratio of 2,1,and 0.5 was(15.07±1.24),(15.61±0.92),(21.94±1.54),and(21.05±1.39)μg/cm2,respectively.Conclusion The optimized preparation process is reasonable and feasible,and the phospholipid complex of safflower extract can obviously improve its membrane permeability.