光甘草定平衡溶解度和油水分配系数的测定

Determination of equilibrium solubility and apparent oil/water partition coefficient of Glabridin

[目的]测定光甘草定的溶解度及油水分配系数,为光甘草定的新剂型研究提供实验依据。[方法]将光甘草定分别加入不同溶剂和不同p H值缓冲盐溶液中,采用摇瓶法制备光甘草定的饱和溶液,所得溶液0.45μm滤膜滤过,进行高效液相色谱法(HPLC)分析,检测光甘草定的含量。同时用上述方法测定光甘草定在正辛醇-水体系中的表观油水分配系数。[结果]光甘草定在丙酮中溶解度最大,为67 862.13 mg/L,在水中的溶解度最小,为0.1 mg/L;光甘草定油水分配系数为71 142.16(lg P=4.85)。[结论]光甘草定为中等极性的化合物,在中等极性的溶剂中有一定的溶解度,而在极性较高或者极性较低的溶剂中几乎不溶,故在制备外用制剂时应考虑结合高分子材料,提高生物利用度。

[Objective] To determine the equilibrium solubility in different solvents p H buffer solvents. [Methods]Shaking flask method was established to preparing saturated solution of glabridin. HPLC method was used to determine the concentration of glabridin. Apparent coefficient was also determined by shaking flask method and HPLC method. [Results] The maximum solubility of glabridin was in acetone, being 67 862.13 mg/L. The solubility in water was 0.1 mg/L. The apparent oil/water partition coefficient of glabridin was 71 142.16（lg P =4.85）.[Conclusion] Glabridin is a soflavones which has moderate-polar. It is soluble in moderate-polar solution and insoluble in water and high lipophilic solution. To elevate the drug concentration and increase bioavailability, the combination of polymers should be considered when peparing external preparation.