目的:测定脱氧土大黄苷的平衡溶解度及表观油水分配系数。方法:采用紫外分光光度-摇瓶法测定脱氧土大黄苷在有机溶剂、水及不同pH磷酸盐缓冲盐中的平衡溶解度和其在正辛醇-水/磷酸盐缓冲盐溶盐中的表观油水分配系数。结果:在温度37℃时,脱氧土大黄苷在水中的溶解度为0.1217mg/m L,乙醇和正辛醇对脱氧土大黄苷的溶解性较好,其溶解度分别为12.1146mg/m L和7.2867mg/m L,在不同pH的磷酸盐缓冲溶液中随着pH的升高其溶解度变化无规律;脱氧土大黄苷在正辛醇-水中的表观油水分配系数Papp为138.52(lg P=2.14);当pH在1~8的磷酸盐缓冲溶液中时,受pH影响几乎无变化,表现为亲脂性。结论:脱氧土大黄苷在水中的平衡溶解度差,受介质的pH影响,且油水分配系数高。因此,在制剂过程中,可通过改变pH增加药物的溶解性和稳定性。其测定结果为进一步研究脱氧土大黄苷的制备、制剂及其在生物体内外的吸收、分布和代谢过程提供重要的参考和依据。
Objective To determine the equilibrium solubility and apparent oil/water partition coefficient of deoxyrhaponticin. Methods Combining shaking flask method and Ultraviolet speetrophotometer (UV) to detect the oil/water partition coefficients of deoxyrhaponticin, the equilibrium solubility of deoxyrhapontiein in the commonly used organic solvents and water and different pH buffer solution were determined by UV analysis. Results In the temperature of 37, solubility of deoxyrhaponticin in water is 0. 1217mg/mL, Commonly used organic solvents such as ethanol and noctyl alcohol are good solvents for deoxyrhaponticin, its solubility are 7. 2867mg/mL and 12. 1146mg/mL respectively, in different pH phosphate buffer solution, with pH increasing, the solubility of deoxyrhaponticin is irregular; in n - oetyl alcohol/water, the oil/water partition coefficients of deoxyrhapontiein (Papp) is 138.52 ( lgP = 2. 14) ; when the pH of buffer solution is in 1 - 8, the oil/water partition coefficients of deoxyrhaponticin almost has no changement, and tend to be lipophilic. Conclusion the equilibrium solubility of deoxyrhaponticin in water is poor and is affected by it's pH, and it's oil/water partition coefficients is high. In the preparation, the solubility and stability of the drug can be increased by changing its pH. The results provide important reference and basis for further research on the preparation, preparation and the absorption, dis- tribution and metabolism in vivo of deoxyrhaponticin.