安石榴苷平衡溶解度与油水分配系数的测定

摘要

目的 考察安石榴苷在不同pH值磷酸盐缓冲液中的平衡溶解度(S)和油水分配系数(PO/W),为其制剂开发提供参考.方法 采用摇瓶-紫外分光光度法测定安石榴苷在不同温度(25℃、37℃)、pH为1.2、2.5、5.0、5.8、6.8、7.4、7.8～8.0的磷酸盐缓冲液中的S值和在正辛醇-缓冲液中的PO/W值.结果 在pH为1.2～8.0条件下,安石榴苷在25℃时的S值和lgPO/W分别为775.00～2 789.00 mg/mL和-3.07～-3.85,在37℃时的S值和lgPO/W分别为1 006.00～2 684.00 mg/mL和-1.32～-3.81;在pH 1.2～8.0范围,均有lgPO/W＜0,pH为1.2时,安石榴苷的S值较低.结论 安石榴苷水溶性较好,亲脂性差,在胃内的溶解性不好,表明透膜性差是影响胃肠道吸收的限速因素.%Objective To determine the equilibrium solubility (S) and the apparent oil/water partition coefficient (PO/W) of punicalagin in different pH phosphate buffer solution,so as to provide the basis for the exploitation of preparations.Methods The S values and the PO/W values of punicalagin in pH1.2,2.5,5.0,5.8,6.8,7.4,7.8-8.0 of phosphate buffer solutions at 25℃ or 37℃ were measured by shaking flask-UV spectrophotometry.Results In pH 1.2-8.0 phosphate buffer solutions,the S values of punicalagin were 775.00～2 789.00 mg/mL and the PO/W values were-3.07～-3.85 at 25℃,and the S values of punicalagin was 1 006.00～2 684.00 mg/mL and the PO/W values were-1.32～-3.81at 37℃.The lgPO/W values were ＜0 at the pH range from 1.2 to 8.0.The S value of punicalagin in pH1.2 is markedly lower than the others.Conclusion Punicalagin has good watersolubility,but its solubility is bad in stomach.Punicalagin has poor liposolubility.It may be poor absorption in the gastrointestinal tract for the poor membrane permeability.