抗癌先导物T-OA在不同介质中的平衡溶解度及表观油水分配系数  

Equilibrium solubility and apparent oil/water partition coefficient of anticancer primer T-OA in various media

作　　者：绪扩[1] 王鹏龙[1] 徐昕[1] 徐士勋[1] 王艳慧[1] 周燊[1] 张宇忠[2] 雷海民[1] 

机构地区：[1]北京中医药大学中药学院,北京100102 [2]北京中医药大学基础医学院

出　　处：《北京中医药大学学报》2013年第8期554-557,共4页Journal of Beijing University of Traditional Chinese Medicine

基　　金：国家自然科学基金项目(No.81173519);北京中医药大学创新团队项目(No.2011-CXTD-15)

摘　　要：目的 测定抗癌先导物T-OA在不同pH（1～10）缓冲溶液和表面活性剂溶液中的平衡溶解度,在正辛醇-水/缓冲液体系中的表观油水分配系数.方法 采用高效液相法测定了T-OA在不同pH（1 ～10）缓冲溶液和表面活性剂溶液中的浓度,采用摇瓶-HPLC法测定了T-OA的表观油水分配系数.结果 T-OA在37℃缓冲液中随pH的增高平衡溶解度逐渐增大,最大平衡溶解度为5.10 mg/L;在32 g/L的十二烷基硫酸钠溶液中其平衡溶解度提高到706.97 mg/L;T-OA的表观油水分配系数为544.71（lg Papp=2.74）,且随溶液pH的增高逐渐降低.结论 T-OA的水溶性较差,可采用适当浓度的十二烷基硫酸钠和吐温80作为溶出介质,这为今后的剂型选择提供了参考.Objective To determine the equilibrium solubility of anticancer primer T-OA in buffer solution and surfactant solution with different pH （1-10）,and its apparent oil/water partition coefficient in n-octanol-water/buffer solution systems.Methods The concentration of T-OA in buffer solution and surfactant solution with different pH （1-10） was determined by using HPLC,and the apparent oil/water partition coefficient of T-OA was detected by using shake flask-HPLC.Results The equilibrium solubility of T-OA in buffer solution at 37℃ increased as pH rising,and the largest value was 5.10 mg/L.In 32 g/L lauryl sodium sulfate solution,the equilibrium solubility of T-OA increased to 706.97 mg/L.The apparent oil/water partition coefficient of T-OA was 544.71 （lg Papp =2.74） and increased as pH rising.Conclusion T-OA has poor water solubility,so lauryl sodium sulfate and polysorbate 80 with appropriate concentration can be taken as solubilizer.The study gives the reference for further preparation selection.

关 键 词：T-OA 平衡溶解度 表观油水分配系数 高效液相色谱法 

分 类 号：R283[医药卫生—中药学]