目的测定新穿心莲内酯在正辛醇-水和正辛醇-缓冲液体系中的表观油水分配系数,为体内吸收研究提供参考。方法采用高效液相色谱(HPLC)法测定新穿心莲内酯的浓度,采用摇瓶法测定新穿心莲内酯的表观油水分配系数。结果37℃下新穿心莲内酯的表观油水分配系数为1.75(10gPapp=0.24),在pH2—12的缓冲液中测得的分别为1.63、1.49、1.62、2.18、2.78、2.32、2.20、2.10、2.09、1.96、1.72、1.19。结论pH值对新穿心莲内酯的表观油水分配系数有一定影响。在一定范围内,pH值增加可使新穿心莲内酯的表观油水分配系数减小。新穿心莲内酯在pH6磷酸盐缓冲液时表观油水分配系数最大[2.78(10gPapp=0.44)]。
Objective To determinate the apparent oil-water partition coefficient of neoandrographolide in n-octanolwater and n-octanol-buffer system, and to provide reference for the in vivo absorption study. Methods The concentration of neoandrographolide was determined by HPLC. The apparent oil-water partition coefficient of neoandrographolide was measured by shaking flask method. Results The apparent oil-water partition coefficient of neoandrographolide was 1.75 ( log Papp = 0.24) in water at 37℃. While the pH values of the buffer solution were from 2 to 12, the apparent oil-water partition coefficients were 1.63, 1.49, 1.62, 2. 18, 2.78, 2.32, 2.20, 2. 10, 2.09, 1.96, 1.72, and 1. 19, respectively. Conclusion The apparent oil-water partition coefficient of neoandrographolide was influenced by pH value, and the higher pH can decrease its relevant apparent oil-water partition coefficient. Neoandrographolide has the highest partition coefficient in phosphate buffer with pH 6.