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目的:测定穿心莲内酯和脱水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:采用摇瓶法测定穿心莲内酯和脱水穿心莲内酯的表观油水分配系数,采用HPLC法测定穿心莲内酯和脱水穿心莲内酯的浓度。结果:37℃下穿心莲内酯和脱水穿心莲内酯表观油水分配系数分别为3.90(log Papp=0.59)和19.75(log Papp=1.30)。结论:pH对穿心莲内酯和脱水穿心莲内酯表观油水分配系数有一定影响。在一定范围内,pH值增加可使穿心莲内酯和脱水穿心莲的表观油水分配系数减小。穿心莲内酯在pH6的磷酸盐缓冲液时表观油水分配系数最大[2.62(log Papp=0.42)],脱水穿心莲内酯则在pH5时达到最大[25.19(log Papp=1.40)]。
OBJECTIVE: To determine the apparent oil-water partition coefficients of andrographolide and dehydroandrographolide in n-octanol-water and n-octanol-buffer systems, providing references for the study of in vivo absorption. Methods: The apparent oil-water partition coefficients of andrographolide and dehydroandrographolide were determined by shake flask method. The concentrations of andrographolide and dehydroandrographolide were determined by HPLC. Results: The apparent oil-water partition coefficients of andrographolide and dehydroandrographolide at 37 ℃ were 3.90 (log Papp = 0.59) and 19.75 (log Papp = 1.30), respectively. CONCLUSION: The pH has an influence on the apparent oil-water partition coefficient of andrographolide and dehydroandrographolide. In a certain range, the increase of pH can reduce the apparent oil-water partition coefficients of andrographolide and dehydroandrographolide. Andrographolide showed the highest apparent water-oil partition coefficient [pH (pH = 6) [2.62 (log Papp = 0.42]] and dehydrated andrographolide reached the maximum at pH 5 [25.19 (log Papp = 1.40]].