HPLC法测定川芎嗪的平衡溶解度和表观油水分配系数

Determination of the equilibrium solubility and oil/water apparent partition coef cient(P) of tetramethylpyrazine by HPLC

目的测定川芎嗪在水、常见非水溶媒和缓冲液中的平衡溶解度及表观油水分配系数。方法采用高效液相法测定川芎嗪的平衡溶解度,采用摇瓶法测定表观油水分配系数。结果 25℃川芎嗪在水、甘油、甲醇、乙醇和正辛醇中平衡溶解度分别为5.09、31.98、507.39、338.79和58.89mg.mL-1;37℃川芎嗪在正辛醇-水表观油水分配系数为18.27(lgPapP=1.26),在正辛醇-pH5.0磷酸缓冲溶液中表观油水分配系数较大,P=26.21(lgPapP=1.42)。结论川芎嗪微溶于水,略溶于甘油,易溶于甲醇、乙醇,能溶于正辛醇;川芎嗪在肠道不同部位溶散情况略有差异,由大到小顺序为:十二指肠>回肠>空肠>结肠。

OBJECTIVE To determine the equilibrium solubility and oil/water apparent partition coef cient （P） of tetramethylpyrazine in water, non-aqueous solvents and a series of buffer solutions of different pH. METHODS The apparent solubility was determined by saturation method, and P was calculated with concentration ratio of drug in oil and water phase after partition equilibrium. RESULTS The equilibrium solubilities of tetramethylpyrazine in water,glycerin,methanol,ethanol,n-octanol were 5.09,31.98,507.39,338. 79 and 58.89mg ·mL^-1＇ at 25℃. The n-octanol/water partition coefficient of tetramethylpyrazine was 26. 21 （ lgPapP = 1.42 ）. The n-octanol/pH = 5.0 buffer solution was 18.27 （ lgPapP = 1.26）. CONCLUSION Tetramethylpyrazine is slightly soluble in water, glycerin, soluble in methanol, ethanol and can be dissolved in octanol;The absorption of tetramethylpyrazine in different parts of the intestine are slightly different. The descending order is duodenum 〉 ileum 〉 jejunum 〉 colon.