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目的:测定番荔枝总内酯的平衡溶解度以及表观油水分配系数,为体内吸收和设计其新剂型提供参考。方法:采用饱和法和超声振荡法分别测定番荔枝总内酯在不同溶剂中的平衡溶解度以及在正辛醇-水/缓冲溶液中的表观油水分配系数,采用比色法测定番荔枝总内酯的含量。结果:番荔枝总内酯在水和石油醚中的溶解度分别为0.06g·L-1和1.27g·L-1,其在乙醚中的溶解度最高,为482.28g·L-1;超声振荡80min后P值达到平衡,25℃下番荔枝总内酯的表观正辛醇/水分配系数P为54.91(logP=1.74),在pH 6.8的缓冲溶液中的表观分配系数最大为32.03(logP=1.51)。结论:番荔枝总内酯易溶于常用的有机溶剂,在中等极性溶剂的溶解度较大;平衡方法、平衡时间及pH对油水分配系数都有一定的影响。
OBJECTIVE: To determine the equilibrium solubility and apparent oil-water partition coefficient of total lactone from Annona auricula, and to provide reference for in vivo absorption and design of new dosage forms. Methods: The equilibrium solubility of total lactone in litchi and the apparent oil-water partition coefficient in n-octanol-water / buffer solution were determined by the method of saturation and ultrasonic vibration respectively. Ester content. Results: The solubility of total lactones in water and petroleum ether were 0.06g · L-1 and 1.27g · L-1, respectively. The solubility of total lactone in ether was 482.28g · L-1; After the P value reached equilibrium, the apparent n-octanol / water partition coefficient P of the total lactone of Annona squama was 54.91 (logP = 1.74) at 25 ℃ and the maximum apparent partition coefficient was 32.03 (logP = 1.51). CONCLUSION: The total lactone of Annona asparagus is easily soluble in common organic solvents and has a relatively high solubility in medium polar solvents. The equilibrium method, equilibration time and pH have a certain impact on the oil-water partition coefficient.