黄癸素平衡溶解度和表观油水分配系数的测定

Determination of equilibrium solubility and apparent oil/water partition coefficient of berberine α-hydroxy β-decanoylethyl sulfonate

目的:研究黄癸素(berberineα-hydroxyβ-decanoylethyl sulfonate,HB)在不同pH磷酸盐缓冲液(PBS)中的平衡溶解度以及在正辛醇-水/PBS中的表观油水分配系数,为开发新型的HB制剂提供依据。方法:采用高效液相色谱法(HPLC)测定HB在不同pH的PBS中的平衡溶解度;采用摇瓶法测定HB在正辛醇-水/PBS中的表观油水分配系数。结果:37℃时HB在水中的平衡溶解度为378.5μg·m L^(-1),pH为5时溶解度最小;HB的表观油水分配系数Papp为0.096,pH>5时,Papp<1,pH<5时,Papp>1。结论:HB的平衡溶解度与表观油水分配系数与介质的pH有关,推测其进入胃肠道后不易被吸收。

Objective： To determine the equilibrium solubility and apparent partition coefficient （Papp） of berberine α-hydroxy β-decanoylethyl sulfonate （HB） in a series of phosphate buffer solutions （PBS） of different pHs to provide a theoretical basis for the exploitation of HB preparations. Methods： A high performance liquid chromatography （HPLC） method was established and used to detect the concentration of HB in water and buffer solutions; the partition coefficients of HB in n-oetanol-water/buffer solution systems were determined by shaking flask method. Results： The equilibrium solubility of HB in water was 378.5 μg. mL-1 at 37 ℃ and the solubility was the lowest at pH 5. The Papp of HB was 0.096, and it was 〈 1 at pH of 〉 5 and 〉 1 at pH of 〈 5. Conclusion： The equilibrium solubility of HB and the apparent oil-water partition coefficient are related to the pH of the medium, suggesting that it is not easily absorbed after entering the gastrointestinal tract.