CBUA-NO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 CBUA-NO

目的:测定2-(4-氯苄叉基)-3-羰基熊果酸-(2-硝氧乙基)酯(CBUA-NO)的平衡溶解度和表观油水分配系数。方法:HPLC法测定CBUA-NO在不同表面活性剂中的溶解度及其在不同pH磷酸盐缓冲液介质中的油水分配系数。结果:不同表面活性剂对CBUA-NO的增溶作用有差异,CBUA-NO在1mg·L^(-1)聚山梨酯80中溶解度最大;正辛醇-水体系中,CBUA-NO油水分配系数随油/水比例的升高而增大,pH=7.6,O/W=1时,CBUA-NO的油水分配系数最大,lgP=2.02。结论:建立的方法准确、可靠,可快速测定CBUA-NO的平衡溶解度和表观油水分配系数,为其体内动态的进一步研究提供依据。

OBJECTIVE To determine the equilibrium solubility and apparent oil/water partition coefficients（logP）of 2-（4-chlorobenzylidene）-3-O-ursolic acid-（2-nitroxyethyl）ester（CBUA-NO）.METHODS A high performance liquid chromatography（HPLC）method was established to determine the equilibrium solubility of CBUA-NO in different surfactants.And the logP was tested in phosphate buffered saline（PBS）at different pH values.RESULTS The interaction between CBUA-NO and various surfactants was observed.The maximum solubility of CBUA-NO was found in 1 mg·L^-1 Tween-80.The lgP of CBUA-NO increased with the increase of oil/water ratio in n-octanol/buffer solution system.And the oil-water partition coefficients had a maximum value at pH=7.6,O/W=1,lgP=2.02.CONCLUSION The established method is accurate and repeatable,which can be used for the rapid determination of the equilibrium solubility and logP of CBUA-NO.These data provide the proof for profound study on the process in vivo.