化合物NCP4在不同pH条件下的平衡溶解度及油水分配系数  

Determination of equilibrium solubility of NCP4 and its partition coefficient

作　　者：牛成成[1] 唐开勇 潘俊芳 方通 张朝辉[1] 

机构地区：[1]江苏大学药学院,镇江212013 [2]上海华拓医药科技发展股份有限公司,上海201203

出　　处：《中国药科大学学报》2012年第1期43-45,共3页Journal of China Pharmaceutical University

基　　金：国家"重大新药创制"科技重大专项资助项目(No.2011ZX11401)~~

摘　　要：采用HPLC法测定化合物NCP4在水、盐酸溶液(pH 1.0)和不同pH磷酸盐缓冲液中的平衡溶解度;采用摇瓶法测定NCP4在正辛醇-水、正辛醇-盐酸(pH 1.0)和正辛醇-缓冲液体系中的油水分配系数。在37℃条件下,NCP4在水、盐酸溶液(pH 1.0)、磷酸盐缓冲液(pH 2.0,3.0,4.0,5.0,6.0,6.8,7.0,7.4,8.0)中的平衡溶解度分别为3.68,24.81,6.25,4.91,6.53,5.98,4.20,4.46,6.39,5.97,17.41μg/L。NCP4在水、盐酸(pH 1.0)、磷酸盐缓冲液(pH 2.0,3.0,4.0,5.0,6.0,6.8,7.0,7.4,8.0)中的lgP(O/W)分别为7.31,7.37,未检测到(ND),ND,7.40,ND,ND,7.57,6.73,7.43,7.44。通过对NCP4平衡溶解度和油水分配系数的测定,可为其剂型的开发提供理论基础。该药的lgP(O/W)大于5,说明不易透过黏膜吸收。Equilibrium solubility of NCP4 at different pH levels was determined by HPLC and shaking flash method was used to detect its partition coefficients in the n-octanol-water,hydrochloric acid,buffer solution systems.With the condition of 37 °C,the equilibrium solubility of NCP4 in water,hydrochloric acid（pH 1.0） andphosphate buffer solution（pH 2.0,3.0,4.0,5.0,6.0,6.8,7.0,7.4,8.0）were 3.68,24.81,6.25,4.91,6.53,5.98,4.20,4.46,6.39,5.97,17.41 μg/L.In the addition,the lgP（O/W） of NCP4 also in the above condition were 7.31,7.37,not detected（ND）,ND,7.40,ND,ND,7.57,6.73,7.43,7.44,respectively.Determination of equilibrium solubility and partition coefficients of NCP4 can provide the basis for its dosage form.The detected values of lgP（O/W） of NCP4 were more than 5,indicating that NCP4 was not easy to absorb on mucosa.

关 键 词：NCP4 抗肿瘤药 平衡溶解度 油水分配系数 

分 类 号：R914[医药卫生—药物化学]