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3.68，24.81，6.25，4.91，6.53，5.98，4.20，4.46，6.39，5.97，17.41 μg/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。
Abstract:
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 NC/P4 were more than 5,indicating that NCP4 was not easy to absorb on mucosa.
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