论文部分内容阅读
目的用高效液相色谱法(HPLC)测定特考韦瑞(ST-246)在37℃水和不同pH缓冲液的平衡溶解度,以及在正辛醇-水/缓冲液系统的油水分配系数。方法采用摇瓶法测定平衡溶解度,通过药物分配平衡后在油相及水相的浓度比,计算油水分配系数。结果 ST-246在37℃水的平衡溶解度为3.35 mg/L,ST-246的表观油水分配系数为230.49(lgP=2.36),在正辛醇/pH4.0缓冲液的油水分配系数最大,为779(lgP=2.89)。结论 ST-246的水溶性较差,脂溶性不佳,其水中溶解度呈pH依赖性,增大pH可增加其溶解度。
OBJECTIVE To determine the equilibrium solubility of teicoplanin (ST-246) in water and different pH buffers at 37 ° C and the partition coefficient of oil and water in n-octanol-water / buffer system by high performance liquid chromatography (HPLC) Methods The equilibrium solubility was determined by shake flask method. The oil-water partition coefficient was calculated by the concentration ratio of the drug in the oil phase and the water phase. Results The equilibrium water solubility of ST-246 was 3.35 mg / L at 37 ℃. The apparent water-oil partition coefficient of ST-246 was 230.49 (lgP = 2.36) Is 779 (lgP = 2.89). Conclusion ST-246 has poor water-solubility and poor lipid-solubility. Its solubility in water is pH-dependent. Increasing pH can increase its solubility.