摘要
目的:测定佐米曲普坦在水和不同pH磷酸缓冲盐中的平衡溶解度以及在正辛醇-水和正辛醇-缓冲液体系中的表观油水分配系数。方法:采用HPLC法测定佐米曲普坦的浓度,用摇瓶法测定佐米曲普坦的表观油水分配系数。结果:佐米曲普坦在37℃水中的平衡溶解度为12.6g/L,在pH值3.6、4.5、6.0、6.8、7.4、8.0、9.0磷酸盐缓冲液中的平衡溶解度依次为1382.0、553.0、85.2、71.5、47.1、11.5、4.85g/L。佐米曲普坦在水中的表观油水分配系数Papp为0.013,在不同的pH值缓冲液中的表观油水分配系数依次为0.04、0.06、0.14、0.20、0.23、0.25、1.44。结论:在pH3.6～9.0范围内,随着pH值增加,佐米曲普坦平衡溶解度减小,而表观油水分配系数则增大。
Objective：To determine the equilibrium solubility of zolmitriptan in various media and its partition coefficients for the n-octanol-water/buffer solution systems.Methods：A high performance liquid chromatography was established and used to detect the concentration of zolmitriptan;the partition coefficients for the n-octanol-water/buffer solution systems of zolmitriptan were determined by shaking flask method.Results：The equilibrium solubility of zolmitriptan in water was 12.6 g/L at 37℃.The equilibrium solubility of zolmitriptan were 1 382.0,553.0,85.2,71.5,47.1,11.5 and 4.85 g/L in buffer solutions with pH values of 3.6,4.5,6.0,6.8,7.4,8.0 and 9.0 respectively.Papp of zolmitriptan was 0.013 in water and were 0.04,0.06,0.14,0.20,0.23,0.25 and 1.44 in buffer solutions with different pH values.Conclusion：In the range of pH3.6 to pH 9.0,the equilibrium solubility of zolmitriptan was decreased while the apparent oil/water partition coefficient was increased with the increasing of pH values.
出处
《重庆医科大学学报》
CAS
CSCD
北大核心
2010年第8期1235-1237,共3页
Journal of Chongqing Medical University
关键词
佐米曲普坦
平衡溶解度
表观油水分配系数
高效液相色谱法
Zolmitriptan
Equilibrium solubility
Apparent oil/water partition coefficient
High performance liquid chromatography.
作者简介
作者介绍：胡荣（1979-），女，硕士，研究方向：速释及缓控释制剂的研究。
通讯作者：黄华，女，教授，E-mail：huangh60@tom．com。
