摘要
目的测定常绿钩吻碱(sempervirine,SPV)在不同pH磷酸盐缓冲液(PBS)中的平衡溶解度和油水分配系数,考察常绿钩吻碱的解离常数,为常绿钩吻碱的剂型开发提供一定的依据。方法采用超高效液相色谱法(UPLC)结合摇瓶法测定常绿钩吻碱在不同pH的磷酸盐缓冲液中的平衡溶解度和正辛醇-磷酸盐缓冲液中的油水分配系数;采用紫外分光光度法测定常绿钩吻碱的解离常数。结果常绿钩吻碱在pH 1.2~7.4的磷酸盐缓冲液中的溶解度为285.356~557.945 mg·L^(-1),油水分配系数在0.316~5.803,解离常数pKa为11.10。结论pH值影响常绿钩吻碱平衡溶解度和油水分配系数,常绿钩吻碱的低溶解度与解离常数可能影响其体内吸收。
Objective The equilibrium solubility and oil-water distribution coefficient of sempervirine(SPV)in phosphate buffers(PBS)with different pH values were determined,and the dissociation constant of sempervirine was investigated,which provided some basis for the development of preparation of sempervirine.Methods Ultra high performance liquid chromatography(UPLC)and flask shaking method were used to determine the equilibrium solubility of sempervirine and the oil-water distribution coefficient of n-octyl alcohol-PBS in different pH.The dissociation constant of sempervirine was determined by ultraviolet spectrophotometry.Results The solubility of sempervirine in PBS at pH 1.2~7.4 ranged from 285.356 mg·L^(-1) to 557.945 mg·L^(-1),and the oil-water distribution coefficient ranged from 0.316 to 5.803.The dissociation constant pKa was 11.10.Conclusion The pH value affects the equilibrium solubility and oil-water distribution coefficient of sempervirine,and the low solubility and dissociation constant of sempervirine may affect its in vivo absorption.
作者
蒋文文
张媛洁
李高攀
宋煜
吴水生
JIANG Wenwen;ZHANG Yuanjie;LI Gaopan;SONG Yu;WU Shuisheng(School of Pharmacy,Fujian University of Traditional Chinese Medicine,Fuzhou 350122,China)
出处
《药学研究》
CAS
2021年第10期656-659,共4页
Journal of Pharmaceutical Research
基金
福建省科技厅引导性项目(No.2020Y0051)
福建省财政资助专项(No.X2019003-财政专项)。
