N-硬脂酰酪氨酸的理化性质研究  

Physicochemical properties of N-stearoyltyrosine

作　　者：殷莎[1] 唐双奇[1] 乐可佳[1] 刘坚华[1] 杨若林[1] 沈征武[1] 谢一凡[1] 陆阳[1] 

机构地区：[1]上海交通大学医学院药学系,上海200025

出　　处：《现代药物与临床》2014年第8期859-864,共6页Drugs & Clinic

基　　金：国家自然科学基金资助项目(30873057;81171245);上海市科委基础重点课题(11JC1406600);上海市科委科技支撑项目(12431900604)

摘　　要：目的表征N-硬脂酰酪氨酸及其盐的理化常数和血浆蛋白结合率。方法采用摇瓶法及HPLC-Uv法测定N-硬脂酰酪氨酸及其盐在不同介质和pH值下的溶解度、表观脂水分配系数，采用平衡透析法测定血浆蛋白结合率。结果N-硬脂酰酪氨酸盐的溶解度和血浆蛋白结合率明显优于其原型药物；N-硬脂酰酪氨酸的溶解度为（27．62±O．43）mg／L，其二钾盐的溶解度为（51．70±O．29）mg／L；N-硬脂酰酪氨酸及其二钾盐的血浆蛋白结合率分别为20．96％-23．1l％、35．41％-40．38％。结论N-硬脂酰酪氨酸成盐后其理化性质得到明显改善。Objective To characterize the physicochemical parameters and plasma binding ratio of N-stearoyltyrosine and its salts. Methods The solubility, the apparent partition coefficient of N-stearoyltyrosine and its salts in various media, and different pH values were measured via a shake flask method and high performance liquid chromatography with ultraviolet detection （HPLC-UV） method. The plasma protein binding ratio was conducted under dialysis equilibrium method. Results The solubility and plasma binding ratio of N-stearoyltyrosinates were better than those of N-stearoyltyrosine. The solubility of N-stearoyltyrosine was （27.62 ± 0.43） mg/L while that of dipotassium N-stearoyltyrosine （NsTyr-2K） （51.70 ± 0.29） mg/L. The plasma protein binding ratios were 20.96% -- 23.11% and 35.41% -- 40.38% for N-stearoyltyrosinate and NsTyr-2K, respectively. Conclusion It has the significant improvement of physicochemical properties of N-stearoyltyrosine after formation of salt.

关 键 词：N-硬脂酰酪氨酸 理化性质 血浆蛋白结合率 

分 类 号：R913[医药卫生—药学]