目的 表征N-硬脂酰酪氨酸及其鹽的理化常數(shù)和血漿蛋白結(jié)合率。方法 采用搖瓶法及HPLC-UV法測定N-硬脂酰酪氨酸及其鹽在不同介質(zhì)和pH值下的溶解度、表觀脂水分配系數(shù)，采用平衡透析法測定血漿蛋白結(jié)合率。結(jié)果 N-硬脂酰酪氨酸鹽的溶解度和血漿蛋白結(jié)合率明顯優(yōu)于其原型藥物；N-硬脂酰酪氨酸的溶解度為（27.62±0.43）mg/L，其二鉀鹽的溶解度為（51.70±0.29）mg/L；N-硬脂酰酪氨酸及其二鉀鹽的血漿蛋白結(jié)合率分別為20.96%～23.11%、35.41%～40.38%。結(jié)論 N-硬脂酰酪氨酸成鹽后其理化性質(zhì)得到明顯改善。

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.

國家自然科學(xué)基金資助項目（30873057，81171245）；上海市科委基礎(chǔ)重點課題（11JC1406600）；上海市科委科技支撐項目（12431900604）