正相HPLC-直链淀粉手性固定相拆分硼替佐米及其光学异构体

Separation of Bortezomib and Its Optical Isomers on Amylose Chiral Stationary Phase by NP-HPLC

摘要: 目的建立硼替佐米光学异构体高效液相手性分离方法。方法在Chiralpak AD-H直链淀粉-三(3,5-二甲基苯基氨基甲酸酯)手性固定相手性柱上拆分硼替佐米异构体，考察流动相中不同浓度的异丙醇与乙醇、柱温和流速对手性拆分的影响。结果最佳拆分流动相组成为正己烷和改性调节剂，最佳色谱条件为正己烷-异丙醇-乙醇(86∶6∶8)，流速为0.6 mL·min^-1，柱温30 ℃。结论本方法可方便地拆分硼替佐米异构体，为硼替佐米原料药质量标准和质量控制提供了科学依据。

Abstract: OBJECTIVE To develop a normal phase HPLC method for the separation of bortezomib and its optical isomers. METHODS The chiral separation of bortezomib and its optical isomers on amylase tris (3,5-dimethylphenylcarbamate) chiral stationary phase was carried out. The effectes of different proportions of n-hexane/isopropanol/ethanol in mobile phase were investigated, and the flow rate of mobile phase and column temperature were also optimized. RESULTS The mobile phase of the established method was n-hexane-isopropanol-ethanol(86∶6∶8), with the flow rate of 0.6 mL·min^-1. The column temperature was set at 30 ℃. CONCLUSION The method is simple, rapid and can be used for analysis of bortezomib and its optical isomers.