Chiral separation of Raltitrexed by cyclodextrin-modified micellar electrokinetic chromatography
 

Chiral separation of Raltitrexed bycyclodextrin-modified micellar electrokinetic chromatography


 Yi Liu1, Xiaofang Fu1, Chao Ma2, Jiasheng Zhong2, Yiping Liao1, Huwei Liu1*
College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China
2Beijing Mediking Pharmaceutical Cooperate Limited, Beijing 102209, China

 

Raltitrexed (RD), an antineoplastic agent that has been applied to the treatment of advanced colorectal cancer, has potential for more convenience and less toxicity [1, 2], which has a chiral center in its molecular structure. In this paper, a rapid and effective method was developed for the chiral separation of raltitrexed enantiomers by carboxymethyl-beta-cyclodextrin (CM-β-CD) modified micellar electrokinetic chromatography (MEKC). Optimization of conditions including the pH, concentration of buffers, cyclodextrin (CD) and sodium dodecylsulfate (SDS) concentration in the buffer system, applied voltage, and capillary temperature were also investigated. The results indicated that the enantiomers of raltitrexed could be separated with satisfactory resolution and linear response under the optimal conditions (see Fig 1). Furthermore, a purity test of a real synthetic drug sample was also carried out, demonstrating the usefulness of this method.

致谢:国家自然科学基金委员会资助项目,批准号:20675004,90709021


参考文献
[1] A.L. Jackman, D.C. Farrugia, W. Gibson, R. Kimbell, K.R. Harrap, T.C. Stephens, M. Azab, F.T. Boyle, Eur. J. Cancer, 31A (1995) 1277.
[2] J.R. Zalcberg, D. Cunningham, E. VanCutsem, E. Francois, J. Schornagel, A. Adenis, M. Green, A. Iveson, M. Azab, I. Seymour, J. Clin. Oncol., 14 (1996) 716.




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