Boudesocque Leslie, Forni Luciano, Martinez Agathe, Nuzillard Jean-Marc, Giraud Matthieu, Renault Jean-Hugues
Institut de Chimie Moléculaire de Reims UMR CNRS 7312, SFR Cap'Santé, Université de Reims Champagne-Ardenne, Reims, France; UMR INRA 1282 Infectiologie Santé Publique, Université de Tours François Rabelais, UFR Sciences Pharmaceutiques Philippe Maupas, Tours, France.
Lonza Ltd, Valais Work CH-3930 Visp, Switzerland.
J Chromatogr A. 2017 Sep 1;1513:78-83. doi: 10.1016/j.chroma.2017.07.003. Epub 2017 Jul 15.
Dirucotide is a synthetic drug candidate for the treatment of multiple sclerosis. This 17-aminoacid peptide was successfully purified by ion exchange centrifugal partition chromatography. The optimized conditions involved the biphasic methyl tert-butyl ether/acetonitrile/n-butanol/water (2:1:2:5, v/v) solvent system in the descending mode, the di(2-ethylhexyl)phosphoric acid cation-exchanger with an exchanger (di(2-ethylhexyl)phosphoric acid)/dirucotide mole ratio of 100 and Ca ions in aqueous solution as displacer. Critical impurities were efficiently eliminated and dirucotide was recovered in high yield and purity (69% and 98%, respectively) and with a productivity of 2.29g per liter of stationary phase per hour.
地鲁库肽是一种用于治疗多发性硬化症的合成候选药物。这种17个氨基酸的肽通过离子交换离心分配色谱法成功纯化。优化条件包括在下行模式下使用双相甲基叔丁基醚/乙腈/正丁醇/水（2:1:2:5，v/v）溶剂系统、二（2-乙基己基）磷酸阳离子交换剂，其中交换剂（二（2-乙基己基）磷酸）/地鲁库肽的摩尔比为100，以及水溶液中的钙离子作为置换剂。关键杂质被有效去除，地鲁库肽以高产率和高纯度回收（分别为69%和98%），每升固定相每小时的生产率为2.29克。
