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J Sep Sci ; 47(12): e2400190, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38894562

RESUMEN

An efficient method for the continuous separation of Voriconazole enantiomers was developed using sulfobutyl ether-ß-cyclodextrin (SBE-ß-CD) as a chiral selector in high-speed countercurrent chromatography (HSCCC) with different types. The separation was performed using a two-phase solvent system consisting of n-hexane/ethyl acetate/100 mmol/L phosphate buffer solution (pH = 3.0, containing 50 mmol/L SBE-ß-CD) (1.5:0.5:2, v/v/v). A fast and predictable scale-up process was achieved using an analytical DE HSCCC instrument. The optimized parameters were subsequently applied to a preparative Tauto HSCCC instrument, resulting in consistent separation time and enantiomeric purity, with throughput boosted by a remarkable 11-fold. Preparative HSCCC successfully separated 506 mg of the racemate, delivering enantiomers exceeding 99% purity as confirmed by high-performance liquid chromatography analysis. This investigation presents an effective methodology for forecasting the HSCCC scale-up process and attaining continuous separation of chiral drugs.


Asunto(s)
Distribución en Contracorriente , Voriconazol , Distribución en Contracorriente/métodos , Estereoisomerismo , Voriconazol/química , Voriconazol/aislamiento & purificación , Cromatografía Líquida de Alta Presión , beta-Ciclodextrinas/química
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