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Distribution behavior of some drug enantiomers in an aqueous two-phase system using counter-current extraction with protein
Authors:T Arai  H Kuroda
Institution:(1) Analytical Research Center, Production Technology Research Laboratories, Daiichi Pharmaceutical Co., Ltd., 1-16-13 Kitakasai, Edogawa-ku, 134 Tokyo, Japan
Abstract:Summary The partial resolution of some drug enantiomers by counter-current extraction in an aqueous two-phase system using bovine serum albumin (BSA) or ovomucoid (OVM) as chiral discriminator is described. The phase system was prepared with dextran 40, polyethylene glycol and a protein. Ofloxacin (OFLX) enantiomer was well recognized by the BSA system, whereas the enantiomers of carvedilol (beta-blocker) and DG-5128 (a new oral hypoglycaemic drug) were hardly recognized by the OVM system. The distribution coefficients of (S)-, (R)- and rac-OFLX varied with pH. Good enantioselectivity for OFLX was obtained at relatively high pH (ge pH 9). The crude optically enriched OFLX enantiomers were extracted from the aqueous fractions and finally purified by thin-layer chromatography.
Keywords:Column liquid chromatography  Counter-current extraction  Chiral resolution  Ofloxacin enantiomers  Aqueous two-phase system
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