Reactive extraction is an emerging technology for large-scale continuous resolution of drug enantiomers. The enantioselective extraction of R,S-naproxen by hydrophilic HP-β-CD in 1,2-dichloroethane was studied at 5℃...Reactive extraction is an emerging technology for large-scale continuous resolution of drug enantiomers. The enantioselective extraction of R,S-naproxen by hydrophilic HP-β-CD in 1,2-dichloroethane was studied at 5℃. The experimental data were described by a reactive extraction model with a homogeneous aqueous phase reaction of R,S-naproxen with HP-β-CD which couples a complete description of chemical equilibria in aqueous phase with the overall phase equilibria of the system. Important parameters of this model were determined experimentally. The physical distribution coefficients for molecular and ionic NAP were 0.041 and 1.730, respectively. Here we show that the efficiency of extraction depends strongly on two process variables including pH and HP-β-CD concentration. The model predictions are compared graphically with the results of pre- vious experiments and there is a good agreement between each other. By the use of modeling and experiment, an optimized extraction condition with pH of 2.5 and HP-β-CD concentration of 0.1 mol/L was obtained with high enantioselectivity （a） of 1.59 and performance factor （pf） of 0,049. The model gives a good means of predicting enantiomers partitioning over a range of experimental conditions.展开更多
基金supported by the National Natural Science Foundation of China (20976041)Program for New Century Excellent Talents in University,Hunan Provincial Natural Science Foundation (10JJ1004)+1 种基金Aid Program for Science and Technology Innovative Research Team in Higher Educational Instituions of Hunan Provincethe Open Fund Project of Key Laboratory in Hunan University (09K095)
文摘Reactive extraction is an emerging technology for large-scale continuous resolution of drug enantiomers. The enantioselective extraction of R,S-naproxen by hydrophilic HP-β-CD in 1,2-dichloroethane was studied at 5℃. The experimental data were described by a reactive extraction model with a homogeneous aqueous phase reaction of R,S-naproxen with HP-β-CD which couples a complete description of chemical equilibria in aqueous phase with the overall phase equilibria of the system. Important parameters of this model were determined experimentally. The physical distribution coefficients for molecular and ionic NAP were 0.041 and 1.730, respectively. Here we show that the efficiency of extraction depends strongly on two process variables including pH and HP-β-CD concentration. The model predictions are compared graphically with the results of pre- vious experiments and there is a good agreement between each other. By the use of modeling and experiment, an optimized extraction condition with pH of 2.5 and HP-β-CD concentration of 0.1 mol/L was obtained with high enantioselectivity （a） of 1.59 and performance factor （pf） of 0,049. The model gives a good means of predicting enantiomers partitioning over a range of experimental conditions.
