Resolution Of Propitocaine Hydrochloride And Bupropion Hydrochloride Enantiomers By HPLC Chiral Mobile Phase Additive

The chirality is the basic feature of organisms systems. The enantiomers will beidentified as different molecules when chiral drugs enter into the organisms; They will showthe different pharmacokinetic, pharmacological and toxicological characteristics and so on. So,we are looking for ingle-enantiomer drugs.It is better selectivity, higher activity, less toxicity,greater efficacy. It is of great significance for correct evaluation the racemic drugs anddirecting clinical therapy. Thus, the study of chirality has become one of the new drugs topics,which can not be avoided.In this paper, under alkaline conditions，the β-CD and chloroacetic acid are used as rawmaterials. Without water, the carboxymethyl-β-cyclodextrin (in short CM-β-CD) wassynthetised. It was characterized by IR spectroscopy, and its degree of substitution wasdetermined. For the prilocaine hydrochloride and bupropion hydrochloride are widely usedwith raceme in the clinical. The chiral separation of them were studied by reversed phasehigh-performance liquid chromatography with CM-β-CD as chiral mobile phase additive. Themethods of enantiomers separation were successfully established on the C18column. Theeffects of organic modifier percentage, the type and concentration of additives, and the pHand flow rate of chiral mobile phase on the resolution have been studied more systematiclly.The results show that the prilocaine hydrochloride enantiomers was separated whenusing acetonitrile, methanol, water (15:60:25,v/v/v) as the mobile phase. The pH value ofmobile phase was4.80and the flow rate was0.40mL.min-1. The concentration of CM-β-CDwas0.4g L-1. The ultraviolet detector was set at202nm. The resolution of enantiomers was1.41. The bupropion hydrochloride enantiomers was separated when using acetonitrile,methanol,water (40:30:30,v/v/v) as the mobile phase. The pH value of mobile phase was4.1and the flow rate was1.20mL.min-1. The concentration of CM-β-CD is0.50g L-1. Theultraviolet detector was set at214nm. The resolution of enantiomers was1.20.