人血清白蛋白柱上药物的手性拆分

Enantiomeric Separation of Drug on Human Serum Albumin Column

考察了４种酸性药物和１种中性药物对映体在人血清白蛋白手性固定相上的保留行为。这５种药物与人血清白蛋白结合的亲和力高，难于实现快速分离，作者提出在流动相中加入短链脂肪酸－正己酸，可快速手性拆分非诺洛芬、萘普生和布洛芬。酮基布洛芬对映体分离选择性随乙腈浓度升高而增大，流动相中加入适量异丙醇可使对映体选择性大大增加（α～１．２３），华法令同样可取得很好分离。

The enantiomeric separation of four acidic drugs and one neutral drug on human serum albumin(HSA) chiral stationary phase was described. The retention behavior of enatiomers of these drugs was investigated on three kinds of mobile phase, and the influence of temperature, concentration of acentonitrile and pH on enantiomeric separationof warfarin was also investigated. All five drugs show high affinity to HSA and strong retention on HSA column, only war farm and ketoprofen can be chirally resolved and eluted out under suitable composition of acentonitrile/water in 20 min; chiral resolution of fenoprofen, naproxen and ibuprofen are achieved with 10 mmol/L n-hexoic acid used as displacing agent in mobile phase. The enantioselectivity of ketoprofen being low, its baseline enantiomeric separation can be achieved by the addition of 4% isopropanol to 15% acetonitrile aqueous solution as mobile phase. A good separation for war farm is likewise realized.