毛细管区带电泳法拆分手性药物萘普生和氟联苯丙酸

 70-72 -------------------------------------------------------------------------------- 以β-环糊精(CD)作为手性选择剂 ，用毛细管区带电泳法成功地拆分了两种弱酸性药物萘普生(naproxen)和氟联苯丙酸(flurb iprofen)，并比较了4种环糊精［β-环糊精(β-CD)、二甲基-β-环糊精( DM-β-CD)、羟丙基-β-环糊精(HP-β-CD)和三甲基-β-环糊精( TM-β-CD)］对手性拆分的影响，同时测定了萘普生对映体在不同环糊精中的出峰次 序。通过实验，发现对于此类化合物拆分的最佳pH值为5左右，即接近于该类化合物的pK a值。该方法适用于酸性手性药物的拆分。

Chiral Separation of Naproxen and Flurbiprofen by Capillary Electrophoresis

The acidic chiral drugs naproxen and flurbiprofen were successfully separated into two enantiomers when beta-cyclodextrins (beta-CDs) were used as chiral selectors by capillary zone electrophoresis, under the conditions of 0.1 mol/L phosphate buffer with pH 4.92. The comparison of four CDs, namely beta-CD, DM-beta-CD, HP-beta-CD and TM-beta-CD for chiral separation was made. Naproxen can be separated by either beta-CD or its derivatives, while flurbiprofen can only be separated by TM-beta-CD among the CDs. The elution order of enantiomers of naproxen in different CDs was also studied, and the R form always eluted before S form when any of the four CDs was used as chiral selectors. The method of chiral separation for weak acidic compounds was also developed. It was proved that the optimum pH value for their chiral separation was about 5, close to its pKa value.