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目的 研究苯丙哌林在健康人体内的对映体选择性动力学过程。方法 以非手性HPLC法测定不同时刻血浆样品中苯丙哌林的浓度 ,再用手性HPLC法测定两对映体的浓度比值 ,计算得到血浆中 (R) 和 (S) 苯丙哌林的浓度。结果 6名受试者血浆中S体浓度始终高于R体 ,S体的AUC0 -t和Cmax的均值分别为R体的 2 12倍和2 18倍 ,但二者的T1/ 2 无显著性差异。服药后 0 5h血浆中S/R对映体浓度比值高达 3 8,此后迅速下降 ,2h后约为 2 2 ,基本保持恒定到 2 4h。结论 口服 (± ) 苯丙哌林后 ,两对映体在人体内的药物动力学过程具有显著的立体选择性。
Objective To study the enantioselective kinetics of benproperine in healthy volunteers. Methods The concentration of benproperine in plasma samples at different time was determined by achiral HPLC method. The concentration ratio of two enantiomers was determined by chiral HPLC and the concentrations of (R) and benproperine (S) in plasma were calculated. concentration. Results The plasma concentration of S was always higher in the 6 subjects than in the R group. The mean values of AUC0-t and Cmax in the S body were 2 12 and 2 18 times of those in the R body, respectively, but the T1 / 2 values of the two subjects were not significant difference. The ratio of S / R enantiomer concentrations in plasma at 0 5h after treatment was as high as 38, then decreased rapidly after 2h and remained about 22 after 2h, with a constant value of 24 h. Conclusions After oral administration of (±) benproperine, the two enantiomers have significant stereoselectivity in the pharmacokinetics of the human body.