Tucker G T, Mather L E, Lennard M S, Gregory A
Department of Medicine and Pharmacology, University of Sheffield, Royal Hallamshire Hospital.
Br J Anaesth. 1990 Sep;65(3):333-6. doi: 10.1093/bja/65.3.333.
A chiral high pressure liquid chromatography method was developed to measure the separate isomers of prilocaine in plasma after administration of the racemate. The concentrations of the isomers in six patients were similar (S(+)/R(-) = 1.06 (SD 0.06)) after brachial plexus block with 1.5% (RS)-prilocaine hydrochloride 35 ml, suggesting that a higher systemic safety margin may not be achieved by substituting racemic prilocaine by one of its isomers. Much higher plasma concentrations of the S(+)- than the R(-)-form after oral administration of 300 mg of the racemate (n = 4) indicated a large difference in intrinsic metabolic clearance of the isomers on first pass through gut, liver or both organs.
建立了一种手性高效液相色谱法，用于测定消旋体给药后血浆中丙胺卡因的对映异构体。6例患者在臂丛神经阻滞中使用35 ml 1.5%（RS）-盐酸丙胺卡因后，其异构体浓度相似（S(+)/R(-)=1.06（标准差0.06）），这表明用其一种异构体替代消旋丙胺卡因可能无法实现更高的全身安全边际。口服300 mg消旋体（n = 4）后，S(+)-型的血浆浓度比R(-)-型高得多，这表明异构体在首次通过肠道、肝脏或两个器官时，其内在代谢清除率存在很大差异。
