Dennhardt R, Fricke M, Stöckert G
Anaesthesist. 1978 Jul;27(7):59-64.
A method is described enabling blood concentrations and urinary and biliary excretion of bupivacaine to be estimated in unanaesthetized rats. After enteral application of bupivacaine, the urine volumes of 40 rats are collected, cleared off and analysed by gas chromatography. 5 fractions are obtained, of which the structures are identified by mass spectrometry and nuclear magnetic resonance. The following five metabolites could be identified: (1) Desbutyl-bupivacaine, (2) 3'-Hydroxy-bupivacaine, (3) N-Butylpipecolyl-2-amide, (4, 5) mono-hydroxylated isomeres on the piperidine ring.
本文描述了一种能够在未麻醉大鼠中估算布比卡因血药浓度以及尿排泄和胆汁排泄情况的方法。经肠道给予布比卡因后，收集40只大鼠的尿量，进行处理并通过气相色谱法分析。得到5个组分，其结构通过质谱和核磁共振进行鉴定。可鉴定出以下5种代谢产物：（1）去丁基布比卡因，（2）3'-羟基布比卡因，（3）N-丁基哌啶-2-酰胺，（4,5）哌啶环上的单羟基异构体。
