Bailey D N, Bessler J B, Sawrey B A
Department of Pathology, University of California Medical Center, San Diego 92103-8320, USA.
J Anal Toxicol. 1997 Jan-Feb;21(1):41-3. doi: 10.1093/jat/21.1.41.
Cocaine (COC)- and cocaethylene (CE)-creatinine clearance ratios (CCR) were determined in five patients. In each case, COC:CCR greatly exceeded CE:CCR, and in four patients the data suggested renal tubular secretion of COC. For all patients, some renal tubular reabsorption of CE was apparent. These findings may be due, at least in part, to the greater hydrophobicity of CE relative to COC and to the lower pKb of CE (8.23) than that of COC (8.60). The pKb of CE was determined by titrimetry and is reported here for the first time. These data may be useful in investigating the pharmacokinetic profiles of COC and CE in humans and may also help to explain the longer plasma half-life of CE relative to that of COC.
测定了5例患者的可卡因（COC）和可口卡因（CE）-肌酐清除率比值（CCR）。在每种情况下，COC:CCR都大大超过CE:CCR，并且在4例患者中，数据提示存在COC的肾小管分泌。对于所有患者，CE的肾小管重吸收均较为明显。这些发现可能至少部分归因于CE相对于COC具有更高的疏水性以及CE的pKb（8.23）低于COC的pKb（8.60）。CE的pKb通过滴定法测定，本文首次报道。这些数据可能有助于研究COC和CE在人体内的药代动力学特征，也可能有助于解释CE相对于COC更长的血浆半衰期。
