Tsai T H, Hung L C, Chen C F
Department of Pharmacology, National Research Institute of Chinese Medicine, National Yang-Ming University, Taipei, Taiwan.
J Pharm Pharmacol. 1999 Aug;51(8):911-5. doi: 10.1211/0022357991773339.
The biliary excretion of chloramphenicol and its glucuronide has been evaluated by use of a microdialysis probe linked to automatic on-line microbore high-performance liquid chromatography. The microdialysis probe was inserted into the bile duct between the liver and the duodenum; to avoid obstruction of the bile duct or bile salt waste, a shunt linear probe was used. After intravenous administration of chloramphenicol succinate (100 mg kg(-1)) the amounts of unbound chloramphenicol and its glucuronide in the bile microdialysate were recorded. According to the pharmacokinetic results disposition of chloramphenicol seems to fit a two-compartment model whereas that of chloramphenicol glucuronide fits a one-compartment model in rat bile. The area under the concentration-time curve for chloramphenicol glucuronide was twice that for chloramphenicol in rat bile duct. Clearance of chloramphenicol glucuronide was significantly higher than that of chloramphenicol in biliary excretion, indicating that chloramphenicol and its glucuronide are actively excreted into the bile.
通过使用与自动在线微径高效液相色谱相连的微透析探针，对氯霉素及其葡糖醛酸苷的胆汁排泄进行了评估。将微透析探针插入肝脏与十二指肠之间的胆管中；为避免胆管阻塞或胆盐浪费，使用了分流线性探针。静脉注射琥珀氯霉素（100 mg kg⁻¹）后，记录胆汁微透析液中游离氯霉素及其葡糖醛酸苷的量。根据药代动力学结果，氯霉素在大鼠胆汁中的处置似乎符合二室模型，而氯霉素葡糖醛酸苷符合一室模型。大鼠胆管中氯霉素葡糖醛酸苷的浓度-时间曲线下面积是氯霉素的两倍。在胆汁排泄中，氯霉素葡糖醛酸苷的清除率显著高于氯霉素，表明氯霉素及其葡糖醛酸苷被主动排泄到胆汁中。
