O'Brien J E, Abbey V, Hinsvark O, Perel J, Finster M
J Pharm Sci. 1979 Jan;68(1):75-8. doi: 10.1002/jps.2600680123.
Blood levels of intact chloroprocaine were determined using a GLC procedure capable of detecting as little as 10 ng of chloroprocaine/ml of blood. It was necessary to detective plasma cholinesterases in collected samples by adding echothiophate iodide to blood sampling tubes. An extraction procedure, followed by a TLC separation and spectrodensitometric assay, was developed for measurement of the metabolite 2-chloro-4-aminobenzoic acid in plasma and urine. With these procedures, data were obtained showing that chloroprocaine is hydrolyzed rapidly by plasma cholinesterases. No unchanged drug could be detected in any blood samples obtained from volunteers who received chloroprocaine by intravenous infusion or from obstetric patients who had epidural anesthesia during labor and delivery. Blood levels of 2-chloro-4-amino-benzoic acid rose promptly with the administration of chloroprocaine and declined rapidly after drug administration. Most of the metabolite was recovered in urine.
使用一种气相色谱法(GLC)来测定血液中完整的氯普鲁卡因水平,该方法能够检测低至每毫升血液10纳克的氯普鲁卡因。有必要通过向血样采集管中添加碘依可酯来检测采集样本中的血浆胆碱酯酶。开发了一种提取程序,随后进行薄层色谱(TLC)分离和光密度测定法,用于测量血浆和尿液中的代谢物2 - 氯 - 4 - 氨基苯甲酸。通过这些程序获得的数据表明,氯普鲁卡因被血浆胆碱酯酶迅速水解。在接受静脉输注氯普鲁卡因的志愿者或在分娩期间接受硬膜外麻醉的产科患者采集的任何血样中,均未检测到未变化的药物。2 - 氯 - 4 - 氨基苯甲酸的血药浓度在给予氯普鲁卡因后迅速上升,并在给药后迅速下降。大部分代谢物在尿液中回收。