Jeong Soo Hee, Newcombe David, Sheridan Janie, Tingle Malcolm
University of Auckland, Pharmacology & Clinical Pharmacology, Auckland, New Zealand.
University of Auckland, School of Population Health, Auckland, New Zealand.
Drug Test Anal. 2015 Jun;7(6):475-82. doi: 10.1002/dta.1707. Epub 2014 Sep 17.
Cytisine, an α4 β2 nicotinic receptor partial agonist, is a plant alkaloid that is commercially extracted for use as a smoking cessation medication. Despite its long history of use, there is very little understanding of the pharmacokinetics of cytisine. To date, no previous studies have reported cytisine concentrations in humans following its use as a smoking cessation agent. A high performance liquid chromatography-ultraviolet (HPLC-UV) method was developed and validated for analysis of Tabex® and nicotine-free oral strips, two commercial products containing cytisine. A sensitive liquid chromatography-mass spectrometry (LC-MS) method was developed and validated for the quantification of cytisine in human plasma and for the detection of cytisine in urine. Single-dose pharmacokinetics of cytisine was studied in healthy smokers. Subjects received a single 3 mg oral dose administration of cytisine. Cytisine was detected in all plasma samples collected after administration, including 15 min post-dose and at 24 h. Cytisine was renally excreted and detected as an unchanged drug. No metabolites were detected in plasma or urine collected in the study. No adverse reactions were reported.
金雀花碱是一种α4β2烟碱受体部分激动剂，是一种从植物中提取的生物碱，可作为戒烟药物进行商业提取。尽管其使用历史悠久，但对金雀花碱的药代动力学了解甚少。迄今为止，尚无先前的研究报告金雀花碱作为戒烟药物使用后在人体中的浓度。开发并验证了一种高效液相色谱-紫外（HPLC-UV）方法，用于分析含有金雀花碱的两种商业产品Tabex®和无尼古丁口腔贴片。开发并验证了一种灵敏的液相色谱-质谱（LC-MS）方法，用于定量人血浆中的金雀花碱以及检测尿液中的金雀花碱。在健康吸烟者中研究了金雀花碱的单剂量药代动力学。受试者接受了单次3mg口服剂量的金雀花碱给药。给药后采集的所有血浆样本中均检测到金雀花碱，包括给药后15分钟和24小时的样本。金雀花碱经肾脏排泄，以原形药物形式被检测到。在该研究采集的血浆或尿液中未检测到代谢物。未报告不良反应。
