Abstract：
Areca nuts have been used as a traditional Chinese medicine (TCM) for thousands of years. Recent studies have shown that it exhibits good pharmacological activity and toxicity. In this study, the pharmacokinetics of five major components of areca nut extract in rats were investigated using a highly sensitive ultra-performance liquid chromatography coupled with triple quadrupole mass spectrometry (UPLC-MS/MS) method. Arecoline, arecaidine, guvacoline, guvacine, and catechin were separated and quantified accurately using gradient elution with mobile phases of (A) water containing 0.1 % formic acid-10 mM ammonium formate, and (B) methanol. The constituents were detected under a timing switch between the positive and negative ion modes using multiple reaction monitoring (MRM). Each calibration curve had a high R2 value of >0.99. The method accuracies ranged -7.09-11.05 % and precision values were less than 14.36 %. The recovery, matrix effect, selectivity, stability, and carry-over of the method were in accordance with the relevant requirements. It was successfully applied for the investigation of the pharmacokinetics of these five constituents after oral administration of areca nut extract. Pharmacokinetic results indirectly indicated a metabolic relationship between the four areca nut alkaloids in rats. For further clarification of its pharmacodynamic basis, this study provided a theoretical reference.
摘要：
槟榔被用作传统中药（TCM）已有数千年的历史。最近的研究表明，它具有良好的药理活性和毒性。在这项研究中,采用高灵敏度超高效液相色谱-三重四极杆质谱(UPLC-MS/MS)方法研究了槟榔提取物中5种主要成分在大鼠体内的药代动力学。槟榔林,Arecaidine,givacoline,Givacine,和儿茶素进行分离和精确定量，使用梯度洗脱，流动相（A）含有0.1％甲酸-10mM甲酸铵的水，和(B)甲醇。使用多反应监测(MRM)在正负离子模式之间的定时切换下检测成分。每个校准曲线具有>0.99的高R2值。方法准确度范围为-7.09-11.05％，精密度值小于14.36％。复苏,基体效应，选择性,稳定性,和结转的方法均符合相关要求。它已成功用于口服槟榔提取物后这五个成分的药代动力学研究。药代动力学结果间接表明了四种槟榔生物碱在大鼠体内的代谢关系。为了进一步阐明其药效学基础，本研究提供了理论参考。
