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超高效液相色谱-串联质谱法研究补骨脂酚在大鼠体内的药代动力学

Ultra-high-performance liquid chromatography-tandem mass spectrometry for pharmacokinetics of bakuchiol in rats.

作者信息

Zhang Shuang-Qing, Fan Yu-Ming

机构信息

Department of Nutrition and Metabolism, National Institute for Nutrition and Food Safety, China Center for Disease Control and Prevention, Beijing, 100050, China.

出版信息

Biomed Chromatogr. 2014 Mar;28(3):433-8. doi: 10.1002/bmc.3051. Epub 2013 Sep 23.

Abstract

Psoralea Corylifolia L. is a traditional Chinese medicine with many beneficial effects in medical therapies. Bakuchiol was the main active ingredient of Psoralea Corylifolia L., used for the treatment of various diseases and also as a natural food additive. A specific and reliable ultra-high performance liquid chromatography-tandem mass spectrometry has been developed and fully validated for the quantification of bakuchiol in rat plasma. Chromatographic separation of bakuchiol and an internal standard, daidzein, was achieved on a Hypersil Gold C18 column with gradient elution that consisted of methanol and water at a flow rate of 0.2 mL/min. The compounds were detected at negative ionization mode using mass transition m/z 255.2 → 172.0 and 252.9 → 132.0 for bakuchiol and daidzein, respectively. Good linearity was obtained over the range of 2-1000 ng/mL and the lower limit of quantification was 2 ng/mL. The intra- and inter-day accuracies ranged from 91.1 to 105.7% and precisions (relative standard deviations) were within 9.3%. Bakuchiol was found to be stable under three freeze-thaw cycles, short-term temperature, post-preparative and long-term temperature conditions. The method was applied to a pharmacokinetic study of bakuchiol intravenously administered to rats at a dose of 5 mg/kg.

摘要

补骨脂是一种在医学治疗中有多种有益作用的传统中药。补骨脂酚是补骨脂的主要活性成分,用于治疗各种疾病,也用作天然食品添加剂。已开发出一种特定且可靠的超高效液相色谱 - 串联质谱法,并对其在大鼠血浆中补骨脂酚的定量进行了全面验证。补骨脂酚和内标染料木黄酮在Hypersil Gold C18柱上进行色谱分离,采用甲醇和水的梯度洗脱,流速为0.2 mL/min。在负离子模式下检测化合物,补骨脂酚和染料木黄酮的质荷比分别为m/z 255.2 → 172.0和252.9 → 132.0。在2 - 1000 ng/mL范围内获得了良好的线性关系,定量下限为2 ng/mL。日内和日间准确度范围为91.1%至105.7%,精密度(相对标准偏差)在9.3%以内。发现补骨脂酚在三个冻融循环、短期温度、制备后和长期温度条件下均稳定。该方法应用于以5 mg/kg剂量静脉注射给大鼠的补骨脂酚的药代动力学研究。

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