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HPLC–MS/MS method for bioavailability study of bruceines D & E in rat plasma
Journal of Chromatography B ( IF 3 ) Pub Date : 2017-08-30 , DOI: 10.1016/j.jchromb.2017.08.037
Farahdina Man , Chee-Yan Choo

Bruceines D and E are quassinoids from seeds of Brucea javanica (L.) Merr. exhibiting hypoglycemia effect. The crude drug is used as a traditional medicine by diabetes patients. The aim of this study is to understand the bioavailability and pharmacokinetics of both the bruceines D & E. A rapid and sensitive HPLC–MS/MS method was developed and validated for the quantification of both quassinoids, bruceines D & E in rat plasma. Both the bruceines D & E were separated with the Zorbax SBC-18 column with gradient elution and mobile phase system of acetonitrile and deionized water with 0.1% formic acid at a flow rate of 0.5 mL/min. Analytes were detected in multiple reaction monitoring (MRM) mode with electrospray positive ionization. The quassinoids, namely bruceines D & E were detected with transitions of m/z 411.2 → 393.2 and m/z 395.2 → 377.2, respectively. Another quassinoid, eurycomanone was used as the internal standard with transition of m/z 409.2 → 391.2. The method was validated and conformed to the regulatory requirements. The validated method was applied to pharmacokinetic and bioavailability studies in rats. The pharmacokinetic study indicated both bruceine D and E were rapidly absorbed into the circulation system and reached its peak concentration at 0.54 ± 0.34 h and 0.66 ± 0.30 h, respectively. Bruceine E was eliminated slower than Bruceine D with t1/2 value almost increased two-fold compared to Bruceine D. In conclusion, a rapid, selective and sensitive HPLC–MS/MS method was developed for the simultaneous determination of both the bruceines D and E in rat plasma. Both bruceines D and E displayed poor oral bioavailability.



中文翻译:

HPLC-MS / MS法测定芥子碱D和E在大鼠血浆中的生物利用度

Bruceines D和E是来自Brucea javanica(L.)Merr种子的quassinoids 。表现出低血糖作用。粗药物被糖尿病患者用作传统药物。这项研究的目的是了解两种水杨酸D和E的生物利用度和药代动力学。建立了一种快速灵敏的HPLC-MS / MS方法,并验证了大鼠血浆中的两种类胡萝卜素,水杨酸D和E的定量。用Zorbax SBC-18色谱柱通过梯度洗脱和乙腈和含0.1%甲酸的去离子水流动相系统,以0.5 mL / min的流速分离水苏氨酸D和E。在多反应监测(MRM)模式下使用电喷雾正电离检测分析物。quassinoids,即brusines D&m / z 411.2→393.2和m / z 395.2→377.2。另一类拟似苦瓜类神经叶酮作为内标,其m / z 409.2→391.2转变。该方法已经过验证并符合法规要求。经验证的方法已应用于大鼠的药代动力学和生物利用度研究。药代动力学研究表明,杜鹃花碱D和E均迅速吸收到循环系统中,并分别在0.54±0.34 h和0.66±0.30 h达到峰值浓度。丁二烯E的消除速度比丁二烯D慢,t为1/2相较于Bruceine D,该值几乎增加了两倍。总之,开发了一种快速,选择性和灵敏的HPLC-MS / MS方法,用于同时测定大鼠血浆中的Bruceine D和E。浅色丁香D和E均显示不良的口服生物利用度。

更新日期:2017-08-30
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