School of Pharmaceutical Sciences, Wenzhou Medical College, Wenzhou, China.
Planta Med. 2013 Sep;79(14):1324-8. doi: 10.1055/s-0033-1350675. Epub 2013 Aug 7.
Panaxadiol is a novel antitumor agent extracted from the Chinese medical herb Panax ginseng. This agent is being developed for the treatment of tumor diseases. A rapid, selective, and simple method based on ultrafast liquid chromatography-tandem mass spectrometry was established and validated to determine panaxadiol in rat plasma following oral and sublingual intravenous administration of panaxadiol. The plasma samples were pretreated with acetic ether, and chromatographic separation was achieved on a Shim-pack XR-ODS III column using isocratic elution with the mobile phase of 0.1 % formic acid and acetonitrile. Analytes and protopanaxadiol (internal standard) were analyzed and identified using electrospray positive ionization mass spectrometry in the multiple reaction-monitoring mode. The MS/MS detection was carried out by monitoring the fragmentation of m/z 461.45 → m/z 127.1 for panaxadiol and m/z 425.4 → m/z 95.1 for protopanaxadiol (internal standard) on a triple-quadrupole mass spectrometer. The result showed good linearity over a wide concentration range (0.1-20 ng/mL) (R2 > 0.999) and its lower limit of detection and quantification were 0.03 and 0.1 ng/mL, respectively. The intra- and interday precision (RSD %) was within 15 % and the accuracy ranged from 94.9 % to 112.0 %. The absolute bioavailability was 12.5 %. The method was fully validated and successfully applied to the pharmacokinetic study of a single dose of panaxadiol.
人参二醇是一种从中药人参中提取的新型抗肿瘤药物。该药物正在开发用于治疗肿瘤疾病。建立并验证了一种基于超快速液相色谱-串联质谱的快速、选择性和简单的方法,用于检测口服和舌下静脉给予人参二醇后大鼠血浆中的人参二醇。用乙酸乙酯预处理血浆样品,采用等度洗脱,以 0.1%甲酸和乙腈为流动相,在 Shim-pack XR-ODS III 柱上进行色谱分离。采用电喷雾正离子化质谱,在多反应监测模式下对分析物和原人参二醇(内标)进行分析和鉴定。三重四极杆质谱仪上对 m/z 461.45→m/z 127.1(人参二醇)和 m/z 425.4→m/z 95.1(内标原人参二醇)进行 MS/MS 检测。结果表明,该方法在较宽的浓度范围内(0.1-20 ng/mL)具有良好的线性关系(R2>0.999),其检测限和定量限分别为 0.03 和 0.1 ng/mL。日内和日间精密度(RSD%)均在 15%以内,准确度范围为 94.9%-112.0%。绝对生物利用度为 12.5%。该方法经过充分验证,并成功应用于单次给予人参二醇的药代动力学研究。