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采用超高效液相色谱/质谱联用方法研究人参果提取物及纯人参皂苷 Re 中人参皂苷 Re 在小鼠体内的药代动力学。

Pharmacokinetic study of ginsenoside Re with pure ginsenoside Re and ginseng berry extracts in mouse using ultra performance liquid chromatography/mass spectrometric method.

机构信息

AMOREPACIFIC CO/R&D Center, Gyeonggi-do, South Korea.

出版信息

J Pharm Biomed Anal. 2010 Jan 5;51(1):278-83. doi: 10.1016/j.jpba.2009.08.013. Epub 2009 Aug 18.

Abstract

Ginsenoside Re is the major ginsenoside in ginseng berry(GB) extract and its pharmacokinetics were studied following the intravenous and oral administration of pure Re or ginseng berry extract in mouse with doses of 10 and 50 mg/kg using ultra performance liquid chromatography mass spectrometric (UPLC/MS) method which can simultaneously determine ginsenoside Re, Rg1 and Rh1 in mouse serum. The serum samples were pretreated by protein precipitation and chromatographic separation was performed on AQUITY UPLC BEH C(18) column using gradient elution with the mobile phase of 5 mM ammonium formate and acetonitrile. Analytes and digoxin (I.S.) were analyzed and identified using an electrospray negative ionization mass spectrometry in the selected ion monitoring mode with the linear concentration range of 5.0-5000 ng/mL and lower limits of detection (LLOD) under 2.5 ng/mL. Ginsenoside Re was rapidly cleared from the body with a short half-life (0.2+/-0.03 h for male and 0.5+/-0.08 h for female mice after i.v.) and oral absorption was generally poor (F% 0.19-0.28). Notably, GB extract showed a superior oral absorption of ginsenoside Re (F% 0.33-0.75) at equivalent ginsenoside Re dose to pure ginsenoside Re, indicating that GB extract might be a good form for ginsenoside Re intake.

摘要

人参果提取物中的主要人参皂苷为人参皂苷 Re,本研究采用超高效液相色谱-串联质谱(UPLC/MS)法,以 10 和 50mg/kg 剂量静脉和口服给予纯 Re 或人参果提取物,研究了 Re 的药代动力学。该方法可以同时测定小鼠血清中的人参皂苷 Re、Rg1 和 Rh1。血清样品经蛋白沉淀预处理,采用 AQUITY UPLC BEH C18 柱,以 5mM 甲酸铵和乙腈为流动相进行梯度洗脱。采用电喷雾负离子质谱(ESI-MS),在选择离子监测模式下进行分析和鉴定,线性浓度范围为 5.0-5000ng/ml,检测限(LLOD)低于 2.5ng/ml。静脉注射后,Re 在体内迅速清除,半衰期较短(雄性小鼠为 0.2+/-0.03h,雌性小鼠为 0.5+/-0.08h),口服吸收一般较差(F%为 0.19-0.28)。值得注意的是,人参果提取物在相当于纯 Re 剂量的情况下,显示出较高的 Re 口服吸收(F%为 0.33-0.75),表明人参果提取物可能是 Re 摄入的一种良好形式。

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