中药中香豆素、栀子苷和大黄酸的临床前药代动力学研究：一种经验证的 LC-MS/MS 方法。
Preclinical Pharmacokinetics of Scoparone, Geniposide and Rhein in an Herbal Medicine Using a Validated LC-MS/MS Method.
机构信息
Institute of Traditional Medicine, School of Medicine, National Yang-Ming University, Taipei 11221, Taiwan.
Department of Chinese Medicine, Kaohsiung Chang Gung Memorial Hospital and Chang Gung University College of Medicine, Kaohsiung 83301, Taiwan.
出版信息
Molecules. 2018 Oct 22;23(10):2716. doi: 10.3390/molecules23102716.
The herbal formula Yin-Chen-Hao-Tang has been reported to have anti-fibrosis properties. The aim of this study was to reveal the pharmacokinetic characteristics of bioactive compounds in this herbal formula. A new high-performance liquid chromatography-tandem mass spectrometry method was developed and validated for simultaneous determination of scoparone, geniposide and rhein in rat plasma. A pharmaceutical herbal powder was administered to rats at doses of 1 g/kg and 3 g/kg orally. The method showed excellent linearity (r² > 0.999) and validation was successfully conducted for the pharmacokinetic study. The results show that the C values and areas under the curve of scoparone, geniposide and rhein were higher and not proportional to the dose in rat plasma, while the T and half-life values were consistent in the group that received 1 g/kg. The clearance of the higher dose (3 g/kg) did not decrease proportionally to that of the low dose. The results showed the nonlinear pharmacokinetic properties of scoparone, geniposide and rhein in Yin-Chen-Hao-Tang that suggested possible accumulation of bioactive compounds through oral administration. This pharmacokinetic study reveals that an increased dose of this herbal formula would largely increase the maximum concentration and bioavailability of scoparone, geniposide and rhein.
茵陈蒿汤的草药配方据称具有抗纤维化特性。本研究旨在揭示该草药配方中生物活性化合物的药代动力学特征。建立并验证了一种新的高效液相色谱-串联质谱法，用于同时测定大鼠血浆中的桉油精、栀子苷和大黄酸。以 1 g/kg 和 3 g/kg 的剂量给大鼠口服给予药草粉末。该方法显示出优异的线性（r²>0.999），并且成功进行了药代动力学研究的验证。结果表明，在大鼠血浆中，桉油精、栀子苷和大黄酸的 C 值和曲线下面积与剂量不成比例地升高，而接受 1 g/kg 剂量的组中的 T 和半衰期值是一致的。高剂量（3 g/kg）的清除率并没有与低剂量成比例地降低。结果表明，茵陈蒿汤中桉油精、栀子苷和大黄酸具有非线性药代动力学特性，提示通过口服给药可能会积累生物活性化合物。这项药代动力学研究表明，增加该草药配方的剂量会大大增加桉油精、栀子苷和大黄酸的最大浓度和生物利用度。
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