Department of Pharmacy, Inner Mongolia Medical University, Hohhot, P. R. China.
State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing, P. R. China.
J Sep Sci. 2020 Sep;43(18):3702-3713. doi: 10.1002/jssc.202000355. Epub 2020 Aug 19.
Tabson-2 decoction is the traditional Mongolian formula for anti-osteoporosis, and the ambiguous of active ingredient is an important factor in restricting its modernization and globalization. Although pharmacokinetic profiles research is a viable approach to find the components being responsible for formula efficacy, the pharmacokinetics study of Tabson-2 decoction has not been elucidated yet. Owing to the existence of isomers, low bioavailability of some small molecule and interference of endogenous, the pharmacokinetics study of Tabson-2 decoction are more difficult than that of chemical drugs. In our experiment, a specific and sensitive liquid chromatography-tandem mass spectrometry method was developed and validated for simultaneous determination of 16 active ingredients in Tabson-2 decoction, which could fulfill the requirements of multi-compounds pharmacokinetic study of Tabson-2 decoction. Additionally, the ingredients with significant distributions in rats were gentianic acid, chlorogenic acid, and aucubin, which could be the main potential active components in Tabson-2 decoction. The components with a significant bioavailability difference between normal and d-galactose induced osteoporosis rats were achieved as well. These data offer useful information for screening the active ingredients in Tabson-2 decoction, and assessing the bioavailability of these active ingredients in different physiological status, which might provide a possible mechanism of anti-osteoporosis efficacy of Tabson-2 decoction.
荜茇宁-2 汤是一种传统的蒙古族抗骨质疏松症配方,其活性成分的不明确性是限制其现代化和全球化的重要因素。虽然药代动力学研究是寻找负责配方功效的成分的可行方法,但荜茇宁-2 汤的药代动力学研究尚未阐明。由于存在异构体、一些小分子的低生物利用度以及内源性物质的干扰,荜茇宁-2 汤的药代动力学研究比化学药物更为困难。在我们的实验中,开发并验证了一种特定且灵敏的液相色谱-串联质谱法,用于同时测定荜茇宁-2 汤中的 16 种活性成分,该方法能够满足荜茇宁-2 汤多化合物药代动力学研究的要求。此外,在大鼠体内分布广泛的成分是龙胆酸、绿原酸和梓醇,它们可能是荜茇宁-2 汤中的主要潜在活性成分。还获得了正常和半乳糖诱导的骨质疏松症大鼠之间生物利用度差异显著的成分。这些数据为筛选荜茇宁-2 汤中的活性成分以及评估这些活性成分在不同生理状态下的生物利用度提供了有用的信息,这可能为荜茇宁-2 汤的抗骨质疏松症功效提供了一种可能的机制。