采用 HPLC-MS/MS 同时测定大鼠体内 tadehaginoside 及其主要代谢物，并将其应用于药代动力学和组织分布研究。
Simultaneous measurement of tadehaginoside and its principal metabolite in rats by HPLC-MS/MS and its application in pharmacokinetics and tissue distribution study.
机构信息
Key Laboratory of Tropical Translational Medicine of Ministry of Education, Hainan Key Laboratory for Research and Development of Tropical Herbs, School of Pharmacy, Hainan Medical University, Haikou, P. R. China.
Pharmaceutical College, Guangxi Medical University, Nanning, China.
出版信息
Pharm Biol. 2021 Dec;59(1):1415-1424. doi: 10.1080/13880209.2021.1990354.
CONTEXT
Tadehaginoside, an active ingredient isolated from (Linn.) Ohashi (Leguminosae), exhibited various biological activities. However, the pharmacokinetics and tissue distribution which affect tadehaginoside's therapeutic actions and application remain elusive.
OBJECTIVE
To clarify the metabolism of tadehaginoside .
MATERIALS AND METHODS
The pharmacokinetics and tissue distribution of tadehaginoside and its metabolite -hydroxycinnamic acid (HYD) were investigated using LC-MS/MS. Pharmacokinetic parameters were determined in 10 Sprague-Dawley rats divided into two groups, the intravenous group (5 mg/kg) and the oral group (25 mg/kg). For the tissue-distribution study, 20 rats were intravenously given tadehaginoside (5 mg/kg) before the experiment ( = 4). Biological samples were collected before drug administration (control group) and after drug administration.
RESULTS
The linearity, accuracy, precision, stability, recovery and matrix effect of the method were well-validated and the results satisfied the requirements of biological sample measurement. Treatment with tadehaginoside intragastric and intravenous administration, the calculated in rats was 6.01 ± 2.14 ng/mL and 109.77 ± 4.29 ng/mL, and was 0.025 ± 0.08 h and 0.08 h, respectively. The results indicated that the quick absorption of tadehaginoside was observed following intravenous administration, and tadehaginoside in plasma of rats with intragastric administration showed relatively low concentration may be due to the formation of its metabolite. Tissue-distribution study indicated that kidney and spleen were the major distribution organs for tadehaginoside in rats and there was no long-term accumulation in most tissues.
DISCUSSION AND CONCLUSION
These results could provide clues for exploring the bioactivity of tadehaginoside based on its pharmacokinetic characteristics.
背景
从 （Linn.）Ohashi（豆科）中分离得到的活性成分桃叶珊瑚苷，表现出多种生物活性。然而，影响桃叶珊瑚苷治疗作用和应用的药代动力学和组织分布仍不清楚。
目的
阐明桃叶珊瑚苷的代谢情况。
材料和方法
采用 LC-MS/MS 法研究桃叶珊瑚苷及其代谢产物 -羟基肉桂酸（HYD）的药代动力学和组织分布。将 10 只 Sprague-Dawley 大鼠分为两组，静脉组（5mg/kg）和口服组（25mg/kg），进行药代动力学参数测定。在实验前（n=4），20 只大鼠静脉给予桃叶珊瑚苷（5mg/kg）进行组织分布研究。采集给药前（对照组）和给药后的生物样本。
结果
该方法的线性、准确性、精密度、稳定性、回收率和基质效应均得到了良好的验证，结果符合生物样品测定的要求。桃叶珊瑚苷灌胃和静脉给药后，大鼠的计算 AUC0-t 分别为 6.01±2.14ng/mL 和 109.77±4.29ng/mL，CL 分别为 0.025±0.08h 和 0.08h，表明静脉给药后桃叶珊瑚苷吸收迅速，灌胃给药后大鼠血浆中桃叶珊瑚苷浓度相对较低，可能是由于其代谢产物的形成。组织分布研究表明，肾脏和脾脏是桃叶珊瑚苷在大鼠体内的主要分布器官，大多数组织中没有长期蓄积。
讨论与结论
这些结果可为基于药代动力学特征探索桃叶珊瑚苷的生物活性提供线索。
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