Pharmacokinetic characterization of oxymatrine and matrine in rats after oral administration of radix Sophorae tonkinensis extract and oxymatrine by sensitive and robust UPLC-MS/MS method
Pharmacokinetic characterization of oxymatrine and matrine in rats after oral administration of radix Sophorae tonkinensis extract and oxymatrine by sensitive and robust UPLC-MS/MS method
复制标题
采用灵敏、稳健的 UPLC-MS/MS 方法表征大鼠口服山豆根提取物和氧化苦参碱后氧化苦参碱和苦参碱的药代动力学
DOI：
10.1016/j.jpba.2013.05.003
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发表时间：
2013-09-01
影响因子：
3.4
通讯作者：
Liu, Zhong-Qiu
中科院分区：
文献类型：
--
作者：
Tang, Lan;Dong, Ling-Na;Liu, Zhong-Qiu
The purpose of this study is to systematically investigate the pharmacokinetic (PR) behaviors of radix Sophorae tonkinensis (S. tonkinensis) using oxymatrine (OMT) and matrine (MT) as the target markers (2 mg/kg OMT and 1.3 mg/kg MT, oral administration). The PM characteristics in radix S. tonkinensis extracts were also compared with those of pure OMT. A fast ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method was developed. OMT absorption was very fast, and no significant differences were observed (p > 0.05) in t(max), CL, and t(1/2) for both pure OMT and extracts. C-max and AUC(0 ->infinity) of pure OMT were significantly higher than those of S. tonkinensis extracts (C-max, 61.64 +/- 6.65 vs. 43.24 +/- 10.14 ng/mL; AUC, 9894.48 +/- 2234.99 vs. 4730.30 +/- 3503.8 min ng/mL) (p < 0.05). However, the absolute OMT bioavailability of pure OMT was higher than that of the compound in radix S. tonkinensis extracts (6.79 +/- 2.52% vs. 1.87 +/- 2.66%). By contrast, the bioavailability of total alkaloids (OMT + MT) after pure OMT administration was 81.14 +/- 8.83%, similar to that of radix S. tonkinensis extracts (69.36 +/- 17.37%) (p > 0.05). It was presumed that OMT absorption has no effect on the bioavailability of the two alkaloids. Other constituents in radix S. tonkinensis extracts can influence the transformation of OMT to MT, which directly leads to variations in the PK behavior of OMT. In addition, the protein binding of OMT and MT in plasma was very low (4.80%-8.95% for OMT, 5.10-10.55% for MT). In conclusion, OMT in radix S. tonkinensis extracts exhibits different PK behaviors with pure OMT through the transformation of OMT to MT due to other complex ingredients. (C) 2013 Published by Elsevier B.V.
