Background: Paederia scandens (Lour.) Merrill, belonging to the Rubiaceae family, was one of the Traditional Chinese Medicines that has been generally used to treat aches and pains, inflammation, bacillary dysentery, piles and rheumatic arthritis. The four iridoid glycosides that Paederosidic acid, Paederoside, Paederosidic acid methyl ester, and Asperuloside from Paederia scandens are considered to be the main bioactive constituents. However, their pharmacokinetics and action mechanisms of these iridoid glycosides still remain unknown. In this study, a method of simultaneous determination of four iridoid glycosides components in rat plasma with LC-MS/MS has been established and successfully applied to a pharmacokinetic study in rats, which would be favourable for further exploration.

Methods: In this study, a sensitive, rapid, accurate bioanalytical method of simultaneous determination of four iridoid glycosides components from Paederia scandens extract in rat plasma with LCMS/ MS has been established. It is easy and rapid for LC-MS/MS to accurately separate and simultaneously quantify the analytes because of its high sensitivity, selectivity and accuracy. This validated method was successfully applied to a pharmacokinetic study in rats with intravenous and oral administrations of Paederia scandens extract.

Results: The resulting data are fully satisfied for the selectivity and the sensitivity. Their lower limit of quantitation are in 0.25-0.5 ng/mL. Intra- and interday precisions were less than 15.0% with accuracy in the range of -15.0% to 15.0%. In the stability measurements including repeated Freeze-thaw, 4 hours at 4°C, 24 hours at 4°C, and 30 days at -80°C, the variations between the measurements and the nominated values of these compounds in plasma were detected to be less than 15.0%. The extraction recoveries of the compounds were from 85.4% to 105.6%. The bioavailability (F) of the four iridoid glycosides were 1.74% to 3.36%.

Conclusion: In summary, a simple, rapid, precise, and sensitive LC-MS/MS method has been established and validated to determine the four iridoid glycosides from Paederia scandens extract in rat plasma, which was successfully applied to pharmacokinetic study in rats. The information obtained from the study will facilitate further exploration on Paederosidic acid, Paederoside, Paederosidic acid methyl ester as well as Asperuloside and these may provide valuable pharmacokinetic reference for human applications.

背景：茜草（Padereria scandens，Lour。）美林属于茜草科，是中药之一，通常被用来治疗疼痛和疼痛，发炎，细菌性痢疾，痔疮和风湿性关节炎。Paederia scandens的Paederosidic酸，Paederoside，Paederosidic酸甲酯和Asperuloside被认为是主要的生物活性成分。但是，这些环烯醚酮苷的药代动力学和作用机理仍然未知。在这项研究中，建立了一种同时测定LC-MS / MS法测定大鼠血浆中四种鸢尾糖苷成分的方法，并将其成功地应用于大鼠的药代动力学研究，这将有利于进一步的研究。

方法：本研究建立了一种灵敏，快速，准确的生物分析方法，该方法可通过LCMS / MS同时测定大鼠血浆中scan药提取物中的四种鸢尾苷成分。由于LC-MS / MS具有高灵敏度，选择性和准确性，因此可以轻松，快速地准确分离并同时定量分析物。这种经过验证的方法已成功地应用于大鼠静脉内和口服scan药提取物的药代动力学研究。

结果：所得数据完全满足选择性和灵敏度的要求。它们的定量下限为0.25-0.5 ng / mL。日内和日间精度低于15.0％，精度范围为-15.0％至15.0％。在包括反复冻融，在4°C下4小时，在4°C下24小时以及在-80°C下30天的稳定性测量中，检测到这些化合物在血浆中的测量值和指定值之间的差异，小于15.0％。化合物的提取回收率为85.4％至105.6％。四种鸢尾苷的生物利用度（F）为1.74％至3.36％。

结论：总之，已建立了一种简单，快速，准确，灵敏的LC-MS / MS方法，并已成功测定了大鼠血浆scan药提取物中的四种鸢尾苷，已成功应用于大鼠药代动力学研究。从研究中获得的信息将有助于进一步研究Paederosidic acid，Paederoside，Paederosidic acid甲酯以及Asperuloside，这些可能为人类应用提供有价值的药代动力学参考。