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Pharmacokinetics of 10-Hydroxy Mesaconitine in Rat Plasma by Ultra-Performance Liquid Chromatography-Tandem Quadrupole Mass Spectrometry

机译:超级性液相色谱 - 串联 - 串联曲调质谱法在大鼠等离子体中的10-羟基己酮的药代动力学

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摘要

Mesaconitine is the predominant active ingredient in Aconitum carmichaelii Debx. The compound 10-hydroxy mesaconitine is one known metabolite of mesaconitine and is toxic. In order to better understand its pharmacokinetics, UPLC-MS/MS was used in this paper to measure the concentration of 10-hydroxy mesaconitine in the plasma of rats after oral (5?mg/kg) and intravenous (0.1?mg/kg) administration of 10-hydroxy mesaconitine. The concentrations of 10-hydroxy mesaconitine in rat plasma measured in the standard curve covered the range of 0.3–60?ng/mL. The intraday and interday precisions of the samples of 10-hydroxy mesaconitine in rat plasma were lower than 15%. In addition, the accuracies ranged between 96.0% and 109.3%, the matrix effects ranged between 88.9% and 98.1%, and the recoveries were all higher than 79.1%. The AUC_((0??? t )) values were 23.6?±?5.9 and 207.6?±?72.9?ng/mL·h for intravenous and oral administration, respectively, and the bioavailability of 10-hydroxy mesaconitine was 17.6%. Lastly, t _(1/2) was 1.3?±?0.6?h and 3.1?±?0.4?h for intravenous and oral administration, respectively.
机译:中皂肽是Aconitum Carmichaelii Debx中的主要活性成分。化合物10-羟基溴代酮苷是一种已知的中丙酮的代谢物,并且是有毒的。为了更好地了解其药代动力学,本文使用UPLC-MS / MS测量口腔(5〜Mg / kg)和静脉内(0.1Ω·mg / kg)的大鼠等血浆中10-羟基己酮的浓度给予10-羟基皂苷碱。在标准曲线中测量的大鼠等离子体中的10-羟基己酸的浓度覆盖在0.3-60Ω·Ng / ml的范围内。大鼠血浆10-羟基己酰样品的盘中和间三精确度低于15%。此外,准确度范围为96.0%和109.3%,基质效应范围为88.9%和98.1%,回收率均高于79.1%。 AUC _((0'Ono-t))值分别为23.6?±5.9和207.6?±72.9?Ng / ml·h,分别用于静脉内和口服给药,10-羟基酸酮的生物利用度为17.6%。最后,T _(1/2)分别为1.3?±0.6Ω,分别为静脉内和口服给药0.6°H和3.1?±0.4℃。

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