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.

中文翻译：

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超高效液相色谱-串联四极杆质谱法研究 10-羟基新乌头碱在大鼠血浆中的药代动力学


新乌头碱是Aconitum carmichaelii Debx 中的主要活性成分。化合物10-羟基新乌头碱是新乌头碱的一种已知代谢物，具有毒性。为了更好地了解其药代动力学，本文采用UPLC-MS/MS法测定了大鼠口服（5 mg/kg）和静脉（0.1 mg/kg）给药后血浆中10-羟基新乌头碱的浓度。 10-羟基新乌头碱。标准曲线中测得的大鼠血浆中10-羟基新乌头碱的浓度范围为0.3-60 ng/mL。大鼠血浆中10-羟基新乌头碱样品的日内和日间精密度均低于15%。此外，准确度在96.0%~109.3%之间，基质效应在88.9%~98.1%之间，加标回收率均高于79.1%。静脉注射和口服给药的AUC _{（0− t ）}值分别为23.6±5.9和207.6±72.9ng/mL·h，10-羟基新乌头碱的生物利用度为17.6%。最后，静脉注射和口服给药的t _1/2分别为 1.3 ± 0.6 小时和 3.1 ± 0.4 小时。