Abstract
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, t1/2 was 1.3 ± 0.6 h and 3.1 ± 0.4 h for intravenous and oral administration, respectively.
Highlights
Aconitum, a genus of flowering plant species, is widely used in the clinic owing to its significant therapeutic effect in the treatment of rheumatic arthralgia [1,2,3]
Validation. e selectivity of the method was evaluated by analyzing six lots of blank rat plasma, blank plasma spiked with 10-hydroxy mesaconitine and internal standard (IS), and a rat plasma sample
No endogenous substances were found to intervene in the detection of 10-hydroxy mesaconitine
Summary
A genus of flowering plant species, is widely used in the clinic owing to its significant therapeutic effect in the treatment of rheumatic arthralgia [1,2,3]. Aconitum contains alkaloids such as mesaconitine and aconitine that exhibit anti-inflammatory and analgesic activity but at the same time suffer from strong toxicity and narrow therapeutic window [4,5,6,7]. E metabolite 10-hydroxyl-mesaconitine is toxic and can be detected in both rat blood and urine; it was selected for quantification in this study. UPLC-MS/MS was used to analyze the metabolite 10-hydroxy mesaconitine in rat plasma after oral and intravenous administration. is study is useful for elucidating the pharmacological effects of aconitine alkaloids
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