Development of a simple and rapid UPLC-MS/MS method for determination of 8-deacetyl-yunaconitine in rat plasma and its application to pharmacokinetics

In this paper, UPLC-MS/MS was used to determine 8-deacetyl-yunaconitine in the plasma of rats after oral and intravenous administration. Six rats were orally (po) administered 8-deacetyl-yunaconitine (5 mg/kg), while another six rats were intravenously (iv) administered the drug (0.1 mg/kg). A standard curve of known concentrations of 8-deacetyl-yunaconitine in rat plasma was generated over the range of 0.3-600 ng/mL. The intra-day and inter-day precision of 8-deacetyl-yunaconitine in rat plasma was lower than 15 %, while the accuracy ranged between 97.7 % and 105.5 %. In addition, the matrix effect ranged between 95.3 % and 105.6 %, while the recovery was greater than 82.8 %. This determined method was then applied in measuring the pharmacokinetics of 8-deacetyl-yunaconitine in rats. The AUC(()(0-)(t)) values were 73.0 +/- 24.6 and 1770.0 +/- 530.6 ng/mL h for intravenous and oral administration, respectively, and the bioavailability was 48.5 %. The half-life (t(1/2)) was determined to be 4.5 +/- 1.7 h and 3.2 +/- 0.7 h for intravenous and oral administration, respectively, indicating that the metabolism of the xenobiotic was quick in the rats. (C) 2021 Elsevier B.V. All rights reserved.

Automated summary

In this study, UPLC-MS/MS was used to determine the concentration of 8-deacetyl-yunaconitine in rat plasma after oral and intravenous administration. The pharmacokinetics of the drug showed differences between intravenous and oral administration, with a quick metabolism observed in rats.