UPLC-MS/MS analysis of SZJ-1207 in rat plasma, urine, feces and bile for pharmacokinetic studies

Abstract

AbstractSZJ-1207 is a natural product extracted from Stephanotis mucronata (Blanco) Merr which has significant antidepressant effects in various depression mouse models, without obvious acute toxicity or sedative-hypnotic side effects. The aim of this study was to preliminarily clarify the pharmacokinetic characteristics of SZJ-1207 in rats after a single intragastric and intravenous administration. In this study, sensitive and reliable UPLC-MS/MS quantification methods were established and then successfully applied to the pharmacokinetic study of SZJ-1207 in rats. The linear range of SZJ-1207 were 0.5–400 ng mL−1 in plasma, feaces, bile and 20–4,000 ng mL−1 in urine, respectively (r > 0.99). All methods met the requirements of ICH M10. The results of pharmaconetic study showed that Cmax, AUC(0-t) and AUC(0-∞) had linear relationships with the administered doses in the range of 0.5–4.5 mg kg−1. There was a significant gender difference in the AUC (0-t) of 0.5 and 1.5 mg kg−1 and Cmax of 1.5 mg kg−1 after ig (P < 0.05). The excretion rates of SZJ-1207 were 8.46 ± 4.82% in feces, 1.89 ± 1.08% in urine, and 0.179 ± 0.118% in bile. The oral absolute bioavailability of SZJ-1207 was calculated as 64.64%.