Development of an UPLC–MS/MS assay to determine psoralidin in rat plasma and its application in a pharmacokinetic study after intragastric administration

Abstract

Psoralidin has a variety of pharmacological activities, such as anti-tumor, anti-depressant, and anti-inflammatory activities. This study aims at developing a rapid ultra-performance liquid chromatography–tandem mass spectrometry (UPLC–MS/MS) method to determine psoralidin in rat plasma and studying the pharmacokinetic characteristic of psoralidin after intragastric administration of 20 and 40 mg/kg. Alpinetin was used as an internal standard (IS), and the plasma samples were precipitated with acetonitrile. The calibration curves were linear over the range of 0.2–250 ng/mL (R2 = 0.993). The pharmacokinetic parameters were calculated by DAS 3.0. Half-life (t1/2) was 7.2 ± 0.97 h and 7.1 ± 0.27 h for different dosages, respectively. Tmax was 4.2 ± 1.1 h and 4.0 ± 1.1 h for different dosages, respectively. Apparent volume of distribution (Vd) for different dosages was 630.1 ± 168.8 and 600.1 ± 138.8 L/kg, respectively. Clearance (CL) was 105.6 ± 29.2 and 100.6 ± 22.2 L/h/kg for different dosages, indicating that psoralidin was mainly distributed in rat tissues. The pharmacokinetic study provided important information for further clinical application in the treatment of cancer and osteoporosis.

A review of alpha-glucosidase inhibitors from plants as potential candidates for the treatment of type-2 diabetes

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“…The half-life (T 1/2 ) was 7.2 h and 7.1 h, Cmax was 0.0095 mg/L and 0.0263 mg/L, and AUC was 0.0954 mg/L h and 0.2 mg/L h for different dosages, respectively. Moreover, psoralidin displayed a large volume of distribution (V d ) (600.1 and 630.1 L/kg for the 20 and 40 mg/kg dosages, respectively) (Feng et al 2020 ). The intravenous administration of this molecule (2 mg/kg) in male Wister rats showed higher bioavailability with Cmax value of 2.19 mg/L, AUC value of 1.95 mg/L.h and half life of 4.45 h (Shi et al 2016b ).…”