Effect of Wuziyanzong pill on metabolism of dapoxetine in vivo and in vitro

Publication date: Available online 15 December 2018Source: Journal of Pharmaceutical and Biomedical AnalysisAuthor(s): Hong-chang Yuan, Zhi-jian Deng, Xin-min Liu, Ting-fang Dong, Xiang-jun Qiu, Zeng NanAbstractIn vitro incubation of rat liver microsomes with 30 µL of 100 μmol L-1 dapoxetine and 30 µL of 10, 100, 250, 500, 1,000, 2,500, or 5,000 μg mL-1 Wuziyanzong pill was performed at 37℃ for 60 min. Dapoxetine concentration was analyzed by high performance liquid chromatography (HPLC). The half maximal inhibitory concentration (IC50) of Wuziyanzong pill on metabolism of dapoxetine was 296.10 μg mL-1in vitro. Twelve SD rats were randomly divided into 2 groups: Control group and Wuziyanzong pill group. The two groups were administrated with 10 mL·kg-1 saline (Control group) or 10 mL·kg-1 Wuziyanzong pill solution (Experimental group, solution contained 200 mg mL-1 Wuziyanzong pill) for 15 consecutive days. Following administration of saline or Wuziyanzong pill on the 15th day, 20 mg kg-1 dapoxetine was administered to all rats. Blood was collected from the tail vein (0.3 mL) at multiple time points, and ultra-high performance liquid chromatography tandem mass spectrometry (UHPLC-MS/MS) was used to determine the concentration of dapoxetine and its main metabolites, dapoxetine-N-Oxide and desmethyldapoxetine in rats. Pharmacokinetic analysis of dapoxetine showed that area under the concentration-time curve (AUC) and mean maximum plasm...
Source: Journal of Pharmaceutical and Biomedical Analysis - Category: Drugs & Pharmacology Source Type: research