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- Title
Evaluation of the Effects of Apatinib on the Pharmacokinetics of Venlafaxine and O‐desmethylvenlafaxine in SD Male Rats by UPLC–MS/MS.
- Authors
Bao, Su‐su; Wen, Jian; Lin, Qian‐meng; Li, Ying‐hui; Huang, Yang‐ge; Zhou, Hong‐yu; Hu, Guo‐xin
- Abstract
The objective of this study was to evaluate the effect of apatinib on the pharmacokinetics of venlafaxine and O‐desmethylvenlafaxine in SD rats and the inhibitory effects of apatinib on venlafaxine in rat and human liver microsomes. Twenty‐one SD male rats were randomly divided into three groups (n = 7): group A (multiple dose of 40 mg/kg apatinib for 7 days), group B (single dose of 40 mg/kg apatinib) and group C (the control group). All samples were measured by UPLC‐MS/MS. The results indicated that a single dose of apatinib increased the AUC(0‐t), AUC(0‐∞) and Cmax of both venlafaxine and O‐desmethylvenlafaxine significantly, while Vz/F and CLz/F were decreased. As for group A, only AUC(0‐t) and CLz/F of venlafaxine were changed, while no parameters of O‐desmethylvenlafaxine were altered. In addition, apatinib was determined to be a mixed inhibitor of venlafaxine.
- Subjects
VENLAFAXINE; DRUG side effects; DRUG efficacy; TREATMENT effectiveness; LABORATORY rats
- Publication
Basic & Clinical Pharmacology & Toxicology, 2018, Vol 123, Issue 6, p721
- ISSN
1742-7835
- Publication type
Article
- DOI
10.1111/bcpt.13081