Simultaneous determination of fosaprepitant and its metabolite aprepitant in human plasma by liquid chromatography-tandem mass spectrometry
10.16438/j.0513-4870.2017-0788
- VernacularTitle:LC-MS/MS法同时测定人血浆中福沙匹坦和代谢物阿瑞匹坦
- Author:
Jia-le SHEN
1
;
Bin ZAN
2
;
Xiao-yan CHEN
2
;
Da-fang ZHONG
1
Author Information
1. College of Pharmacy, Zhejiang University of Technology, Hangzhou 310014, China
2. Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
- Publication Type:ORIGINAL ARTICLES
- Keywords:
LC-MS/MS;
fosaprepitant;
aprepitant;
stability;
human pharmacokinetics
- From:
Acta Pharmaceutica Sinica
2018;53(1):121-126
- CountryChina
- Language:Chinese
-
Abstract:
An LC-MS/MS method was developed for the simultaneous determination of fosaprepitant and aprepitant in human plasma, and applied to a pharmacokinetic study of 150 mg fosaprepitant dimeglumine injection to 12 Chinese healthy volunteers. The analytes and internal standards were extracted from plasma by protein precipitation with acetonitrile and separated on a Cortex C18+ (50 mm×2.1 mm, 2.7 μm) column using a gradient elution procedure. Mass spectrometry was performed in negative MRM mode, and parent-to-produce transitions were as follows:m/z 613.1→78.9 for fosaprepitant, m/z 617.0→78.9 for d4-fosaprepitant, m/z 533.2→275.1 for aprepitant and m/z 537.2→279.1 for d4-aprepitant. Plasma sample was basified to stabilize fosaprepitant. The standard curves were demonstrated to be liner in the range of 15.0 to 6 000 ng·mL-1 for fosaprepitant and 10.0 to 4 000 ng·mL-1 for aprepitant. The intra-day precisions and inter-day precisions and accuracy were within the acceptable limits for all concentrations.
