Volume 21 Issue 11
Nov.  2023
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Article Navigation >  Chinese Journal of General Practice  > 2023  >  21(11): 1841-1844
LI Hongtao, HE Cuixia, ZHOU Huan, WANG Huaxue. Pharmacokinetic study of single-dose fosaprepitant dimeglumine (150 mg) in healthy Chinese volunteers[J]. Chinese Journal of General Practice, 2023, 21(11): 1841-1844. doi: 10.16766/j.cnki.issn.1674-4152.003238
Citation: LI Hongtao, HE Cuixia, ZHOU Huan, WANG Huaxue. Pharmacokinetic study of single-dose fosaprepitant dimeglumine (150 mg) in healthy Chinese volunteers[J]. Chinese Journal of General Practice, 2023, 21(11): 1841-1844. doi: 10.16766/j.cnki.issn.1674-4152.003238
shu

Pharmacokinetic study of single-dose fosaprepitant dimeglumine (150 mg) in healthy Chinese volunteers

doi: 10.16766/j.cnki.issn.1674-4152.003238
  • 1.

    Clinical Trials Center, the First Affiliated Hospital of Bengbu Medical College, Bengbu, Anhui 233004, China

Funds:

 KJ2021A0815

 2023SYKFZ06

 2008085QH401

  • Received Date: 2022-12-11
    Available Online: 2024-01-13
    Abstract
  •   Objective  To study the time course of blood concentration after single-dose intravenous infusion of fosaprepitant dimeglumine for injection manufactured by Jiangsu Aosaikang Pharmaceutical Co., Ltd. in healthy Chinese subjects and to estimate the corresponding pharmacokinetic parameters. To evaluate the safety of fosaprepitant dimeglumine for injection in healthy Chinese subjects.  Methods  This was a single-centre, single-dose, single-dose study. Twelve subjects were enrolled under fasting conditions. Each of them received fosaprepitant dimeglumine for injection 150 mg for (30±2) min. The concentrations of fosaprepitant and its metabolite aprepitant in human plasma were determined by liquid chromatography tandem-mass spectrometry. WinNonlin6.4 pharmacokinetic software from Phoenix was used for pharmacokinetic calculation and SAS 9.4 for statistical analysis.  Results  In healthy volunteers, fosaprepitant dimeglumine (150 mg) was administered intravenously for (30±2) min and plasma fosaprepitant peaked and was rapidly cleared. The main pharmacokinetic parameters were as follows: Tmax was 0.333 h; Cmax was 4.316 μg/mL; AUC0-t is 2.090 h·μg·mL-1; AUC0-∞ is 2.098 h·μg·mL-1. Fosaprepitant is rapidly converted to aprepitant in the body and its blood concentration peaks at the end of the infusion. Key pharmacokinetic parameters were as follows: Tmax was 0.583 h; Cmax was 4.888 μg/mL; AUC0-t was 49.483 h·μg·mL-1; AUC0-∞ was 54.658 h·μg·mL-1. Aprepitant was slowly eliminated in vivo with a mean elimination half-life of 19.3 h. The plasma exposure of aprepitant was much higher than that of the originator drug fosaprepitant, approximately 25.7 times that of fosaprepitant. There were no unexpected adverse events, serious adverse events or adverse events leading to subject withdrawal throughout the study.  Conclusion  After a single intravenous infusion of fosaprepitant dimeglumine (150 mg) for injection, the pharmacokinetic parameters of fosaprepitant and aprepitant were consistent with those reported in the original research, and they were well tolerated in healthy Chinese volunteers.

     

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