Population pharmacokinetic/pharmacodynamic modelling of nifekalant in healthy Chinese volunteers.


Journal

European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
ISSN: 1879-0720
Titre abrégé: Eur J Pharm Sci
Pays: Netherlands
ID NLM: 9317982

Informations de publication

Date de publication:
01 Aug 2020
Historique:
received: 25 10 2019
revised: 11 05 2020
accepted: 19 05 2020
pubmed: 27 5 2020
medline: 22 6 2021
entrez: 27 5 2020
Statut: ppublish

Résumé

Nifekalant is a class III antiarrhythmic drug, and its major adverse effect is prolongation of the QT interval. This study analysed data generated from a pharmacokinetic (PK) study to develop a population PK/pharmacodynamics (PD) model for describing the relationship between plasma concentrations and prolongation of the QT interval over time following intravenous administration of nifekalant. This open-labelled, phase I clinical study comprised two dose level groups of eight healthy Chinese volunteers. Concentrations of nifekalant in plasma samples collected at set time-points were determined using a liquid chromatography-tandem mass spectrometry (LC-MS/MS) method. A PK/PD model was constructed using a non-linear mixed-effects approach (Phoenix NLME 8.1). Furthermore, demographic covariates of the model were investigated and a concentration factor (Conc

Identifiants

pubmed: 32454129
pii: S0928-0987(20)30174-3
doi: 10.1016/j.ejps.2020.105385
pii:
doi:

Substances chimiques

Pyrimidinones 0
nifekalant 5VZ7GZM43E

Types de publication

Clinical Trial, Phase I Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

105385

Informations de copyright

Copyright © 2020 Elsevier B.V. All rights reserved.

Auteurs

Jiashan Zhang (J)

Department of Phase I Clinical Trial Unit, General Hospital of Northern Theater Command; Department of Clinical Pharmacy, School of Life Science and Biopharmaceutical Institute, Shenyang Pharmaceutical University, Shenyang, China.

Ying Zan (Y)

Clinical Trial Institution Office, PKUCare Luzhong Hospital, Zibo, China.

Hua Huo (H)

Department of Phase I Clinical Trial Unit, General Hospital of Northern Theater Command.

Yanfang Liu (Y)

Department of Phase I Clinical Trial Unit, General Hospital of Northern Theater Command.

Yunbiao Tang (Y)

Department of Phase I Clinical Trial Unit, General Hospital of Northern Theater Command. Electronic address: tangyb99@163.com.

Yaling Han (Y)

Cardiovascular Research Institute and Department of Cardiology, General Hospital of Northern Theater Command. Electronic address: hanyaling01@163.com.

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Classifications MeSH