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Pharmacokinetics of esomeprazole following intravenous and oral administration in healthy dogs
Investigation into the pharmacokinetic profile of esomeprazole was conducted using eight healthy dogs after intravenous (IV) and oral (po) administration in a two-part randomized crossover study. The dogs were fasted for a minimum of 12 hours and then received esomeprazole either intravenously (dose...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Dove Medical Press
2016
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6044797/ https://www.ncbi.nlm.nih.gov/pubmed/30050845 http://dx.doi.org/10.2147/VMRR.S112643 |
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author | Cook, Emily K Satake, Nana Sykes, Ben W Bennett, Emma L Mills, Paul C |
author_facet | Cook, Emily K Satake, Nana Sykes, Ben W Bennett, Emma L Mills, Paul C |
author_sort | Cook, Emily K |
collection | PubMed |
description | Investigation into the pharmacokinetic profile of esomeprazole was conducted using eight healthy dogs after intravenous (IV) and oral (po) administration in a two-part randomized crossover study. The dogs were fasted for a minimum of 12 hours and then received esomeprazole either intravenously (dose range 0.93–1.48 mg/kg) or orally using an enteric-coated formulation (dose range 0.95–1.50 mg/kg). After a 1-week washout period, the dogs received an alternative treatment. Serial blood samples were collected at predetermined time points, and plasma esomeprazole concentrations were determined by using ultra-high-performance liquid chromatography–mass spectrometry. Noncompartmental pharmacokinetic analyses were performed. Then, the area under the plasma concentration/time curve (AUC) and maximal plasma concentration (C(max)) values were normalized to a 1.0 mg/kg dose of esomeprazole, that is, AUC/dose. Median (range) dose-normalized peak plasma concentration (C(max)) values for the IV and po formulations were 4.06 µg/mL (2.47–4.57 µg/mL) and 1.04 µg/mL (0.31–1.91 µg/mL), respectively. The median (range) time-to-peak concentration (T(max)) for the po formulation was 105 minutes (45–360 minutes). Median (range) plasma terminal half-life (t(½)) was 45.56 minutes (39.43–64.20 minutes) for the IV formulation and 63.97 minutes (44.02–109.94 minutes) for the enteric-coated po formulation. The median (range) po bioavailability was 63.33% (32.26%–79.77%). Clinically, both po and IV formulations were well tolerated with minimal side effects observed. |
format | Online Article Text |
id | pubmed-6044797 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2016 |
publisher | Dove Medical Press |
record_format | MEDLINE/PubMed |
spelling | pubmed-60447972018-07-26 Pharmacokinetics of esomeprazole following intravenous and oral administration in healthy dogs Cook, Emily K Satake, Nana Sykes, Ben W Bennett, Emma L Mills, Paul C Vet Med (Auckl) Original Research Investigation into the pharmacokinetic profile of esomeprazole was conducted using eight healthy dogs after intravenous (IV) and oral (po) administration in a two-part randomized crossover study. The dogs were fasted for a minimum of 12 hours and then received esomeprazole either intravenously (dose range 0.93–1.48 mg/kg) or orally using an enteric-coated formulation (dose range 0.95–1.50 mg/kg). After a 1-week washout period, the dogs received an alternative treatment. Serial blood samples were collected at predetermined time points, and plasma esomeprazole concentrations were determined by using ultra-high-performance liquid chromatography–mass spectrometry. Noncompartmental pharmacokinetic analyses were performed. Then, the area under the plasma concentration/time curve (AUC) and maximal plasma concentration (C(max)) values were normalized to a 1.0 mg/kg dose of esomeprazole, that is, AUC/dose. Median (range) dose-normalized peak plasma concentration (C(max)) values for the IV and po formulations were 4.06 µg/mL (2.47–4.57 µg/mL) and 1.04 µg/mL (0.31–1.91 µg/mL), respectively. The median (range) time-to-peak concentration (T(max)) for the po formulation was 105 minutes (45–360 minutes). Median (range) plasma terminal half-life (t(½)) was 45.56 minutes (39.43–64.20 minutes) for the IV formulation and 63.97 minutes (44.02–109.94 minutes) for the enteric-coated po formulation. The median (range) po bioavailability was 63.33% (32.26%–79.77%). Clinically, both po and IV formulations were well tolerated with minimal side effects observed. Dove Medical Press 2016-08-31 /pmc/articles/PMC6044797/ /pubmed/30050845 http://dx.doi.org/10.2147/VMRR.S112643 Text en © 2016 Cook et al. This work is published and licensed by Dove Medical Press Limited The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License (http://creativecommons.org/licenses/by-nc/3.0/). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. |
spellingShingle | Original Research Cook, Emily K Satake, Nana Sykes, Ben W Bennett, Emma L Mills, Paul C Pharmacokinetics of esomeprazole following intravenous and oral administration in healthy dogs |
title | Pharmacokinetics of esomeprazole following intravenous and oral administration in healthy dogs |
title_full | Pharmacokinetics of esomeprazole following intravenous and oral administration in healthy dogs |
title_fullStr | Pharmacokinetics of esomeprazole following intravenous and oral administration in healthy dogs |
title_full_unstemmed | Pharmacokinetics of esomeprazole following intravenous and oral administration in healthy dogs |
title_short | Pharmacokinetics of esomeprazole following intravenous and oral administration in healthy dogs |
title_sort | pharmacokinetics of esomeprazole following intravenous and oral administration in healthy dogs |
topic | Original Research |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6044797/ https://www.ncbi.nlm.nih.gov/pubmed/30050845 http://dx.doi.org/10.2147/VMRR.S112643 |
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