Pharmacokinetics of esomeprazole following intravenous and oral administration in healthy dogs

Emily K Cook, Nana Satake, Ben W Sykes, Emma L Bennett, Paul C Mills School of Veterinary Sciences, The University of Queensland, Gatton, Queensland, Australia Abstract: Investigation into the pharmacokinetic profile of esomeprazole was conducted using eight healt...

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Autores principales:	Cook EK, Satake N, Sykes BW, Bennett EL, Mills PC
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2016
Materias:	esomeprazole dog proton pump inhibitors gastric ulcers Veterinary medicine SF600-1100
Acceso en línea:	https://doaj.org/article/d4cd161394b14691aa0c797c7f602406
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spelling	oai:doaj.org-article:d4cd161394b14691aa0c797c7f6024062021-12-02T07:18:58ZPharmacokinetics of esomeprazole following intravenous and oral administration in healthy dogs2230-2034https://doaj.org/article/d4cd161394b14691aa0c797c7f6024062016-08-01T00:00:00Zhttps://www.dovepress.com/pharmacokinetics-of-esomeprazole-following-intravenous-and-oral-admini-peer-reviewed-article-VMRRhttps://doaj.org/toc/2230-2034Emily K Cook, Nana Satake, Ben W Sykes, Emma L Bennett, Paul C Mills School of Veterinary Sciences, The University of Queensland, Gatton, Queensland, Australia Abstract: 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 (Cmax) values were normalized to a 1.0 mg/kg dose of esomeprazole, that is, AUC/dose. Median (range) dose-normalized peak plasma concentration (Cmax) 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 (Tmax) for the po formulation was 105 minutes (45–360 minutes). Median (range) plasma terminal half-life (t½) 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. Keywords: proton pump inhibitors, gastric ulcers, and oesophagitisCook EKSatake NSykes BWBennett ELMills PCDove Medical Pressarticleesomeprazoledogproton pump inhibitorsgastric ulcersVeterinary medicineSF600-1100ENVeterinary Medicine: Research and Reports, Vol Volume 7, Pp 123-131 (2016)
institution	DOAJ
collection	DOAJ
language	EN
topic	esomeprazole dog proton pump inhibitors gastric ulcers Veterinary medicine SF600-1100
spellingShingle	esomeprazole dog proton pump inhibitors gastric ulcers Veterinary medicine SF600-1100 Cook EK Satake N Sykes BW Bennett EL Mills PC Pharmacokinetics of esomeprazole following intravenous and oral administration in healthy dogs
description	Emily K Cook, Nana Satake, Ben W Sykes, Emma L Bennett, Paul C Mills School of Veterinary Sciences, The University of Queensland, Gatton, Queensland, Australia Abstract: 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 (Cmax) values were normalized to a 1.0 mg/kg dose of esomeprazole, that is, AUC/dose. Median (range) dose-normalized peak plasma concentration (Cmax) 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 (Tmax) for the po formulation was 105 minutes (45–360 minutes). Median (range) plasma terminal half-life (t½) 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. Keywords: proton pump inhibitors, gastric ulcers, and oesophagitis
format	article
author	Cook EK Satake N Sykes BW Bennett EL Mills PC
author_facet	Cook EK Satake N Sykes BW Bennett EL Mills PC
author_sort	Cook EK
title	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_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_sort	pharmacokinetics of esomeprazole following intravenous and oral administration in healthy dogs
publisher	Dove Medical Press
publishDate	2016
url	https://doaj.org/article/d4cd161394b14691aa0c797c7f602406
work_keys_str_mv	AT cookek pharmacokineticsofesomeprazolefollowingintravenousandoraladministrationinhealthydogs AT sataken pharmacokineticsofesomeprazolefollowingintravenousandoraladministrationinhealthydogs AT sykesbw pharmacokineticsofesomeprazolefollowingintravenousandoraladministrationinhealthydogs AT bennettel pharmacokineticsofesomeprazolefollowingintravenousandoraladministrationinhealthydogs AT millspc pharmacokineticsofesomeprazolefollowingintravenousandoraladministrationinhealthydogs
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Pharmacokinetics of esomeprazole following intravenous and oral administration in healthy dogs

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