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Pharmacokinetics in plasma and alveolar regions of healthy calves subcutaneously administered a single dose of enrofloxacin

This study aimed to analyze the pharmacokinetics of enrofloxacin (ERFX) and its metabolite ciprofloxacin (CPFX) in plasma, as well as their migration to, and retention in, the epithelial lining fluid (ELF) and alveolar cells within the bronchoalveolar fluid (BALF). Four healthy calves were subcutane...

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Autores principales: KURAMAE, Tetsuro, OTOMARU, Konosuke, HIRATA, Masaya, ISHIKAWA, Shingo, NOGUCHI, Michiko, IKEDO, Tomonobu, HORINOUCHI, Chie, HAYASHI, Jun, TSUMAGARI, Keita, HOBO, Seiji
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Japanese Society of Veterinary Science 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7468075/
https://www.ncbi.nlm.nih.gov/pubmed/32565494
http://dx.doi.org/10.1292/jvms.20-0110
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author KURAMAE, Tetsuro
OTOMARU, Konosuke
HIRATA, Masaya
ISHIKAWA, Shingo
NOGUCHI, Michiko
IKEDO, Tomonobu
HORINOUCHI, Chie
HAYASHI, Jun
TSUMAGARI, Keita
HOBO, Seiji
author_facet KURAMAE, Tetsuro
OTOMARU, Konosuke
HIRATA, Masaya
ISHIKAWA, Shingo
NOGUCHI, Michiko
IKEDO, Tomonobu
HORINOUCHI, Chie
HAYASHI, Jun
TSUMAGARI, Keita
HOBO, Seiji
author_sort KURAMAE, Tetsuro
collection PubMed
description This study aimed to analyze the pharmacokinetics of enrofloxacin (ERFX) and its metabolite ciprofloxacin (CPFX) in plasma, as well as their migration to, and retention in, the epithelial lining fluid (ELF) and alveolar cells within the bronchoalveolar fluid (BALF). Four healthy calves were subcutaneously administered a single dose of ERFX (5 mg/kg). ERFX and CPFX dynamics post-administration were analyzed via a non-compartment model, including the absorption phase. The Cmax of plasma ERFX was 1.6 ± 0.4 µg/ml at 2.3 ± 0.5 hr post-administration and gradually decreased to 0.14 ± 0.03 µg/ml at 24 hr following administration. The mean residence time between 0 and 24 hr (MRT(0–24)) in plasma was 6.9 ± 1.0 hr. ERFX concentrations in ELF and alveolar cells peaked at 3.0 ± 2.0 hr and 4.0 ± 2.3 hr following administration, respectively, and gradually decreased to 0.9 ± 0.8 µg/ml and 0.8 ± 0.5 µg/ml thereafter. The plasma half-life (t1/2) of ERFX was 6.5 ± 0.7 hr, while that in ELF and alveolar cells was 6.5 ± 3.6 and 7.4 ± 4.3 hr, respectively. The Cmax and the area under the concentration-time curve for 0–24 hr for ERFX were significantly higher in alveolar cells than in plasma (P<0.05). These results suggest that ERFX is distributed at high concentrations in ELF and is retained at high concentrations in alveolar cells after 24 hr in the BALF region; hence, ERFX may be an effective therapeutic agent against pneumonia.
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spelling pubmed-74680752020-09-08 Pharmacokinetics in plasma and alveolar regions of healthy calves subcutaneously administered a single dose of enrofloxacin KURAMAE, Tetsuro OTOMARU, Konosuke HIRATA, Masaya ISHIKAWA, Shingo NOGUCHI, Michiko IKEDO, Tomonobu HORINOUCHI, Chie HAYASHI, Jun TSUMAGARI, Keita HOBO, Seiji J Vet Med Sci Internal Medicine This study aimed to analyze the pharmacokinetics of enrofloxacin (ERFX) and its metabolite ciprofloxacin (CPFX) in plasma, as well as their migration to, and retention in, the epithelial lining fluid (ELF) and alveolar cells within the bronchoalveolar fluid (BALF). Four healthy calves were subcutaneously administered a single dose of ERFX (5 mg/kg). ERFX and CPFX dynamics post-administration were analyzed via a non-compartment model, including the absorption phase. The Cmax of plasma ERFX was 1.6 ± 0.4 µg/ml at 2.3 ± 0.5 hr post-administration and gradually decreased to 0.14 ± 0.03 µg/ml at 24 hr following administration. The mean residence time between 0 and 24 hr (MRT(0–24)) in plasma was 6.9 ± 1.0 hr. ERFX concentrations in ELF and alveolar cells peaked at 3.0 ± 2.0 hr and 4.0 ± 2.3 hr following administration, respectively, and gradually decreased to 0.9 ± 0.8 µg/ml and 0.8 ± 0.5 µg/ml thereafter. The plasma half-life (t1/2) of ERFX was 6.5 ± 0.7 hr, while that in ELF and alveolar cells was 6.5 ± 3.6 and 7.4 ± 4.3 hr, respectively. The Cmax and the area under the concentration-time curve for 0–24 hr for ERFX were significantly higher in alveolar cells than in plasma (P<0.05). These results suggest that ERFX is distributed at high concentrations in ELF and is retained at high concentrations in alveolar cells after 24 hr in the BALF region; hence, ERFX may be an effective therapeutic agent against pneumonia. The Japanese Society of Veterinary Science 2020-06-19 2020-08 /pmc/articles/PMC7468075/ /pubmed/32565494 http://dx.doi.org/10.1292/jvms.20-0110 Text en ©2020 The Japanese Society of Veterinary Science This is an open-access article distributed under the terms of the Creative Commons Attribution Non-Commercial No Derivatives (by-nc-nd) License. (CC-BY-NC-ND 4.0: https://creativecommons.org/licenses/by-nc-nd/4.0/)
spellingShingle Internal Medicine
KURAMAE, Tetsuro
OTOMARU, Konosuke
HIRATA, Masaya
ISHIKAWA, Shingo
NOGUCHI, Michiko
IKEDO, Tomonobu
HORINOUCHI, Chie
HAYASHI, Jun
TSUMAGARI, Keita
HOBO, Seiji
Pharmacokinetics in plasma and alveolar regions of healthy calves subcutaneously administered a single dose of enrofloxacin
title Pharmacokinetics in plasma and alveolar regions of healthy calves subcutaneously administered a single dose of enrofloxacin
title_full Pharmacokinetics in plasma and alveolar regions of healthy calves subcutaneously administered a single dose of enrofloxacin
title_fullStr Pharmacokinetics in plasma and alveolar regions of healthy calves subcutaneously administered a single dose of enrofloxacin
title_full_unstemmed Pharmacokinetics in plasma and alveolar regions of healthy calves subcutaneously administered a single dose of enrofloxacin
title_short Pharmacokinetics in plasma and alveolar regions of healthy calves subcutaneously administered a single dose of enrofloxacin
title_sort pharmacokinetics in plasma and alveolar regions of healthy calves subcutaneously administered a single dose of enrofloxacin
topic Internal Medicine
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7468075/
https://www.ncbi.nlm.nih.gov/pubmed/32565494
http://dx.doi.org/10.1292/jvms.20-0110
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