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Effects of diclofenac on the pharmacokinetics of celastrol in rats and its transport
Context: Diclofenac and celastrol are always used together for the treatment of rheumatoid arthritis; the herb–drug interaction potential between diclofenac and celastrol is still unknown. Objective: This study investigates the effects of diclofenac on the pharmacokinetics of celastrol in rats. Mate...
Autores principales: | , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Taylor & Francis
2018
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6130456/ https://www.ncbi.nlm.nih.gov/pubmed/29651912 http://dx.doi.org/10.1080/13880209.2018.1459740 |
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author | Wang, Zengfu Chen, Dali Wang, Zhongwei |
author_facet | Wang, Zengfu Chen, Dali Wang, Zhongwei |
author_sort | Wang, Zengfu |
collection | PubMed |
description | Context: Diclofenac and celastrol are always used together for the treatment of rheumatoid arthritis; the herb–drug interaction potential between diclofenac and celastrol is still unknown. Objective: This study investigates the effects of diclofenac on the pharmacokinetics of celastrol in rats. Materials and methods: Twelve male Sprague-Dawley rats were divided into two groups and received celastrol (1 mg/kg) or both celastrol (1 mg/kg) and diclofenac (10 mg/kg) by oral gavage, and blood samples were collected via the oculi chorioideae vein and determined using the LC-MS method developed in this study. Additionally, the effects of diclofenac on the transport of celastrol were investigated using a Caco-2 cell transwell model. Results: Diclofenac could significantly (p < 0.05) decrease the C(max) (from 66.93 ± 10.28 to 41.25 ± 8.06 ng/mL) and AUC(0-t) (from 765.84 ± 163.61 to 451.33 ± 110.88 μg × h/L) of celastrol in rats. The efflux ratio of celastrol increased significantly (p < 0.05) from 3.12 to 4.55 with the treatment of diclofenac. Discussion and conclusion: These results indicated that diclofenac could decrease the system exposure of celastrol in rats when they are co-administered, and these effects might be exerted via decreasing its absorption in intestine. |
format | Online Article Text |
id | pubmed-6130456 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2018 |
publisher | Taylor & Francis |
record_format | MEDLINE/PubMed |
spelling | pubmed-61304562018-09-27 Effects of diclofenac on the pharmacokinetics of celastrol in rats and its transport Wang, Zengfu Chen, Dali Wang, Zhongwei Pharm Biol Research Article Context: Diclofenac and celastrol are always used together for the treatment of rheumatoid arthritis; the herb–drug interaction potential between diclofenac and celastrol is still unknown. Objective: This study investigates the effects of diclofenac on the pharmacokinetics of celastrol in rats. Materials and methods: Twelve male Sprague-Dawley rats were divided into two groups and received celastrol (1 mg/kg) or both celastrol (1 mg/kg) and diclofenac (10 mg/kg) by oral gavage, and blood samples were collected via the oculi chorioideae vein and determined using the LC-MS method developed in this study. Additionally, the effects of diclofenac on the transport of celastrol were investigated using a Caco-2 cell transwell model. Results: Diclofenac could significantly (p < 0.05) decrease the C(max) (from 66.93 ± 10.28 to 41.25 ± 8.06 ng/mL) and AUC(0-t) (from 765.84 ± 163.61 to 451.33 ± 110.88 μg × h/L) of celastrol in rats. The efflux ratio of celastrol increased significantly (p < 0.05) from 3.12 to 4.55 with the treatment of diclofenac. Discussion and conclusion: These results indicated that diclofenac could decrease the system exposure of celastrol in rats when they are co-administered, and these effects might be exerted via decreasing its absorption in intestine. Taylor & Francis 2018-04-13 /pmc/articles/PMC6130456/ /pubmed/29651912 http://dx.doi.org/10.1080/13880209.2018.1459740 Text en © 2018 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. http://creativecommons.org/licenses/by/4.0/ This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Research Article Wang, Zengfu Chen, Dali Wang, Zhongwei Effects of diclofenac on the pharmacokinetics of celastrol in rats and its transport |
title | Effects of diclofenac on the pharmacokinetics of celastrol in rats and its transport |
title_full | Effects of diclofenac on the pharmacokinetics of celastrol in rats and its transport |
title_fullStr | Effects of diclofenac on the pharmacokinetics of celastrol in rats and its transport |
title_full_unstemmed | Effects of diclofenac on the pharmacokinetics of celastrol in rats and its transport |
title_short | Effects of diclofenac on the pharmacokinetics of celastrol in rats and its transport |
title_sort | effects of diclofenac on the pharmacokinetics of celastrol in rats and its transport |
topic | Research Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6130456/ https://www.ncbi.nlm.nih.gov/pubmed/29651912 http://dx.doi.org/10.1080/13880209.2018.1459740 |
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