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Determination of cepharanthine in rat plasma by LC–MS/MS and its application to a pharmacokinetic study

Context: Cepharanthine (CPA) has been reported to possess a wide range of pharmacological activities. Objective: This study investigates the pharmacokinetic characteristics after oral or intravenous administration of CPA by using a sensitive and rapid LC–MS/MS method. Materials and methods: A sensit...

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Autores principales: Deng, Yingbin, Wu, Weijun, Ye, Sunzhi, Wang, Wei, Wang, Zhiyi
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2017
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6130670/
https://www.ncbi.nlm.nih.gov/pubmed/28521597
http://dx.doi.org/10.1080/13880209.2017.1328446
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author Deng, Yingbin
Wu, Weijun
Ye, Sunzhi
Wang, Wei
Wang, Zhiyi
author_facet Deng, Yingbin
Wu, Weijun
Ye, Sunzhi
Wang, Wei
Wang, Zhiyi
author_sort Deng, Yingbin
collection PubMed
description Context: Cepharanthine (CPA) has been reported to possess a wide range of pharmacological activities. Objective: This study investigates the pharmacokinetic characteristics after oral or intravenous administration of CPA by using a sensitive and rapid LC–MS/MS method. Materials and methods: A sensitive and rapid LC–MS/MS method was developed for the determination of CPA in Sprague–Dawley rat plasma. Twelve rats were equally randomized into two groups, including the intravenous group (1 mg/kg) and the oral group (10 mg/kg). Blood samples (250 μL) were collected at designated time points and determined using this method. The pharmacokinetic parameters were calculated. Results: The calibration curve was linear within the range of 0.1–200 ng/mL (r = 0.999) with the lower limit of quantification at 0.1 ng/mL. After 1 mg/kg intravenous injection, the concentration of CPA reached a maximum of 153.17 ± 16.18 ng/mL and the t(1/2) was 6.76 ± 1.21 h. After oral administration of 10 mg/kg of CPA, CPA was not readily absorbed and reached C(max) 46.89 ± 5.25 ng/mL at approximately 2.67 h. The t(1/2) was 11.02 ± 1.32 h. The absolute bioavailability of CPA by oral route was 5.65 ± 0.35%, and the bioavailability was poor. Discussion and conclusions: The results indicate that the bioavailability of CPA was poor in rats, and further research should be conducted to investigate the reason for its poor bioavailability and address this problem.
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spelling pubmed-61306702018-09-27 Determination of cepharanthine in rat plasma by LC–MS/MS and its application to a pharmacokinetic study Deng, Yingbin Wu, Weijun Ye, Sunzhi Wang, Wei Wang, Zhiyi Pharm Biol Research Article Context: Cepharanthine (CPA) has been reported to possess a wide range of pharmacological activities. Objective: This study investigates the pharmacokinetic characteristics after oral or intravenous administration of CPA by using a sensitive and rapid LC–MS/MS method. Materials and methods: A sensitive and rapid LC–MS/MS method was developed for the determination of CPA in Sprague–Dawley rat plasma. Twelve rats were equally randomized into two groups, including the intravenous group (1 mg/kg) and the oral group (10 mg/kg). Blood samples (250 μL) were collected at designated time points and determined using this method. The pharmacokinetic parameters were calculated. Results: The calibration curve was linear within the range of 0.1–200 ng/mL (r = 0.999) with the lower limit of quantification at 0.1 ng/mL. After 1 mg/kg intravenous injection, the concentration of CPA reached a maximum of 153.17 ± 16.18 ng/mL and the t(1/2) was 6.76 ± 1.21 h. After oral administration of 10 mg/kg of CPA, CPA was not readily absorbed and reached C(max) 46.89 ± 5.25 ng/mL at approximately 2.67 h. The t(1/2) was 11.02 ± 1.32 h. The absolute bioavailability of CPA by oral route was 5.65 ± 0.35%, and the bioavailability was poor. Discussion and conclusions: The results indicate that the bioavailability of CPA was poor in rats, and further research should be conducted to investigate the reason for its poor bioavailability and address this problem. Taylor & Francis 2017-05-19 /pmc/articles/PMC6130670/ /pubmed/28521597 http://dx.doi.org/10.1080/13880209.2017.1328446 Text en © 2017 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
Deng, Yingbin
Wu, Weijun
Ye, Sunzhi
Wang, Wei
Wang, Zhiyi
Determination of cepharanthine in rat plasma by LC–MS/MS and its application to a pharmacokinetic study
title Determination of cepharanthine in rat plasma by LC–MS/MS and its application to a pharmacokinetic study
title_full Determination of cepharanthine in rat plasma by LC–MS/MS and its application to a pharmacokinetic study
title_fullStr Determination of cepharanthine in rat plasma by LC–MS/MS and its application to a pharmacokinetic study
title_full_unstemmed Determination of cepharanthine in rat plasma by LC–MS/MS and its application to a pharmacokinetic study
title_short Determination of cepharanthine in rat plasma by LC–MS/MS and its application to a pharmacokinetic study
title_sort determination of cepharanthine in rat plasma by lc–ms/ms and its application to a pharmacokinetic study
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6130670/
https://www.ncbi.nlm.nih.gov/pubmed/28521597
http://dx.doi.org/10.1080/13880209.2017.1328446
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