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Evaluation of Pharmacokinetics and Safety with Bioequivalence of Ibuprofen Sustained-Release Capsules of Two Formulations, in Chinese Healthy Volunteers: Bioequivalence Study
PURPOSE: Ibuprofen is the first of the nonsteroidal anti-inflammatory drug (NSAID) to be used in the clinic. Our aim was to explore the pharmacokinetics (PK), bioequivalence, food effect, and safety of oral ibuprofen sustained-release capsules by two sponsors in healthy volunteers (HVs). METHODS: Tw...
Autores principales: | , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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Dove
2023
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10295470/ https://www.ncbi.nlm.nih.gov/pubmed/37384214 http://dx.doi.org/10.2147/DDDT.S404756 |
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author | Huang, Chunqi Yin, Zhou Yang, Yeqing Mo, Nan Yang, Hui Wang, Ying |
author_facet | Huang, Chunqi Yin, Zhou Yang, Yeqing Mo, Nan Yang, Hui Wang, Ying |
author_sort | Huang, Chunqi |
collection | PubMed |
description | PURPOSE: Ibuprofen is the first of the nonsteroidal anti-inflammatory drug (NSAID) to be used in the clinic. Our aim was to explore the pharmacokinetics (PK), bioequivalence, food effect, and safety of oral ibuprofen sustained-release capsules by two sponsors in healthy volunteers (HVs). METHODS: Two separate randomized, open-label, single-dose, crossover-design studies were conducted: a fasting study (n = 24) and a fed study (n = 24). In each study, HVs were 1:1 divided into two groups (T-R and R-T) and received 0.3-g/capsule ibuprofen with a 3-day washout. The plasma was collected for up to 24 hours at the time point after dosing on Day 1/Day 4. The plasma concentrations of ibuprofen were measured using an HPLC-MS/MS method, and PK parameters were determined by noncompartmental methods. RESULTS: Forty-eight healthy volunteers were enrolled. In fasting subjects, the maximum plasma concentration (C(max), mean ± SD) was 14.86±3.19 μg/mL at 5.0 (4.0, 7.0) hours (median [min, max]) for sponsor T, and 13.88±2.60 μg/mL at 4.5 (3.0, 8.0) hours for sponsor R. In fed subjects, C(max) was 21.31±4.08 μg/mL at 5.6 (4.3, 10.0) hours for sponsor T, and 19.77±3.36 μg/mL at 6.0 (2.0, 8.0) hours for sponsor R. All 90% confidence intervals (CIs) for C(max), AUC(0-t), and AUC(0-∞) were within the bioequivalence bounds (80–125%) both fasting and fed studies. CONCLUSION: Ibuprofen is well tolerated and has a favorable safety profile. In both fasting and fed study, there were no serious AEs, or AEs leading to withdrawal. Bioequivalence is achieved under fasting and fed conditions, supporting the demonstration of biosimilarity. |
format | Online Article Text |
id | pubmed-10295470 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2023 |
publisher | Dove |
record_format | MEDLINE/PubMed |
spelling | pubmed-102954702023-06-28 Evaluation of Pharmacokinetics and Safety with Bioequivalence of Ibuprofen Sustained-Release Capsules of Two Formulations, in Chinese Healthy Volunteers: Bioequivalence Study Huang, Chunqi Yin, Zhou Yang, Yeqing Mo, Nan Yang, Hui Wang, Ying Drug Des Devel Ther Clinical Trial Report PURPOSE: Ibuprofen is the first of the nonsteroidal anti-inflammatory drug (NSAID) to be used in the clinic. Our aim was to explore the pharmacokinetics (PK), bioequivalence, food effect, and safety of oral ibuprofen sustained-release capsules by two sponsors in healthy volunteers (HVs). METHODS: Two separate randomized, open-label, single-dose, crossover-design studies were conducted: a fasting study (n = 24) and a fed study (n = 24). In each study, HVs were 1:1 divided into two groups (T-R and R-T) and received 0.3-g/capsule ibuprofen with a 3-day washout. The plasma was collected for up to 24 hours at the time point after dosing on Day 1/Day 4. The plasma concentrations of ibuprofen were measured using an HPLC-MS/MS method, and PK parameters were determined by noncompartmental methods. RESULTS: Forty-eight healthy volunteers were enrolled. In fasting subjects, the maximum plasma concentration (C(max), mean ± SD) was 14.86±3.19 μg/mL at 5.0 (4.0, 7.0) hours (median [min, max]) for sponsor T, and 13.88±2.60 μg/mL at 4.5 (3.0, 8.0) hours for sponsor R. In fed subjects, C(max) was 21.31±4.08 μg/mL at 5.6 (4.3, 10.0) hours for sponsor T, and 19.77±3.36 μg/mL at 6.0 (2.0, 8.0) hours for sponsor R. All 90% confidence intervals (CIs) for C(max), AUC(0-t), and AUC(0-∞) were within the bioequivalence bounds (80–125%) both fasting and fed studies. CONCLUSION: Ibuprofen is well tolerated and has a favorable safety profile. In both fasting and fed study, there were no serious AEs, or AEs leading to withdrawal. Bioequivalence is achieved under fasting and fed conditions, supporting the demonstration of biosimilarity. Dove 2023-06-23 /pmc/articles/PMC10295470/ /pubmed/37384214 http://dx.doi.org/10.2147/DDDT.S404756 Text en © 2023 Huang et al. https://creativecommons.org/licenses/by-nc/3.0/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/ (https://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. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms (https://www.dovepress.com/terms.php). |
spellingShingle | Clinical Trial Report Huang, Chunqi Yin, Zhou Yang, Yeqing Mo, Nan Yang, Hui Wang, Ying Evaluation of Pharmacokinetics and Safety with Bioequivalence of Ibuprofen Sustained-Release Capsules of Two Formulations, in Chinese Healthy Volunteers: Bioequivalence Study |
title | Evaluation of Pharmacokinetics and Safety with Bioequivalence of Ibuprofen Sustained-Release Capsules of Two Formulations, in Chinese Healthy Volunteers: Bioequivalence Study |
title_full | Evaluation of Pharmacokinetics and Safety with Bioequivalence of Ibuprofen Sustained-Release Capsules of Two Formulations, in Chinese Healthy Volunteers: Bioequivalence Study |
title_fullStr | Evaluation of Pharmacokinetics and Safety with Bioequivalence of Ibuprofen Sustained-Release Capsules of Two Formulations, in Chinese Healthy Volunteers: Bioequivalence Study |
title_full_unstemmed | Evaluation of Pharmacokinetics and Safety with Bioequivalence of Ibuprofen Sustained-Release Capsules of Two Formulations, in Chinese Healthy Volunteers: Bioequivalence Study |
title_short | Evaluation of Pharmacokinetics and Safety with Bioequivalence of Ibuprofen Sustained-Release Capsules of Two Formulations, in Chinese Healthy Volunteers: Bioequivalence Study |
title_sort | evaluation of pharmacokinetics and safety with bioequivalence of ibuprofen sustained-release capsules of two formulations, in chinese healthy volunteers: bioequivalence study |
topic | Clinical Trial Report |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10295470/ https://www.ncbi.nlm.nih.gov/pubmed/37384214 http://dx.doi.org/10.2147/DDDT.S404756 |
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