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Pharmacokinetics and Bioequivalence of Rasagiline Tablets in Chinese Healthy Subjects Under Fasting and Fed Conditions: An Open, Randomized, Single-Dose, Double-Cycle, Two-Sequence, Crossover Trial
Objective: This study evaluated the pharmacokinetics, safety, and bioequivalence (BE) of two formulations of rasagiline tablets in healthy Chinese subjects under fasting and fed conditions. Methods: An open, randomized, single-dose, double-cycle, two-sequence, self-crossover pharmacokinetic study in...
Autores principales: | , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Frontiers Media S.A.
2020
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7750811/ https://www.ncbi.nlm.nih.gov/pubmed/33364947 http://dx.doi.org/10.3389/fphar.2020.571747 |
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author | Li, Yinjuan Qi, Lu Bai, Haihong Liu, Ying Fan, Rongxia Tu, Yongrui Sun, Yongqiang Wang, Juxiang Qi, Qi Feng, Xiaohui Zhou, Da Wang, Xinghe |
author_facet | Li, Yinjuan Qi, Lu Bai, Haihong Liu, Ying Fan, Rongxia Tu, Yongrui Sun, Yongqiang Wang, Juxiang Qi, Qi Feng, Xiaohui Zhou, Da Wang, Xinghe |
author_sort | Li, Yinjuan |
collection | PubMed |
description | Objective: This study evaluated the pharmacokinetics, safety, and bioequivalence (BE) of two formulations of rasagiline tablets in healthy Chinese subjects under fasting and fed conditions. Methods: An open, randomized, single-dose, double-cycle, two-sequence, self-crossover pharmacokinetic study in healthy Chinese subjects under fasting and high-fat postprandial conditions was performed. A total of 108 healthy subjects (36 in the fasting group and 72 in the postprandial group) were recruited. In each cycle of the study under both conditions, subjects received a single oral dose of 1 mg of a test or reference preparation of rasagiline tablets (1 mg each). A washout period of 3 days was observed. Blood samples were obtained up to 10 h post-intake. Primary endpoints were the BE of major pharmacokinetic parameters (AUC(0–t) and AUC(0–∞)) and the maximum observed serum concentration (C(max)). Secondary endpoints were safety parameters. Results: The 90% confidence interval (CI) of the geometric mean ratio (GMR) of the test drug vs. the reference drug for rasagiline was 94.16–105.35% for the AUC(0–t) under fasting conditions and 99.88–107.07% under postprandial conditions. The 90% CIs for the AUC(0–∞) were 93.55–105.01% and 99.59–107.05% under fasting and postprandial conditions, respectively. The 90% CIs for the C(max) were 88.26–108.46% and 89.54–118.23% under fasting and postprandial conditions, respectively. The 90% CIs for the test/reference AUC ratio and C(max) ratio were within the acceptable range (0.80–1.25) for BE. In this BE study, there were no serious adverse events (AEs). Conclusion: BE between the test and the reference products was established in both fasting and postprandial conditions. The two formulations of rasagiline showed good tolerability and a similar safety profile. Clinical Trial Registration: chinaDrugtrials.org.cn, identifier CTR20181466. |
format | Online Article Text |
id | pubmed-7750811 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | Frontiers Media S.A. |
record_format | MEDLINE/PubMed |
spelling | pubmed-77508112020-12-22 Pharmacokinetics and Bioequivalence of Rasagiline Tablets in Chinese Healthy Subjects Under Fasting and Fed Conditions: An Open, Randomized, Single-Dose, Double-Cycle, Two-Sequence, Crossover Trial Li, Yinjuan Qi, Lu Bai, Haihong Liu, Ying Fan, Rongxia Tu, Yongrui Sun, Yongqiang Wang, Juxiang Qi, Qi Feng, Xiaohui Zhou, Da Wang, Xinghe Front Pharmacol Clinical Trial Objective: This study evaluated the pharmacokinetics, safety, and bioequivalence (BE) of two formulations of rasagiline tablets in healthy Chinese subjects under fasting and fed conditions. Methods: An open, randomized, single-dose, double-cycle, two-sequence, self-crossover pharmacokinetic study in healthy Chinese subjects under fasting and high-fat postprandial conditions was performed. A total of 108 healthy subjects (36 in the fasting group and 72 in the postprandial group) were recruited. In each cycle of the study under both conditions, subjects received a single oral dose of 1 mg of a test or reference preparation of rasagiline tablets (1 mg each). A washout period of 3 days was observed. Blood samples were obtained up to 10 h post-intake. Primary endpoints were the BE of major pharmacokinetic parameters (AUC(0–t) and AUC(0–∞)) and the maximum observed serum concentration (C(max)). Secondary endpoints were safety parameters. Results: The 90% confidence interval (CI) of the geometric mean ratio (GMR) of the test drug vs. the reference drug for rasagiline was 94.16–105.35% for the AUC(0–t) under fasting conditions and 99.88–107.07% under postprandial conditions. The 90% CIs for the AUC(0–∞) were 93.55–105.01% and 99.59–107.05% under fasting and postprandial conditions, respectively. The 90% CIs for the C(max) were 88.26–108.46% and 89.54–118.23% under fasting and postprandial conditions, respectively. The 90% CIs for the test/reference AUC ratio and C(max) ratio were within the acceptable range (0.80–1.25) for BE. In this BE study, there were no serious adverse events (AEs). Conclusion: BE between the test and the reference products was established in both fasting and postprandial conditions. The two formulations of rasagiline showed good tolerability and a similar safety profile. Clinical Trial Registration: chinaDrugtrials.org.cn, identifier CTR20181466. Frontiers Media S.A. 2020-12-03 /pmc/articles/PMC7750811/ /pubmed/33364947 http://dx.doi.org/10.3389/fphar.2020.571747 Text en Copyright © 2020 Li, Qi, Bai, Liu, Fan, Tu, Sun, Wang, Qi, Feng, Zhou and Wang http://creativecommons.org/licenses/by/4.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms. |
spellingShingle | Clinical Trial Li, Yinjuan Qi, Lu Bai, Haihong Liu, Ying Fan, Rongxia Tu, Yongrui Sun, Yongqiang Wang, Juxiang Qi, Qi Feng, Xiaohui Zhou, Da Wang, Xinghe Pharmacokinetics and Bioequivalence of Rasagiline Tablets in Chinese Healthy Subjects Under Fasting and Fed Conditions: An Open, Randomized, Single-Dose, Double-Cycle, Two-Sequence, Crossover Trial |
title | Pharmacokinetics and Bioequivalence of Rasagiline Tablets in Chinese Healthy Subjects Under Fasting and Fed Conditions: An Open, Randomized, Single-Dose, Double-Cycle, Two-Sequence, Crossover Trial |
title_full | Pharmacokinetics and Bioequivalence of Rasagiline Tablets in Chinese Healthy Subjects Under Fasting and Fed Conditions: An Open, Randomized, Single-Dose, Double-Cycle, Two-Sequence, Crossover Trial |
title_fullStr | Pharmacokinetics and Bioequivalence of Rasagiline Tablets in Chinese Healthy Subjects Under Fasting and Fed Conditions: An Open, Randomized, Single-Dose, Double-Cycle, Two-Sequence, Crossover Trial |
title_full_unstemmed | Pharmacokinetics and Bioequivalence of Rasagiline Tablets in Chinese Healthy Subjects Under Fasting and Fed Conditions: An Open, Randomized, Single-Dose, Double-Cycle, Two-Sequence, Crossover Trial |
title_short | Pharmacokinetics and Bioequivalence of Rasagiline Tablets in Chinese Healthy Subjects Under Fasting and Fed Conditions: An Open, Randomized, Single-Dose, Double-Cycle, Two-Sequence, Crossover Trial |
title_sort | pharmacokinetics and bioequivalence of rasagiline tablets in chinese healthy subjects under fasting and fed conditions: an open, randomized, single-dose, double-cycle, two-sequence, crossover trial |
topic | Clinical Trial |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7750811/ https://www.ncbi.nlm.nih.gov/pubmed/33364947 http://dx.doi.org/10.3389/fphar.2020.571747 |
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