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Bioequivalence of two esomeprazole magnesium enteric-coated formulations in healthy Chinese subjects
BACKGROUND: The pharmacokinetics and bioequivalence of esomeprazole in healthy Chinese subjects and the effects of food on the pharmacokinetics have not been well studied. AIM: To evaluate the pharmacokinetic characteristics of esomeprazole magnesium (Eso) enteric- coated capsule in the healthy subj...
Autores principales: | , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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Baishideng Publishing Group Inc
2020
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7716327/ https://www.ncbi.nlm.nih.gov/pubmed/33344542 http://dx.doi.org/10.12998/wjcc.v8.i22.5518 |
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author | Liu, Zheng-Zhi Ren, Qing Zhou, Yan-Nan Yang, Hai-Miao |
author_facet | Liu, Zheng-Zhi Ren, Qing Zhou, Yan-Nan Yang, Hai-Miao |
author_sort | Liu, Zheng-Zhi |
collection | PubMed |
description | BACKGROUND: The pharmacokinetics and bioequivalence of esomeprazole in healthy Chinese subjects and the effects of food on the pharmacokinetics have not been well studied. AIM: To evaluate the pharmacokinetic characteristics of esomeprazole magnesium (Eso) enteric- coated capsule in the healthy subjects in China and the bioequivalence of the two formulations. METHODS: This study was conducted in the Phase I Clinical Trial Unit of the Affiliated Hospital of Changchun University of Chinese Medicine. A total of 64 healthy subjects were enrolled in the study. Thirty-two subjects fasted or fed, took the test or reference formulation Eso enteric-coated capsule by a four-cycle, two-sequence crossover of fasting/fed, self-controlled method. The liquid chromatography-mass spectrometry was performed to determine the drug plasma concentration at 16 different time points within 12 h after drug administration. The pharmacokinetic parameters C(max), area under the curve (AUC)(0-t), and AUC(0-inf) were calculated to evaluate the bioequivalence. RESULTS: Pharmacokinetic parameters were evaluated after subjects took the test formulation and control formulation under fasting status. The ratio of geometric means of C(max) was 104.15%, with a confidence interval (CI) of 98.20-110.46%. The ratio of geometric means of AUC(0-t) was 105.26%, with a CI of 99.80-111.01%. The ratio of geometric means of AUC(0-inf) was 105.37%, with a CI of 99.97-111.06%. The pharmacokinetic parameters were also evaluated after subjects took the reference formulation of Eso enteric-coated capsule after eating. The upper limit of 95% CI of the geometric mean ratio of pharmacokinetic parameters of Eso enteric-coated capsules in the postprandial state C(max )was -0.1689, and the point estimate was 0.9509 (0.80-1.25). The upper limit of 95% CI of the geometric mean ratio of pharmacokinetic parameters of Eso enteric-coated capsules in the postprandial state AUC(0-t )was -0.1015 (≤ 0) , and the point estimate was 0.9003 (0.80-1.25). The upper limit of 95% CI of the geometric mean ratio of pharmacokinetic parameters of Eso enteric-coated capsules in the postprandial state AUC(0-inf )was -0.0593 (≤ 0), and the point estimate was 0.8453 (0.80-1.25). The results indicated that the two formulations were bioequivalent under both fasting and fed states. CONCLUSION: The two types of esomeprazole tablets were bioequivalent under both fasting and fed states, and both were generally well tolerated. |
format | Online Article Text |
id | pubmed-7716327 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | Baishideng Publishing Group Inc |
record_format | MEDLINE/PubMed |
spelling | pubmed-77163272020-12-18 Bioequivalence of two esomeprazole magnesium enteric-coated formulations in healthy Chinese subjects Liu, Zheng-Zhi Ren, Qing Zhou, Yan-Nan Yang, Hai-Miao World J Clin Cases Case Control Study BACKGROUND: The pharmacokinetics and bioequivalence of esomeprazole in healthy Chinese subjects and the effects of food on the pharmacokinetics have not been well studied. AIM: To evaluate the pharmacokinetic characteristics of esomeprazole magnesium (Eso) enteric- coated capsule in the healthy subjects in China and the bioequivalence of the two formulations. METHODS: This study was conducted in the Phase I Clinical Trial Unit of the Affiliated Hospital of Changchun University of Chinese Medicine. A total of 64 healthy subjects were enrolled in the study. Thirty-two subjects fasted or fed, took the test or reference formulation Eso enteric-coated capsule by a four-cycle, two-sequence crossover of fasting/fed, self-controlled method. The liquid chromatography-mass spectrometry was performed to determine the drug plasma concentration at 16 different time points within 12 h after drug administration. The pharmacokinetic parameters C(max), area under the curve (AUC)(0-t), and AUC(0-inf) were calculated to evaluate the bioequivalence. RESULTS: Pharmacokinetic parameters were evaluated after subjects took the test formulation and control formulation under fasting status. The ratio of geometric means of C(max) was 104.15%, with a confidence interval (CI) of 98.20-110.46%. The ratio of geometric means of AUC(0-t) was 105.26%, with a CI of 99.80-111.01%. The ratio of geometric means of AUC(0-inf) was 105.37%, with a CI of 99.97-111.06%. The pharmacokinetic parameters were also evaluated after subjects took the reference formulation of Eso enteric-coated capsule after eating. The upper limit of 95% CI of the geometric mean ratio of pharmacokinetic parameters of Eso enteric-coated capsules in the postprandial state C(max )was -0.1689, and the point estimate was 0.9509 (0.80-1.25). The upper limit of 95% CI of the geometric mean ratio of pharmacokinetic parameters of Eso enteric-coated capsules in the postprandial state AUC(0-t )was -0.1015 (≤ 0) , and the point estimate was 0.9003 (0.80-1.25). The upper limit of 95% CI of the geometric mean ratio of pharmacokinetic parameters of Eso enteric-coated capsules in the postprandial state AUC(0-inf )was -0.0593 (≤ 0), and the point estimate was 0.8453 (0.80-1.25). The results indicated that the two formulations were bioequivalent under both fasting and fed states. CONCLUSION: The two types of esomeprazole tablets were bioequivalent under both fasting and fed states, and both were generally well tolerated. Baishideng Publishing Group Inc 2020-11-26 2020-11-26 /pmc/articles/PMC7716327/ /pubmed/33344542 http://dx.doi.org/10.12998/wjcc.v8.i22.5518 Text en ©The Author(s) 2020. Published by Baishideng Publishing Group Inc. All rights reserved. http://creativecommons.org/licenses/by-nc/4.0/ This article is an open-access article which was selected by an in-house editor and fully peer-reviewed by external reviewers. It is distributed in accordance with the Creative Commons Attribution Non Commercial (CC BY-NC 4.0) license, which permits others to distribute, remix, adapt, build upon this work non-commercially, and license their derivative works on different terms, provided the original work is properly cited and the use is non-commercial. |
spellingShingle | Case Control Study Liu, Zheng-Zhi Ren, Qing Zhou, Yan-Nan Yang, Hai-Miao Bioequivalence of two esomeprazole magnesium enteric-coated formulations in healthy Chinese subjects |
title | Bioequivalence of two esomeprazole magnesium enteric-coated formulations in healthy Chinese subjects |
title_full | Bioequivalence of two esomeprazole magnesium enteric-coated formulations in healthy Chinese subjects |
title_fullStr | Bioequivalence of two esomeprazole magnesium enteric-coated formulations in healthy Chinese subjects |
title_full_unstemmed | Bioequivalence of two esomeprazole magnesium enteric-coated formulations in healthy Chinese subjects |
title_short | Bioequivalence of two esomeprazole magnesium enteric-coated formulations in healthy Chinese subjects |
title_sort | bioequivalence of two esomeprazole magnesium enteric-coated formulations in healthy chinese subjects |
topic | Case Control Study |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7716327/ https://www.ncbi.nlm.nih.gov/pubmed/33344542 http://dx.doi.org/10.12998/wjcc.v8.i22.5518 |
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