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Comparison of pharmacokinetics and safety characteristics between two olopatadine hydrochloride 5 mg tablet formulations in healthy Korean subjects

Histamine acts by binding to four histamine receptors (H1 to H4), of which the H1 is known to participate in dilate blood vessels, bronchoconstriction, and pruritus. Olopatadine hydrochloride blocks the release of histamine from mast cells and it inhibits H1 receptor activation. Olopatadine hydrochl...

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Autores principales: Kim, Jae Hoon, Lee, Minyu, Kim, Namsick, Oh, Tae-Young, Nam, Seung-Kwan, Choi, Yoon Seok, Kwon, In Sun, Jung, Jin Gyu, Hong, Jang Hee
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Korean Society for Clinical Pharmacology and Therapeutics 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8020358/
https://www.ncbi.nlm.nih.gov/pubmed/33855002
http://dx.doi.org/10.12793/tcp.2021.29.e6
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author Kim, Jae Hoon
Lee, Minyu
Kim, Namsick
Oh, Tae-Young
Nam, Seung-Kwan
Choi, Yoon Seok
Kwon, In Sun
Jung, Jin Gyu
Hong, Jang Hee
author_facet Kim, Jae Hoon
Lee, Minyu
Kim, Namsick
Oh, Tae-Young
Nam, Seung-Kwan
Choi, Yoon Seok
Kwon, In Sun
Jung, Jin Gyu
Hong, Jang Hee
author_sort Kim, Jae Hoon
collection PubMed
description Histamine acts by binding to four histamine receptors (H1 to H4), of which the H1 is known to participate in dilate blood vessels, bronchoconstriction, and pruritus. Olopatadine hydrochloride blocks the release of histamine from mast cells and it inhibits H1 receptor activation. Olopatadine hydrochloride is anti-allergic agent that is effectively used. The object of this study had conducted to compare the pharmacokinetics (PKs) and safety characteristics between olopatadine hydrochloride 5 mg (test formulation) and olopatadine hydrochloride 5 mg (reference formulation; Alerac (®)) in Korean subjects. This study had conducted an open-label, randomized, fasting condition, single-dose, 2-treatment, 2-period, 2-way crossover. Subjects received single-dosing of reference formulation or test formulation in each period and blood samples were collected over 24 hours after administration for PK analysis. A wash-out period of 7 days was placed between the doses. Plasma concentration of olopatadine were determined using liquid chromatography-tandem spectrometry mass (LC-MS/MS). A total of 32 subjects were enrolled and 28 subjects completed. There were not clinical significantly different in the safety between two treatment groups for 32 subjects who administered the study drug more than once. The geometric mean ratio of test formulation to reference formulation and its 90% confidence intervals for The peak plasma concentration (C(max)) and the areas under the plasma concentration–time curve from 0 to the last concentration (AUC(last)) were 1.0845 (1.0107–1.1637) and 1.0220 (1.0005–1.0439), respectively. Therefore, the test formulation was bioequivalent in PK characteristics and was equally safe as the reference formulation. TRIAL REGISTRATION: Clinical Research Information Service Identifier: KCT0005943
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spelling pubmed-80203582021-04-13 Comparison of pharmacokinetics and safety characteristics between two olopatadine hydrochloride 5 mg tablet formulations in healthy Korean subjects Kim, Jae Hoon Lee, Minyu Kim, Namsick Oh, Tae-Young Nam, Seung-Kwan Choi, Yoon Seok Kwon, In Sun Jung, Jin Gyu Hong, Jang Hee Transl Clin Pharmacol Original Article Histamine acts by binding to four histamine receptors (H1 to H4), of which the H1 is known to participate in dilate blood vessels, bronchoconstriction, and pruritus. Olopatadine hydrochloride blocks the release of histamine from mast cells and it inhibits H1 receptor activation. Olopatadine hydrochloride is anti-allergic agent that is effectively used. The object of this study had conducted to compare the pharmacokinetics (PKs) and safety characteristics between olopatadine hydrochloride 5 mg (test formulation) and olopatadine hydrochloride 5 mg (reference formulation; Alerac (®)) in Korean subjects. This study had conducted an open-label, randomized, fasting condition, single-dose, 2-treatment, 2-period, 2-way crossover. Subjects received single-dosing of reference formulation or test formulation in each period and blood samples were collected over 24 hours after administration for PK analysis. A wash-out period of 7 days was placed between the doses. Plasma concentration of olopatadine were determined using liquid chromatography-tandem spectrometry mass (LC-MS/MS). A total of 32 subjects were enrolled and 28 subjects completed. There were not clinical significantly different in the safety between two treatment groups for 32 subjects who administered the study drug more than once. The geometric mean ratio of test formulation to reference formulation and its 90% confidence intervals for The peak plasma concentration (C(max)) and the areas under the plasma concentration–time curve from 0 to the last concentration (AUC(last)) were 1.0845 (1.0107–1.1637) and 1.0220 (1.0005–1.0439), respectively. Therefore, the test formulation was bioequivalent in PK characteristics and was equally safe as the reference formulation. TRIAL REGISTRATION: Clinical Research Information Service Identifier: KCT0005943 Korean Society for Clinical Pharmacology and Therapeutics 2021-03 2021-03-23 /pmc/articles/PMC8020358/ /pubmed/33855002 http://dx.doi.org/10.12793/tcp.2021.29.e6 Text en Copyright © 2021 Translational and Clinical Pharmacology https://creativecommons.org/licenses/by-nc/4.0/ It is identical to the Creative Commons Attribution Non-Commercial License (https://creativecommons.org/licenses/by-nc/4.0/).
spellingShingle Original Article
Kim, Jae Hoon
Lee, Minyu
Kim, Namsick
Oh, Tae-Young
Nam, Seung-Kwan
Choi, Yoon Seok
Kwon, In Sun
Jung, Jin Gyu
Hong, Jang Hee
Comparison of pharmacokinetics and safety characteristics between two olopatadine hydrochloride 5 mg tablet formulations in healthy Korean subjects
title Comparison of pharmacokinetics and safety characteristics between two olopatadine hydrochloride 5 mg tablet formulations in healthy Korean subjects
title_full Comparison of pharmacokinetics and safety characteristics between two olopatadine hydrochloride 5 mg tablet formulations in healthy Korean subjects
title_fullStr Comparison of pharmacokinetics and safety characteristics between two olopatadine hydrochloride 5 mg tablet formulations in healthy Korean subjects
title_full_unstemmed Comparison of pharmacokinetics and safety characteristics between two olopatadine hydrochloride 5 mg tablet formulations in healthy Korean subjects
title_short Comparison of pharmacokinetics and safety characteristics between two olopatadine hydrochloride 5 mg tablet formulations in healthy Korean subjects
title_sort comparison of pharmacokinetics and safety characteristics between two olopatadine hydrochloride 5 mg tablet formulations in healthy korean subjects
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8020358/
https://www.ncbi.nlm.nih.gov/pubmed/33855002
http://dx.doi.org/10.12793/tcp.2021.29.e6
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