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In Vitro Bioavailability Study of an Antiviral Compound Enisamium Iodide

An investigation into the biopharmaceutics classification and a study of the in vitro bioavailability (permeability and solubility) of the antiviral compound enisamium iodide (4-(benzylcarbamoyl)-1-methylpyridinium iodide) were carried out. The solubility of enisamium iodide was determined in four d...

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Autores principales: Haltner-Ukomadu, Eleonore, Gureyeva, Svitlana, Burmaka, Oleksii, Goy, Andriy, Mueller, Lutz, Kostyuk, Grygorii, Margitich, Victor
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5874533/
https://www.ncbi.nlm.nih.gov/pubmed/29324660
http://dx.doi.org/10.3390/scipharm86010003
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author Haltner-Ukomadu, Eleonore
Gureyeva, Svitlana
Burmaka, Oleksii
Goy, Andriy
Mueller, Lutz
Kostyuk, Grygorii
Margitich, Victor
author_facet Haltner-Ukomadu, Eleonore
Gureyeva, Svitlana
Burmaka, Oleksii
Goy, Andriy
Mueller, Lutz
Kostyuk, Grygorii
Margitich, Victor
author_sort Haltner-Ukomadu, Eleonore
collection PubMed
description An investigation into the biopharmaceutics classification and a study of the in vitro bioavailability (permeability and solubility) of the antiviral compound enisamium iodide (4-(benzylcarbamoyl)-1-methylpyridinium iodide) were carried out. The solubility of enisamium iodide was determined in four different buffers. Apparent intestinal permeability (P(app)) of enisamium iodide was assessed using human colon carcinoma (Caco-2) cells at three concentrations. The solubility of enisamium iodide in four buffer solutions from pH 1.2 to 7.5 is about 60 mg/mL at 25 °C, and ranges from 130 to 150 mg/mL at 37 °C, depending on the pH. Based on these results, enisamium iodide can be classified as highly soluble. Enisamium iodide demonstrated low permeability in Caco-2 experiments in all tested concentrations of 10–100 μM with permeability coefficients between 0.2 × 10(−6) cm s(−1) and 0.3 × 10(−6) cm s(−1). These results indicate that enisamium iodide belongs to class III of the Biopharmaceutics Classification System (BCS) due to its high solubility and low permeability. The bioavailability of enisamium iodide needs to be confirmed in animal and human studies.
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spelling pubmed-58745332018-03-30 In Vitro Bioavailability Study of an Antiviral Compound Enisamium Iodide Haltner-Ukomadu, Eleonore Gureyeva, Svitlana Burmaka, Oleksii Goy, Andriy Mueller, Lutz Kostyuk, Grygorii Margitich, Victor Sci Pharm Article An investigation into the biopharmaceutics classification and a study of the in vitro bioavailability (permeability and solubility) of the antiviral compound enisamium iodide (4-(benzylcarbamoyl)-1-methylpyridinium iodide) were carried out. The solubility of enisamium iodide was determined in four different buffers. Apparent intestinal permeability (P(app)) of enisamium iodide was assessed using human colon carcinoma (Caco-2) cells at three concentrations. The solubility of enisamium iodide in four buffer solutions from pH 1.2 to 7.5 is about 60 mg/mL at 25 °C, and ranges from 130 to 150 mg/mL at 37 °C, depending on the pH. Based on these results, enisamium iodide can be classified as highly soluble. Enisamium iodide demonstrated low permeability in Caco-2 experiments in all tested concentrations of 10–100 μM with permeability coefficients between 0.2 × 10(−6) cm s(−1) and 0.3 × 10(−6) cm s(−1). These results indicate that enisamium iodide belongs to class III of the Biopharmaceutics Classification System (BCS) due to its high solubility and low permeability. The bioavailability of enisamium iodide needs to be confirmed in animal and human studies. MDPI 2018-01-11 2018 /pmc/articles/PMC5874533/ /pubmed/29324660 http://dx.doi.org/10.3390/scipharm86010003 Text en © 2018 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Haltner-Ukomadu, Eleonore
Gureyeva, Svitlana
Burmaka, Oleksii
Goy, Andriy
Mueller, Lutz
Kostyuk, Grygorii
Margitich, Victor
In Vitro Bioavailability Study of an Antiviral Compound Enisamium Iodide
title In Vitro Bioavailability Study of an Antiviral Compound Enisamium Iodide
title_full In Vitro Bioavailability Study of an Antiviral Compound Enisamium Iodide
title_fullStr In Vitro Bioavailability Study of an Antiviral Compound Enisamium Iodide
title_full_unstemmed In Vitro Bioavailability Study of an Antiviral Compound Enisamium Iodide
title_short In Vitro Bioavailability Study of an Antiviral Compound Enisamium Iodide
title_sort in vitro bioavailability study of an antiviral compound enisamium iodide
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5874533/
https://www.ncbi.nlm.nih.gov/pubmed/29324660
http://dx.doi.org/10.3390/scipharm86010003
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