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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| Format: | Article |
| Language: | English |
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MDPI AG
2018-01-01
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| Series: | Scientia Pharmaceutica |
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| Online Access: | http://www.mdpi.com/2218-0532/86/1/3 |
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| author | Eleonore Haltner-Ukomadu Svitlana Gureyeva Oleksii Burmaka Andriy Goy Lutz Mueller Grygorii Kostyuk Victor Margitich |
| author_facet | Eleonore Haltner-Ukomadu Svitlana Gureyeva Oleksii Burmaka Andriy Goy Lutz Mueller Grygorii Kostyuk Victor Margitich |
| author_sort | Eleonore Haltner-Ukomadu |
| collection | DOAJ |
| 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 (Papp) 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. |
| first_indexed | 2024-04-14T05:27:30Z |
| format | Article |
| id | doaj.art-aa8a88dce0c7441da1070f99cb5751cc |
| institution | Directory Open Access Journal |
| issn | 2218-0532 |
| language | English |
| last_indexed | 2024-04-14T05:27:30Z |
| publishDate | 2018-01-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Scientia Pharmaceutica |
| spelling | doaj.art-aa8a88dce0c7441da1070f99cb5751cc2022-12-22T02:09:55ZengMDPI AGScientia Pharmaceutica2218-05322018-01-01861310.3390/scipharm86010003scipharm86010003In Vitro Bioavailability Study of an Antiviral Compound Enisamium IodideEleonore Haltner-Ukomadu0Svitlana Gureyeva1Oleksii Burmaka2Andriy Goy3Lutz Mueller4Grygorii Kostyuk5Victor Margitich6Across Barriers, Science Park 1, 66123 Saarbruecken, GermanyJoint Stock Company Farmak, 63 Kyrylivska Street, 04080 Kiev, UkraineJoint Stock Company Farmak, 63 Kyrylivska Street, 04080 Kiev, UkraineJoint Stock Company Farmak, 63 Kyrylivska Street, 04080 Kiev, UkraineDr. Regenold GmbH, Zoellinplatz 4, 79410 Badenweiler, GermanyJoint Stock Company Farmak, 63 Kyrylivska Street, 04080 Kiev, UkraineJoint Stock Company Farmak, 63 Kyrylivska Street, 04080 Kiev, UkraineAn 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 (Papp) 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.http://www.mdpi.com/2218-0532/86/1/3bioavailabilitybiopharmaceutics classification systempermeabilitysolubility |
| spellingShingle | Eleonore Haltner-Ukomadu Svitlana Gureyeva Oleksii Burmaka Andriy Goy Lutz Mueller Grygorii Kostyuk Victor Margitich In Vitro Bioavailability Study of an Antiviral Compound Enisamium Iodide Scientia Pharmaceutica bioavailability biopharmaceutics classification system permeability solubility |
| 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 | bioavailability biopharmaceutics classification system permeability solubility |
| url | http://www.mdpi.com/2218-0532/86/1/3 |
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