Year-end Sale % OFF 
Abstract
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.
Highlights
Influenza is an acute respiratory illness caused by influenza A and B viruses
The results provide no evidence for active transport of enisamium iodide and indicate dose linearity during the transport experiments
The solubility found for enisamium iodide indicates that amounts of at least 31.8 g can be dissolved in 250 mL of buffer solution at 37 °C
Summary
Influenza is an acute respiratory illness caused by influenza A and B viruses. A single class of antiviral drugs—neuraminidase inhibitors: oseltamivir, zanamivir and peramivir—is currently recommended for treatment of influenza in adults and children. The shortage of antiviral medicines for the treatment of influenza dictates the need to develop new compounds that act on targets other than neuraminidase viral proteins. Enisamium iodide (IUPAC NAME: 4-(benzylcarbamoyl)-1-methylpyridinium iodide (molecular formula: C14 H15 IN2 O)) (see Figure 1), a derivative of isonicotinic acid, was demonstrated to exhibit antiviral effects in vitro [1] and in vivo [2] against influenza H1N1, H3N2 and type B viruses.
Sign-in/Register to view highlights & summary Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
