The study of the dose-dependent antiexudative effect of a new anti-inflammatory nasal spray




acute rhinosinusitis, Enisamium iodide nasal spray, Ibuprofen, anti-inflammatory activity, dose-dependent effect


It is possible to assume that intranasal forms of drugs with the anti-inflammatory effect (AIE) can be effective for the pathogenic therapy of acute rhinosinusitis (ARS) to relieve nasal congestion.

Aim. To determine AIE of Enisamium iodide (EI), assess the dose dependence of the effect, and substantiate the choice of the concentration for the active substance of EI in the form of a nasal spray for external use.

Materials and methods. Enisamium iodide nasal spray – “Amizon” manufactured by JSC Farmak (Ukraine) was used in different concentrations extracutaneously. As a reference drug Ibuprofen – “Nurofen”, film-coated tablets, 200 mg, was used intragastrically in the dose of 48 mg/kg. The primary screening for the study of EI antiexudative action in three concentrations was conducted on the carrageenan-induced acute inflammatory model in rats. The anti-inflammatory activity (AIA) of EI in the concentrations of 5, 10 and 20 mg/ml was assessed in three hours compared to Ibuprofen.

Results. EI in all studied concentrations had a statistically significant anti-inflammatory activity of various degrees with a non-linear character in the route of administration studied and the concentration range selected. Therefore, the choice of the most optimal concentration of EI (nasal spray) was on the basis of the comparative analysis of AIA of the drug test samples studied. The most pronounced AIA (35.3 %) was in the EI concentration of 10 mg/ml. This concentration is recommended for further preclinical studies.

Conclusions. The study of AIA of Enisanium iodide (nasal spray) in the range of concentrations of 5, 10 and 20 mg/ml has shown the “activity-concentration” non-linear dependence. The most pronounced AIA is in the EI concentration of 10 mg/ml. Enisamium iodide (nasal spray) is a promising drug for further preclinical studies.

Author Biographies

T. S. Zhulay, National University of Pharmacy

teaching assistant of the Department of Clinical Pharmacology and Clinical Pharmacy

S. K. Shebeko, National University of Pharmacy

Candidate of Pharmacy (Ph.D.), associate professor of the Clinical Pharmacology and Clinical Pharmacy Department

I. A. Zupanets, National University of Pharmacy

Doctor of Medicine (Dr. habil.), professor, head of the Clinical Pharmacology and Clinical Pharmacy Department


Fokkens, W. J., Lund, V. J., Mullol, J. et al. (2012). EPOS 2012: European position paper on rhinosinusitis and nasal polyps 2012. Asummary for otorhinolaryngologists. Rhinology, 50 (1), 1–12.

Chow, A. W., Benninger, M. S., Brook, I. et al. (2012). Infectious Diseases Society of IDSA clinical practice guideline for acute bacterial rhinosinusitis in children and adults. Clin. Infect. Dis.,54 (8), e72–e112.

Nakaz MOZ Ukrainy №85 vid 11.02.2016. Unifikovanyi klinichnyi protokol pervynnoi, vtorynnoi (spetsializovanoi) ta tretynnoi (vysokospetsializovanoi) medychnoi dopomohy. Hostryi rynosynusyt. Kyiv: MOZ Ukrainy.

4. Nakaz MOZ Ukrainy №921 vid 16.11.2012. Instruktsiia dlia medychnoho zastosuvannia preparatu «Amizon®». Available at: 31489

Kovalenko, V. N. (2016). Kompendium 2016 – lekarstvennye preparaty. K.: Morion, 2416.

Sigidin, Ya. A., Shvartc, G. Ya., Arzamastcev, A. P., Liberman, S. S. (1988). Lekarstvennaia terapiia vospalitelnogo protcessa: eksperimentalnaia i klinicheskaia farmakologiia protivovospalitelnykh preparatov. Moscow: Meditcina, 240.

Nakaz MOZ Ukrainy № 461 vid 22.06.2012. Instruktsiia dlia medychnoho zastosuvannia preparatu «Nurofen». Available at:

Stefanov, A. V. (2002). Doklinicheskie issledovaniia lekarstvennykh sredstv. Kiev: Avitcenna, 528.

Kozhemiakin, Yu. M., Khromov, O. S., Filonenko, M. A., Saifetdinova, H. A. (2002). Naukovo–praktychni rekomendatsii z utrymannia laboratornykh tvaryn ta roboty z nymy. Kyiv: Derzhavnyi farmakolohichnyi tsentr MOZ Ukrainy, 155.

Guide for the care and use of laboratory animals, 8th edition. (2011).Washington: The National Academies Press, 246.

Sharp, P., Villano, J. S. (2012). The laboratory rat, 2nd edition. CRC Press, 399.

European convention for the protection of vertebrate animals used for experimental and other scientific purpose : Council of Europe. (1986).Strasbourg, 52.

Good Laboratory Practice (2005). OECD principles and guidance for compliance monitoring. OECD.

Zakon Ukrainy №3447–IV vid 21.02.2006 r. zi zminamy. Pro zakhyst tvaryn vid zhorstokoho povodzhennia. Available at:–iv–3976

Lapach, S. N., Chubenko, A. V., Babych, P. N. (2000). Statisticheskie metody v medikobiologicheskikh issledovaniiakh s ispolzovaniem Excel.Kiev: Morion, 320.

Prozorovskii, V. B. (2007). Psikhofarmakologiia i biologicheskaia narkologiia, 7 (3–4), 2090–2120.





Pre-clinical studies of new drugs