Abstract

Introduction. Influenza and acute respiratory viral infection (hereinafter – ARVI) are serious diseases that affect up to 500 million people worldwide every year. From 27.3 to 41.2 million people are registered annually in Russia. Thus, the urgent task is to develop new effective drugs aimed at the prevention and treatment of the above diseases. The drug composition for intranasal use based on aminocaproic acid with antiviral activity and a copolymer of N-vinylpyrrolidone and 2-methyl-5-vinylpyridine with a proven immunostimulating action was developed.Aim. Study of the antiviral activity of the complex drug composition with aminocaproic acid and a copolymer of N-vinylpyrrolidone and 2-methyl-5-vinylpyridine.Materials and methods. To reach this goal, preparations with different ratios of active substances were used to identify the best efficacy. The study was conducted in comparison with the known drug zanamivir. Antiviral activity was studied against influenza A/Puerto Rico/8/34 (H1N1) virus in white outbred mice upon nasal administration of the test samples. The activity evaluation of the studied drugs was carried out according to the weight values and the death dynamics control and experimental groups of animals. Infectious activity of the virus in the lung tissue of animals was assessed on day 5 after infection by titration on a culture of MDCK cells in a nutrient medium MEM. Virus titer was expressed in logarithm of 50% of the virus experimental infectious dose (lg TCID50) per 200 μl of medium.Results and discussion. Based on the data obtained during the study of the weight values dynamics and the dynamics of animal death, the drug showed a maximum antiviral activity with a 2:1 ratio of active substances, which is confirmed by the data on viral activity in the lungs of animals, the virus titer was 1.9±0.3 (p=0.616) lg TCID50/0.2 ml.Conclusion. Antiviral activity of the complex preparation based on aminocaproic acid and N-vinylpyrrolidone and 2-methyl-5-vinylpyridine copolymer was studied, the most effective ratio of active substances was found, it is 2:1. Thus this complex preparation with a ratio of active substances 2:1 reduced the viral load level in the lung tissue of infected mice by more than two times relative to the control group. Therefore, this combination of active substances can be used to develop a promising drug for nasal use as treatment and prevention of influenza and ARVI.

Highlights

  • Influenza and acute respiratory viral infection are serious diseases that affect up to 500 million people worldwide every year

  • The drug composition for intranasal use based on aminocaproic acid with antiviral activity and a copolymer of N-vinylpyrrolidone and 2-methyl-5-vinylpyridine with a proven immunostimulating action was developed

  • Based on the data obtained during the study of the weight values dynamics and the dynamics of animal death, the drug showed a maximum antiviral activity with a 2:1 ratio of active substances, which is confirmed by the data on viral activity in the lungs of animals, the virus titer was 1.9±0.3 (p=0.616) lg TCID50/0.2 ml

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Summary

Conclusion

Antiviral activity of the complex preparation based on aminocaproic acid and N-vinylpyrrolidone and 2-methyl-5-vinylpyridine copolymer was studied, the most effective ratio of active substances was found, it is 2:1. Кроме вируса гриппа на сегодняшний день описано более 200 видов респираторных вирусов, таких как аденовирусы, риновирусы, респираторно-синцитиальные вирусы, вызывающих гриппоподобные заболевания у человека. В качестве активных веществ разрабатываемого лекарственного препарата предложены аминокапроновая кислота (далее – АКК) и сополимер N-винилпирролидона и 2-метил-5-винилпиридина (далее – сополимер). Однако известны и ее противовирусные свойства, врачи назначают ее больным в виде раствора для ингаляций во время вирусных заболеваний, а также для профилактики. Таким образом АКК и сополимер являются перспективными веществами для создания на их основе лекарственного препарата для профилактики гриппа и ОРВИ, так как ожидается, что АКК будет проявлять краткосрочный противовирусный эффект, а сополимер будет оказывать общее иммуностимулирующее действие. Объем исследований определялся действующими нормативными документами [7]

МАТЕРИАЛЫ И МЕТОДЫ
Оценка динамики весовых показателей животных
Оценка динамики гибели животных
Findings
Дни исследования
Full Text
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