Comprehensive studies for development of galenicals with antimicrobial activity from hypericum perforatum L. Herb

This article describes the development galenicals with antimicrobial activity from Hypericum perforatum L. herb. Based on the working hypotheses, we developed a mathematical model. Its adequacy was verified experimentally, and it was noted that the working hypotheses suggested were not disapproved. Carrying out microbiological studies, we found that the maximum level of ethanol-water extract’s antimicrobial activity was observed in the samples obtained with ethanol 72 and 97 % v/v. It was determined that the level of antimicrobial activity of ethanol-water extracts (1:5 w/v) with ethanol 72 and 97 % v/v was equal to that of reference drug «Chlorhexidine bigluconate water solution 0.05 %». It was found that using the filtration method of extraction for one hour, it is possible to obtain the liquid extract (1:1 w/v) with the concentration of dry residue that equals 13.0 ± 0.7 w/v, and in two hours, we can obtain the tincture (1:5 w/o) with the yield of main biologically active substances more than 90 %. The comprehensive studies conducted increase theoretical knowledge in the field of development of galenicals with antimicrobial activity from Hypericum perforatum L. herb. © 2019, Folium Ltd. All rights reserved

Разработка галеновых препаратов с антимикробной активностью из травы зверобоя продырявленного

This article describes the development galenicals with antimicrobial activity from Hypericum perforatum L. herb. Based on the working hypotheses, we developed a mathematical model. Its adequacy was verified experimentally, and it was noted that the working hypotheses suggested were not disapproved. Carrying out microbiological studies, we found that the maximum level of ethanol-water extract’s antimicrobial activity was observed in the samples obtained with ethanol 72 and 97 % v/v. It was determined that the level of antimicrobial activity of ethanol-water extracts (1:5 w/v) with ethanol 72 and 97 % v/v was equal to that of reference drug «Chlorhexidine bigluconate water solution 0.05 %». It was found that using the filtration method of extraction for one hour, it is possible to obtain the liquid extract (1:1 w/v) with the concentration of dry residue that equals 13.0 ± 0.7 w/v, and in two hours, we can obtain the tincture (1:5 w/o) with the yield of main biologically active substances more than 90 %. The comprehensive studies conducted increase theoretical knowledge in the field of development of galenicals with antimicrobial activity from Hypericum perforatum L. herb.Описаны комплексные исследования в области разработки галеновых препаратов с антимикробной активностью из травы зверобоя продырявленного. Обнаружено, что максимальный уровень антимикробной активности спиртоводных извлечений наблюдается у тех образцов, которые были получены при использовании этанола с концентрацией 72 и 97 об.% Уровень антимикробной активности спиртоводных извлечений (1:5 м/о) не уступает уровню активности препарата сравнения «Хлоргексидин биглюконат водный раствор 0,05 %». С помощью метода фильтрационной экстракции в течение 1 ч можно получить жидкий экстракт (1:1 м/о) с концентрацией сухого остатка 13,0 ± 0,7 % м/о, а за 2 ч можно получить настойку (1:5 м/о) с выходом основных БАВ более 90 %

Исследования в области разработки галенового препарата с антимикробной активностью из бутонов гвоздики

The article presents the results of studies on the development of a galenical drug with antimicrobial activity from clove buds. For studies, we used grinded clove buds with particles fraction less than 0.5 mm. As an extractant, we used ethanol with different concentration 26, 43, 56, 72, 82, 97±1% v/v. Methods of extraction: simple maceration and filtration extraction. Methods of analyses: RP HPLC and gravimetry. Standard substances were eugenol and gallic acid. Analytical wave lengths were 370, 282, and 270 nm. For the antibacterial study of extracts, we used the agar well diffusion method. In our research, we used six test-strain microorganisms: Escherichia coli ATCC 25922, Staphylococcus aureus ATCC 25923, Proteus vulgaris ATCC 4636, Pseudomonas aeruginosa ATCC 27853, Candida albicans ATCC 885/653, and Bacillus subtilis ATCC 6633. Ethanol concentration, which extracts most of the substances was found; minimal eugenol concentration in the extract and tincture for their standardizations was suggested; the level of antimicrobial activity of ethanol-water extracts equivalent to a reference drug was determined. It was found that the major yield among the substances determined is observed with an ethanol concentration of 80±5% v/v. It was found that using filtration extraction method for one hour of the extraction process, we could obtain the liquid extract 1:1 m/v with eugenol concentration of 13.8% m/v and its yield 93%. In two and a half hours of the extraction process, we could obtain the tincture 1:5 m/v with eugenol concentration of 3.0% m/v and its yield 100%. RP HPLC method of analysis determined the presence of the following nine main substances: eugenol, acetyl eugenol, gallic acid, three flavonoids, and three non-identified substances in ethanol-water extracts from clove buds. It was suggested to carry out standardization of the resulting galenical drugs by eugenol. For the extract (1:1 m/v), low limit of eugenol concentration 13.0% m/v was suggested, and for the tincture (1:10 m/v), low limit of eugenol concentration 1.3% m/v was suggested. Antimicrobial activity of ethanol-water solutions of the extract (1:1 m/v) was studied; the lowest eugenol concentration of 0.44% m/v in ethanol-water solutions equivalent in terms of its antimicrobial activity to the reference drug 0.05% chlorhexidine digluconate water solution.Цель исследований - разработка галенового препарата с антимикробной активностью из бутонов гвоздики. Материалом служили измельченные бутоны гвоздики с фракцией частиц менее 0,5 мм. В качестве экстрагента использовали этиловый спирт различной концентрации 26, 43, 56, 72, 82, 97±1 % об. Методы экстракции: простая мацерация и фильтрационная экстракция. Методы анализа: ОФ ВЭЖХ, гравиметрия. Вещество-стандарт - эвгенол, галловая кислота. Применение метода ОФ ВЭЖХ анализа показало присутствие в спиртоводных извлечениях из бутонов гвоздики девяти основных веществ, среди которых были идентифицированы: эвгенол, ацетилэвгенол, галловая кислота, флавоноиды и два не идентифицированных соединения. Стандартизацию суммарных препаратов предложено проводить по эвгенолу. Для экстракта (1:1 м/о) рекомендован нижний предел концентрации эвгенола 13,0% м/о, для настойки (1:10 м/о) рекомендован нижний предел концентрации эвгенола 1,3% м/о. Изучена антимикробная активность спиртоводных растворов на основе экстракта (1:1 м/о), выявлена наименьшая концентрация эвгенола 0,44% м/о в спиртоводных растворах, которая эквивалентна препарату сравнения - 0,05%-ного водного раствора хлоргексидина биглюконата

Study of antimicrobial activity and technology optimization of calendulae flos galenicals

The article presents materials on optimization of manufacture technology for Calendulae flos galenicals with medium level of antibacterial activity. For antibacterial study of extracts, we used agar well diffusion method. In our research, we utilized six test-strain microorganisms: E. coli ATCC 25922, S. aureus ATCC 25923, P. vulgaris ATCC 4636, P. aeruginosa ATCC 27853, C. albicans ATCC 885/653, and B. subtilis ATCC 6633. We have found that the maximum level of extracts’ antimicrobial activity is achieved in the range of ethanol content in the extractant from 70 to 97 % v/v. Basing on these results, we have suggested a highly effective filtration technology of extraction for manufacture of liquid extract and tincture with medium level of antimicrobial activity from Calendulae flos. Based on HPLC analysis of extracts we detected the following main groups of compounds: quercetin and caffeic acid of derivatives. We have found that the antimicrobial activity of galenicals have good correlation with dry residue concentration but not with the rutin and chlorogenic acid concentration. © 2019 Boyko et al