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<article article-type="research-article" dtd-version="1.3" xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" xml:lang="ru"><front><journal-meta><journal-id journal-id-type="publisher-id">pmedpharm</journal-id><journal-title-group><journal-title xml:lang="ru">Фармация и фармакология</journal-title><trans-title-group xml:lang="en"><trans-title>Pharmacy &amp; Pharmacology</trans-title></trans-title-group></journal-title-group><issn pub-type="ppub">2307-9266</issn><issn pub-type="epub">2413-2241</issn><publisher><publisher-name>Pyatigorsk Medical and Pharmaceutical Institute - branch of Volgograd State Medical Univer</publisher-name></publisher></journal-meta><article-meta><article-id pub-id-type="doi">10.19163/2307-9266-2018-6-4-367-379</article-id><article-id custom-type="elpub" pub-id-type="custom">pmedpharm-315</article-id><article-categories><subj-group subj-group-type="heading"><subject>Research Article</subject></subj-group><subj-group subj-group-type="section-heading" xml:lang="ru"><subject>ФАРМАКОЛОГИЯ И КЛИНИЧЕСКАЯ ФАРМАКОЛОГИЯ</subject></subj-group><subj-group subj-group-type="section-heading" xml:lang="en"><subject>PHARMACOLOGY AND CLINICAL PHARMACOLOGY</subject></subj-group></article-categories><title-group><article-title>ПРОТИВОЯЗВЕННАЯ АКТИВНОСТЬ ДИНИТРАТА  2-ФЕНИЛ-9-ДИЭТИЛАМИНОЭТИЛИМИДАЗО[1,2-А]БЕНЗИМИДАЗОЛА ПРИ ГЕЛИКОБАКТЕРОПОДОБНОМ ПОВРЕЖДЕНИИ СЛИЗИСТОЙ ОБОЛОЧКИ ЖЕЛУДКА</article-title><trans-title-group xml:lang="en"><trans-title>ANTIULCER ACTIVITY OF DINITRATE 2-PHENYL-9DIETHYLAMINOETHYLAMINE[1,2-A]BENZIMIDAZOLE  WITH HELICOBACTER PYLORI-LIKE DAMAGE OF GASTRIC MUCOSA</trans-title></trans-title-group></title-group><contrib-group><contrib contrib-type="author" corresp="yes"><name-alternatives><name name-style="eastern" xml:lang="ru"><surname>Черников</surname><given-names>М. В.</given-names></name><name name-style="western" xml:lang="en"><surname>Chernikov</surname><given-names>M. V.</given-names></name></name-alternatives><bio xml:lang="ru"><p>Черников Максим Валентинович – доктор медицинских наук, доцент, заведующий кафедрой биологии и физиологии.</p><p>357500, Пятигорск, пр. Калинина, 11</p></bio><bio xml:lang="en"><p>Chernikov Maxim Valentinovich –PhD (Medicine), Head of the Department of Biology.</p><p>11, Kalinin ave., Pyatigorsk, 357532</p></bio><email xlink:type="simple">pharmax@list.ru</email><xref ref-type="aff" rid="aff-1"/></contrib><contrib contrib-type="author" corresp="yes"><name-alternatives><name name-style="eastern" xml:lang="ru"><surname>Оганова</surname><given-names>М. А.</given-names></name><name name-style="western" xml:lang="en"><surname>Oganova</surname><given-names>M. A.</given-names></name></name-alternatives><bio xml:lang="ru"><p>Оганова Марина Альбертовна – кандидат фармацевтических наук, доцент кафедры биологии и физиологии.</p><p>357500, Пятигорск, пр. Калинина, 11</p></bio><bio xml:lang="en"><p>Oganova Marina Albertovna – PhD (Pharmacy), Associate Professor of the Department of Biology.</p><p>11, Kalinin ave., Pyatigorsk, 357532</p></bio><email xlink:type="simple">marina-oganova81@mail.ru</email><xref ref-type="aff" rid="aff-1"/></contrib><contrib contrib-type="author" corresp="yes"><name-alternatives><name name-style="eastern" xml:lang="ru"><surname>Герасименко</surname><given-names>А. С.</given-names></name><name name-style="western" xml:lang="en"><surname>Gerasimenko</surname><given-names>A. S.</given-names></name></name-alternatives><bio xml:lang="ru"><p>Герасименко Анна Сергеевна – преподаватель кафедры патологии.</p><p>357500, Пятигорск, пр. Калинина, 11</p></bio><bio xml:lang="en"><p>Gerasimenko Anna Sergeevna – lecturer of the Department of pathology.</p><p>11, Kalinin ave., Pyatigorsk, 357532</p></bio><email xlink:type="simple">ger_ann5@ro.ru</email><xref ref-type="aff" rid="aff-1"/></contrib><contrib contrib-type="author" corresp="yes"><name-alternatives><name name-style="eastern" xml:lang="ru"><surname>Артемьев</surname><given-names>Е. А.</given-names></name><name name-style="western" xml:lang="en"><surname>Artemyev</surname><given-names>E. A.</given-names></name></name-alternatives><bio xml:lang="ru"><p>Артемьев Евгений Альбертович – аспирант кафедры биологии и физиологии, патологии.</p><p>357500, Пятигорск, пр. Калинина, 11</p></bio><bio xml:lang="en"><p>Artemyev Evgeny Albertovich – post-graduate student of the Department of biology and physiology.</p><p>11, Kalinin ave., Pyatigorsk, 357532</p></bio><email xlink:type="simple">johni1001@rambler.ru</email><xref ref-type="aff" rid="aff-1"/></contrib></contrib-group><aff-alternatives id="aff-1"><aff xml:lang="ru"><institution>Пятигорский медико-фармацевтический институт – филиал ФГБОУ ВО ВолгГМУ Минздрава России</institution><country>Россия</country></aff><aff xml:lang="en"><institution>Pyatigorsk Medical and Pharmaceutical Institute – branch of Volgograd State Medical University</institution><country>Russian Federation</country></aff></aff-alternatives><pub-date pub-type="collection"><year>2018</year></pub-date><pub-date pub-type="epub"><day>13</day><month>09</month><year>2018</year></pub-date><volume>6</volume><issue>4</issue><fpage>367</fpage><lpage>379</lpage><permissions><copyright-statement>Copyright &amp;#x00A9; Черников М.В., Оганова М.А., Герасименко А.С., Артемьев Е.А., 2018</copyright-statement><copyright-year>2018</copyright-year><copyright-holder xml:lang="ru">Черников М.В., Оганова М.А., Герасименко А.С., Артемьев Е.А.</copyright-holder><copyright-holder xml:lang="en">Chernikov M.V., Oganova M.A., Gerasimenko A.S., Artemyev E.A.</copyright-holder><license xml:lang="ru" license-type="creative-commons-attribution" xlink:href="https://creativecommons.org/licenses/by/4.0/" xlink:type="simple"><license-p>Данная работа распространяется под лицензией Creative Commons Attribution 4.0.</license-p></license><license xml:lang="en" license-type="creative-commons-attribution" xlink:href="https://creativecommons.org/licenses/by/4.0/" xlink:type="simple"><license-p>This work is licensed under a Creative Commons Attribution 4.0 License.</license-p></license></permissions><self-uri xlink:href="https://www.pharmpharm.ru/jour/article/view/315">https://www.pharmpharm.ru/jour/article/view/315</self-uri><abstract><p>Поиск новых лекарственных средств, обеспечивающих эффективную и безопасную терапию кислотозависимых заболеваний желудочно-кишечного тракта, продолжает оставаться актуальной проблемой современной фармакотерапии. Одним из наиболее значимых патогенетических механизмов развития данных заболеваний является, ассоциированное с Helicobacter pylori, повреждение слизистой оболочки желудка.</p><p>Целью данного исследования явилось экспериментальное изучение противоязвенной активности субстанции 2-фенил-9-диэтиламиноэтилимидазо [1,2-а] бензимидазола (далее субстанция, производное бензимидазола) на модели геликобактероподобного повреждения слизистой желудка в сочетании с иммобилизационным стрессом.</p><sec><title>Материалы и методы</title><p>Материалы и методы. Для моделирования повреждения слизистой оболочки экспериментальным животным (белые крысы-самцы линии Wistar) вводили 120 ммоль/л раствора аммиака после 24-часового иммобилизационного стресса. В качестве препаратов сравнения были выбраны официнальные противоязвенные средства, широко применяемые в клинической практике: ранитидин (30 мг/кг, 10 мг/кг и 3 мг/кг) и омепразол (3 мг/кг, 1 мг/кг и 0,3 мг/кг). Изучаемое соединение использовалось в дозах 30 мг/кг, 10 мг/кг и 3 мг/кг. Максимальные дозы препаратов сравнения рассчитывались исходя из максимальной суточной дозы для человека с учетом межвидового коэффициента пересчета. Максимальная доза исследуемого вещества была подобрана экспериментально. Для удобства дальнейших расчетов значения ЕD50 был использован логарифмический диапазон доз. Все исследуемые объекты вводились внутрижелудочно с помощью атравматичного зонда.</p></sec><sec><title>Результаты и обсуждение</title><p>Результаты и обсуждение. Установлено, что изучаемая субстанция достоверно относительно контрольных значений снижала площадь повреждения слизистой оболочки при моделировании геликобактероподобного повреждения, спровоцированного введением раствора аммиака на фоне ишемии слизистой желудка после 24-часовой иммобилизации. При этом, в группах животных, получавших производное бензимидазола в дозе 30 мг/кг, ингибирование образования эрозий достигло 78%, в то время как в группах, получавших ранитидин и омепразол 66% и 50% соответственно. Расчетные значения ЕD50 для изучаемой субстанции составили 16,03 мг/кг, а для ранитидина – 15,99 мг/кг.</p></sec><sec><title>Заключение</title><p>Заключение. Полученные результаты свидетельствуют о том, что изучаемое производное бензимидазола превосходит аналоги по способности подавлять изъязвление слизистой желудка, спровоцированное геликобактероподобным воздействием, что подтверждает актуальность дальнейшего исследования противоязвенной активности и разработки готовой лекарственной формы на его основе.</p></sec></abstract><trans-abstract xml:lang="en"><p>The search for new drugs providing effective and safe therapy of acid-dependent diseases of the gastrointestinal tract, continues to be an actual problem of modern pharmacotherapy. One of the most significant pathogenetic mechanisms of these diseases is associated with Helicobacter pylori damage to the gastric mucosa.</p><p>The aim of this study is the experimental investigation of the antiulcer effect of 2-phenyl-9-diethylaminoethylamine [1,2-a] benzimidazole substance (hereinafter a Benzimidazole derivative substance) on the model of Helicobacter pylori-like gastric mucosal injury in combination with immobilization stress (a restraint).</p><sec><title>Materials and methods</title><p>Materials and methods. For modeling a mucous membrane damage to experimental animals (white Wistar male rats), they were injected 120 mmol/l ammonia solution after a 24-hour immobilization stress (restraint). As reference drugs, the following officinal anti-ulcer drugs widely used in clinical practice, had been chosen: Rranitidine (30 mg/kg, 10 mg/kg and 3 mg/kg) and Omeprazole (3 mg/kg, 1 mg/kg and 0.3 mg/kg). The study substance was used in the doses of 30 mg/kg, 10 mg/kg and 3 mg/kg. The maximum doses of the reference drugs were calculated on the basis of maximum daily doses for humans, taking into consideration the interspecies conversion factor. The maximum dose of the substance under study was selected experimentally. The logarithmic dose range was used for the convenience of further calculations of the ED50 value. All the studied objects were introduced intragastrically through a non-traumatic tube.</p></sec><sec><title>Results and discussion</title><p>Results and discussion. It has been established that the studied substance significantly reduced the area of mucosal damage relative to the control values in modeling Helicobacter pylori-like gastric mucosal injury provoked by the administration of ammonia solution against the background of gastric mucosal ischemia after a 24-hour restraint. At the same time, the inhibition of ulceration reached 78%, while in the groups receiving Ranitidine and Omeprazole, it reached 66% and 50%, respectively. The calculated ED50 values were the following: for the substance under study – 16.03 mg/kg, and for Ranitidine – 15.99 mg/kg.</p></sec><sec><title>Conclusion</title><p>Conclusion. The gained results indicate that the studied Benzimidazole derivative is superior to analogs in its ability to suppress gastric mucosal ulceration provoked by Helicobacter pylori-like gastric mucosal injury, which confirms the relevance of further study of anti-ulcer activity and the development of the pharmaceutical dosage form based on it.</p></sec></trans-abstract><kwd-group xml:lang="ru"><kwd>2-фенил-9-диэтиламиноэтилимидазо[1</kwd><kwd>2-а] бензимидазол</kwd><kwd>противоязвенное действие</kwd><kwd>геликобактероподобная язва</kwd></kwd-group><kwd-group xml:lang="en"><kwd>2-phenyl-9-diethylaminoethylamine[1</kwd><kwd>2-a] benzimidazole</kwd><kwd>antiulcer effect</kwd><kwd>Helicobacter pylori-like ulcer</kwd></kwd-group><funding-group><funding-statement xml:lang="ru">Федеральная целевая программа «Развитие фармацевтической и медицинской промышленности Российской Федерации на период до 2020 года и дальнейшую перспективу». Тема работы: «Доклинические исследования Н2-гистаминоблокирующего лекарственного средства, снижающего геликобактероподобные повреждения, на основе производного бензимидазола», государственный контракт №14.N08.11.1042 от 14.11.2017</funding-statement><funding-statement xml:lang="en">The study was carried out in accordance with the Federal target program “Development of the pharmaceutical and medical industry of the Russian Federation for the period up to 2020 and beyond”. The topic  of work: “Preclinical studies of H2-histamine-blocking drug that reduces Helicobacter-like damage based on benzimidazole derivative”, state contract № 14.N08.11.1042 from 14.11.2017</funding-statement></funding-group></article-meta></front><back><ref-list><title>References</title><ref id="cit1"><label>1</label><citation-alternatives><mixed-citation xml:lang="ru">Krishna Prasad P.M., Avdhut K. Potent biological agent benzimidazole–a review // Int. J. of Pharmacy and Pharm. Sciences. 2016. Vol. 8. Is. 12. 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