STUDY OF ANTISECRETORY ACTIVITY OF DINITRATE 2-PHENYL-9-DIETHYLAMINOETHYLimidazo[1,2-A] BENZIMIDAZOLE BY METHOD OF CONTINUOUS PERFUSION OF RATS’ STOMACHS

M. Chernikov, M. Oganova, A. Gerasimenko, E. A. Artemyev
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引用次数: 1

Abstract

Nowadays, effective pharmacotherapy of acid-dependent gastrointestinal diseases remains an urgent problem of modern gastroenterology. In this regard, the search for new drugs with a pronounced antisecretory activity still continues; their aim is to keep the control over the acid production safe and effective.The aimof this study was an experimental study of the antisecretory activity of the substance and the finished dosage form (FDF) of dinitrate 2-phenyl-9-diethylaminoethylimidazo[1,2-a]benzimidazole.Materials and Methods.The study of antisecretory activity was performed by method of a continuous perfusion of rats’ stomachs. The studied substance was administered at the doses of 3, 10 and 30 mg/kg, and the FDF – at the doses of 13 and 26 mg/kg. The substance of Ranitidine (Sigma Аldrich, USA) was used as a reference object in the study of the antisecretory activity of the substance under study, and Ranitidine (Hemofarm A.D., Serbia) was used as a reference drug in the study of the FDF. In order to determine the stimulated secretion immediately before collecting the samples of the perfusate, histamine was administered subcutaneously at the dose of 5 mg/kg. The content of hydrochloric acid in the perfusate was determined by titration of a 0.01 M sodium hydroxide solution. The acidity value was determined in terms of the debit-hour of hydrochloric acid.Results and discussion.The obtained experimental data showed that the studied substance at the dose of 30 mg/kg decreased the basal hydrochloric acid secretion by 54%, which significantly exceeded the antisecretory effect of Ranitidine by 1.8 times. The FDF at the dose of 26 mg/kg, statistically reliable relative to the control and the group treated with Ranitidine, decreased the basal secretion of gastric juice by 33%. The substance at the dose of 30 mg/kg reliably suppressed the stimulated secretion of hydrochloric acid by 80%, while Ranitidine did it by 56%. The FDF at the dose of 26 mg/kg decreased the histamine-stimulated secretion by 66%, and Ranitidine did it by 52%, which was statistically reliable.Сonclusions.The studied substance and its dosage form are more effective in suppressing basal activities and exceed the anisecretory activity of H2 -histamine antagonists of Ranitidine under the conditions of the secretion stimulated by histamine.
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2-苯基-9-二乙基氨基-乙基咪唑[1,2- a]苯并咪唑大鼠胃连续灌注抗分泌活性的研究
目前,酸依赖性胃肠道疾病的有效药物治疗仍然是现代胃肠病学亟待解决的问题。在这方面,寻找具有明显抗分泌活性的新药仍在继续;他们的目的是保持对酸生产的安全有效的控制。本研究的目的是实验研究该物质的抗分泌活性和硝酸盐2-苯基-9-二乙基氨基乙基咪唑[1,2-a]苯并咪唑的成品剂型(FDF)。材料与方法。采用大鼠胃连续灌注法研究其抗分泌活性。所研究物质的剂量分别为3、10和30 mg/kg, FDF -的剂量分别为13和26 mg/kg。研究物质的抗分泌活性以雷尼替丁(Sigma Аldrich, USA)为参比对象,FDF研究以雷尼替丁(Hemofarm a.d., Serbia)为参比药物。为了在收集灌注液样品前立即测定受刺激的分泌,皮下注射组胺,剂量为5 mg/kg。用0.01 M氢氧化钠溶液滴定法测定灌注液中盐酸的含量。酸度值是根据盐酸的借方小时来确定的。结果和讨论。得到的实验数据表明,所研究物质在剂量为30 mg/kg时,使盐酸基础分泌减少54%,明显超过雷尼替丁的1.8倍。FDF剂量为26 mg/kg,与对照组和雷尼替丁组相比,统计学可靠,使胃液基础分泌减少33%。该物质在30 mg/kg剂量下可靠地抑制受刺激的盐酸分泌80%,而雷尼替丁的抑制率为56%。26 mg/kg剂量的FDF使组胺刺激分泌减少66%,雷尼替丁使组胺刺激分泌减少52%,统计学差异为reliable.Сonclusions。在组胺刺激分泌的条件下,所研究的物质及其剂型更有效地抑制基础活性,并超过雷尼替丁H2 -组胺拮抗剂的分泌活性。
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