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• W2764133740 abstract "CHOICE OF RATIONAL EXCIPIENTS TO CREATE «HYPERTRIL» TABLETS BY DIRECT PRESSING Report 1. «Investigation of the effect of excipients on the technological characteristics of the tablets «Hypertril» N. V. Parnyuk, L. I. Kucherenko, O. O. Portna Zaporizhian State Medical University Scientific-and-Production Corporation «Pharmatron», Zaporizhzhia Introduction Despite the variety of serious diseases which are relevant to the modern world, cardiovascular diseases remain the leading causes of death in the world. Proper treatment and competent prevention of cardiovascular diseases will help reduce the number of patients suffering from coronary disease, strokes and other ailments. Staff members of SPA Farmatron (Zaporizhzhia) in collaboration with the Department of Pharmaceutical Chemistry of Zaporizhzhia State Medical University under Professor Mazur I.A. synthesized new original hypertril medication (bromide 1-(β-phenylethyl)-4-amino-1,2,4-triazole), which shows antihypertensive, antiischemic and antioxidant properties. After preclinical studies we have established ED 50 for animals and predicted human advisability of taking 20 mg of hypertril per reception. Thus the development of technology of tablet dosage form containing 20 mg of active substance became a burning issue of today. Objective.  Development of technology of Hypertril tablets by direct pressing on the basis of selection of rational excipients. Methods.  In previous studies, we have studied six excipients groups which possess different physical and technological properties. In this paper, we concentrate on the study of the effect of different excipients groups on pharmaco-technological properties hypertril tablets. One tablet contained0.02 g of hypertril,0.082 g sample of microcrystalline cellulose (factor A),0.040 g of sugar sample (factor B),0.010 g of disintegrant (factor C),0.040 g of crystalline substances (factor D),0,006 grams of glidants (factor E) and0.002 g of lubricants (factor F). In the study of six qualitative factors we used one of the plans of analysis of variance – six-factor experiment based on Hyper-Greco-Latin square. The results of experimental studies were analyzed by analysis of variance upon which we concluded studied impact of factors on the technological properties of hypertril tablets. Results and discussion.  The results of analysis of variance showed that only factor A affects the process of pressing of Hypertril tablets under statistical insignificance of the other five factors. All six factors affect the uniformity of tablets weight in the following order: D> A> C> F> E> V, tablets strength - A> E> D> F> B> C, tablets abrasion: A > D> C> F> B> E, tablets disintegration - C ˃ F ˃ in ˃ D ˃ E ˃ A. The conducted researches have shown that studied six groups of excipients manifest leaders in effect on one or another technological tablets index. As a result of the conducted researches the rational excipients, which made it possible to offer optimal composition of Hypertril tablets, were chosen. Findings The effect of six excipients groups on technological characteristics of hypertril tablets is studied and the possibility of their receiving by straight pressing was proved. As a result of complex pharmaco-technological researches an optimal composition of new Hypertril tablet medication with 20 mg of active substance was developed. References Belenychev Y.F. Nekotorie aspekti kardyoprotektornoho deystvyya novoho β-adrenoblokatora s NO-mymetycheskym ehffektom «Hypertryl» na modely ynfarkta myokarda / Belenychev Y.F., Kucherenko L.Y., Volchyk Yu.A., Abramov A.V., Bukhtyyarova N.V // Farmakolohiya ta likars'ka toksykolohiya. - 2014. - # 4–5 (40) – C. 11-16. Derzhavna Farmakopeya Ukrayiny / DP Naukovo-ekspert¬nyy farmakopeynyy tsentr. - 1-e vyd. - Kharkiv: RIHER, 2001. - 556s. Mazur Y.A., Belenychev Y.F., Chekman Y.S. y dr. Prymenenye bromyda 1-(beta-fenylehtyl)-4-amyno-1,2,4-tryazolyya (Hypertryl) kak aktyvnoy osnovy lekarstvennykh sredstv dlya korrektsyy narushenyy funktsyonyrovanyya nytroksyderhycheskoy systemi orhanov-mysheney pry homotsysteynemyy y ostrykh narushenyyakh mozhovoho kroobrashchenyya. Patent 2532394 Rossyyskaya Federatsyya. MPK A61K31/4196 (2006.01) A61P9/10 (2006.01) A61P43/00 (2006.01). Zayavytel' y patentoobladatel' OOO NPO «Farmatron». - # 2013148306. Zayavl. 29.10.2013, opubl. 10.11.2014. Mazur I.A., Byelyenichev I.F., Chekman I.S. ta in. Zastosuvannya bromidu 1-(β-feniletyl)-4-amino-1,2,4-tryazoliyu yak aktyvnoyi osnovy likars'kykh zasobiv dlya korektsiyi porushen' funktsionuvannya nitroksyderhichnoyi systemy pry aterosklerozi i tsukrovomu diabeti. Patent 84351 Ukrayina. MPK A61K 31/41 (2006.01), A61P 9/10 (2006.01). Zayavnyk i patentovlasnyk TOV NVO «Farmatron». - # a201212500. Zayav. 02.11.2012, opubl. 25.10.2013. Matematychne planuvannya eksperymentu pry provedenni naukovykh doslidzhen' v farmatsiyi / [Hroshovyy T.A., Martsenyuk V.P., Kucherenko L.I. ta in.] –  Ternopil': Ukrmedknyha, 2008. – p. 368. Parnyuk N.V. Vybir ratsional'nykh dopomizhnykh rechovyn z metoyu stvorennya tabletok «Hipertryl» metodom pryamoho presuvannya Povidomlennya 1. «Doslidzhennya vplyvu dopomizhnykh rechovyn na tekhnolohichni kharakterystyky poroshkovykh mas» / Parnyuk N.V., Kucherenko L.I., Portna O.O.// Farmatsevtychnyy chasopys – 2015, # 4 – S. 19-24. BeckettN.S., Peters R., Fletchers A.E. et al. Treatment of  Hypertension in Patients 80 Years of Age or Older// N Engl J Med. 2011; 358:1887–1888. Coca A. Cerebral involvement in hypertensive cardiovascular disease// Eur. Heart J. 2010; 5 (Suppl): P. 19–25." @default.
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