CHOICE OF RATIONAL EXCIPIENTS TO CREATE «ANGIOLIN» TABLETS BY WET FRANUALTION

Authors

  • O. S. Bіdnenko Zaporizhzhia State Medical University
  • L. I. Kucherenko Zaporizhzhia State Medical University, SPA “Farmatron”, Zaporizhzhia
  • I. A. Mazur Zaporizhzhia State Medical University, SPA “Farmatron”, Zaporizhzhia
  • Z. B. Moryak Zaporizhzhia State Medical University, SPA “Farmatron”, Zaporizhzhia

DOI:

https://doi.org/10.11603/2312-0967.2016.2.6644

Keywords:

angiolin, excipients, tablets, wet franualtion.

Abstract

Introduction.  Cardiovascular diseases along with cancer and diabetes firmly lead among the most common and most dangerous diseases of XX, and now the XXI century. Diseases of the cardiovascular system are numerous. In Ukraine morbidity in circulatory diseases and its first position in the structure of total mortality indicate a growing prevalence of this pathology and is an unfavorable indicator of population health. The mortality is about 65.8%, where in the coronary heart disease (CHD) is 71.1%.

Coronary heart disease is one of the most dangerous diseases, which accounts for one of the highest mortality rates from diseases of the circulatory system. CHD contributing factors are smoking, hypertension, high cholesterol, genetic predisposition and sedentary lifestyle.

We have been looking for the effective cardiovascular drugs made from new chemical compounds and have been basing on enhanced studying and elucidation of new mechanisms of existing drugs that have proven themselves in clinical practice. We have been found new properties in these clinically proven pharmaceutically active compounds. With the combination of structural fragments of molecules, the staff members of SPA "Farmatron" together with employees of Zaporozhye State Medical University created "Angiolin" - a new drug with cation-anion effect. "Angiolin" is the salt formed between the amino acid lysine and 3-methyl-1,2,4-triazole-5-thio-acetic acid. The compounds are planned to use for the treatment of cardiovascular diseases, especially in chronic pathologies of the cardiovascular system.

Medicines that are able to interrupt or reduce the ischemic unfavorable metabolic reactions caused by ischemia and united as "metabolitetropic cardioprotectors", have a protective effect on the myocardium and have undoubted promise in clinical practice. The numerous studies on the impact of dosage form for the therapeutic efficacy of drugs have found that the optimal activity of the drug is achieved only in a rational dosage form. Also in this case, you can avoid many side effects of drugs on the organism.

Investigation methods. The studied literature shows that "metabolitetropic cardioprotectors" in most cases should be used during a long time, and even lifelong. Therefore, the most drugs for the treatment of cardiovascular diseases are used in pill form.

Based on the foregoing, the development of technology of "Angiolin" tablets is relevant. Thus the purpose of our work is to select the excipients for tablets containing 200 mg of active substance by wet granulation.

Results and discussions. The four excipients groups which have different physical and technological properties have been investigated. We’ve investigated16 excipients, most of which appeared on the market in recent years and have no examples in the pharmaceutical technology in the creation of tablet products. In the study of four qualitative factors, one of the analyses of variance - Graeco-Latin square factorial design was used.

Conclusions.  As a result of these studies we have found so called "leaders" among studied four excipient groups, in the effects on one or another pharmacotechnological parameter of powder masses.

References

Georgievskij G.V. Razrabotka kompleksa fiziko-himicheskih metodik, obespechivayushchih sozdanie i kontrol' kachestva original'nyh otechestvennyh preparatov, proizvodnyh 1,2,4-triazola / G.V. Georgievskij // Zaporozhskij medicinskij zhurnal. – 2011. – T. 13. – № 1. – S. 58–69.

Derzhavna Farmakopeya Ukraїni : v 3 t. / Derzhavne pіdpriєmstvo «Ukraїns'kij naukovij farmakopejnij centr yakostі lіkars'kih zasobіv». — 2-e vid. — Harkіv: Derzhavne pіdpriєmstvo «Ukraїns'kij naukovij farmakopejnij centr yakostі lіkars'kih zasobіv». – 2016.

Kompendium. Lekarstvennye preparaty 2012. /Pod red. prof. Kovalenko V.N.//K.: Morion, 2012. – 2320 s.

Matematichne planuvannya eksperimentu pri provedennі naukovih doslіdzhen' v farmacії / [Groshovij T. A., Marcenyuk V. P., Kucherenko L. І. ta іn.]. – Ternopіl': Ukrmedkniga, 2008. – 368 s.

Metabolitotropnye preparaty / I.A. Mazur, I.S. Chekman, I.F. Belenichev – Zaporozh'e, 2007. – 304 s.

Podhody k razrabotke i sozdaniyu metabolitotropnyh preparatov – proizvodnyh 1,2,4-triazola / I.A. Mazur, I.F. Belenichev, L.I. Kucherenko, Pavlyuk I.V., Steblyuk V.S., Georgievskij G.V. // Farmakom. – 2012. – №3. – S. 78–82.

Sercevo-sudinna zahvoryuvanіst' v Ukraїnі ta rekomendacії shchodo pokrashchannya zdorov’ya v suchasnih umovah / Kornac'kij V.M., Dorogoj A.P., Manojlenko T.S. // Analіtichno- statistichnij posіbnik. – K., 2012. – 117 s.

Shchodo postadіjnogo kontrolyu virobnictva tabletok / L.І. Kucherenko, O.V. Hromil'ova, Z.B. Moryak // Aktual'nі pitannya farmacevtichnoї і medichnoї nauki ta praktiki. – 2014. – №2. – S. 31–34.

Andersson B, Stromblad S.O, Lomsky M, Waangstein F. Heart rate dependency of cardiac performance in heart failure patients treated // Eur Heart J. -2009.-Vol. 20.-P. 575- 580 10. European Pharmacopoeia. – 6th-еd. Сouncil of Europe. – Strasbourg, 2007. – 3857.

Published

2016-07-08

How to Cite

Bіdnenko O. S., Kucherenko, L. I., Mazur, I. A., & Moryak, Z. B. (2016). CHOICE OF RATIONAL EXCIPIENTS TO CREATE «ANGIOLIN» TABLETS BY WET FRANUALTION. Pharmaceutical Review Farmacevtičnij časopis, (2), 16–21. https://doi.org/10.11603/2312-0967.2016.2.6644

Issue

Section

Pharmaceutical technology, biopharmacy, homeopathy, biotechnology