ВИБІР РАЦІОНАЛЬНИХ ДОПОМІЖНИХ РЕЧОВИН З МЕТОЮ СТВОРЕННЯ ТАБЛЕТОК «ГІПЕРТРИЛ» МЕТОДОМ ПРЯМОГО ПРЕСУВАННЯ Повідомлення 1. «Дослідження впливу допоміжних речовин на технологічні характеристики порошкових мас»

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 hypertril's powder masses”

N.V. Parnyuk, L.I. Kucherenko, O. O. Portna

Zaporozhye State Medical University, Zaporozhye

Key words: hypertril, excipients, powders masses, direct pressing

Introduction

Cardiovascular diseases are the most common cause of death in the Ukraine and in the world, but in the Ukrainian society awareness of the risk factors is very low, and mortality - is very high. Arterial hypertension (AH) is the most common among the pathologies of the cardiovascular system.

Staff members of SPA "Farmatron" (Zaporizhzhia) in collaboration with the Department of Pharmaceutical Chemistry of Zaporizhzhia State Medical University synthesized new original compound bromide 1- (β- phenylethyl)-4-amino-1,2,4-triazole and got the certificate of trademark called "Hypertril". During pharmacological studies, we revealed that hypertril has combined properties of cardioselective ß₁- adrenoceptor blocking agent and peripheral vasodilator, thus showing antihypertensive, antiischemic and antioxidant properties. Systematic preclinical studies of hypertril as antihypertensive drug made it possible to establish ED (effective dose) of 50 to animal and predict the advisability of its taking to human in dose of 20 mg per reception. In the course of studying the literature sources we came to the conclusion that drugs for the treatment of hypertension are used for a long time. Most drugs for the treatment of cardiovascular diseases are used in tablet form. Based on the foregoing, it is urgent to develop technology of tablets based on "Hypertril" containing 20 mg of active ingredient.

Thus, the aim of our work is the development of technology of "Hypertril" tablets with 20 mg of active ingredient.

Materials and Methods

The studies of rational choice of excipients to create "Hypertril" tablets by direct pressing were undertaked. We studied six excipients groups having different physical and technological properties.

 We studied 30 excipients, most of which appeared on the market in recent years and have no examples in pharmaceutical technology for tablet drugs creating. One tablet contained 0.02g of hypertril, 0.082 g samples of MCC (microcrystalline cellulose) (factor A), 0.040g of sugar sample (factor B), 0.010g of disintegrant (factor C), 0.040g of crystalline substances (factor D), 0,006g of glidants (factor E) and 0.002g 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. Based on this carried out analysis we concluded the impact of studied factors on pharmaco-technological properties of the hypertril powder masses.

Research results

The results of analysis of variance showed that all six studied factors as follows: D> A> C> F> E> B affect hypertril’s free bulk of powder blend; after shrinkage - A> D> C> E > B> F affect hypertril’s tapped bulk density, also all the factors affect flow powder blend: D> E> B> A> C> F, angle of natural repose of hypertril’s powders - D> C> E> A> B> F.

In the study of powder masses on indicants of free bulk of powder blend, tapped bulk density, fluidity and angle of natural repose, we found that in most series of experiments powder masses have technological properties that indicate the possibility of tablets’ creating by direct pressing.

The studies have shown that studied six groups of excipients manifest "leaders" in effect on one or another pharmaco-technological powder masses index.

Conclusions

1. The effect of six excipients groups on technological characteristics of hypertril’s powder masses is studied.
2. In most series of experiments, powder masses have technological properties that indicate the possibility of tablets’ creating by direct pressing.

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