Selection of disintegrants for wet granulation method of “Angiolin” tablets

No5 (98) 2016 ISSN 2306-4145 UDC: 615.453.6’27.012/.014:615.014.47 DOI: 10.14739/2310-1210.2016.5.82698 I. A. Mazur1,2, L. I. Kucherenko1,2, O. S. Bidnenko1, Ye. A. Portnaya1,2 Selection of disintegrants for wet granulation method of “Angiolin” tablets 1Zaporizhzhia State Medical University, Ukraine, 2SPA «Farmatron», Zaporizhzhia, Ukraine

Выводы. Отобран разрыхлитель, а именно -натрия кроскармелоза, который показал лучшие результаты и в дальнейшем будет использован в получении таблеток «Ангиолин» методом влажной грануляции. E very year there are about 9.4 million people who die from cardiovascular diseases. Among them, 51 % of people are dying from stroke, and 45 % -from coronary heart disease. Today the disease of the cardiovascular system is number 1 problem in the world, and in Ukraine. Annually cardiovascular disease kills more than 500 thousands of Ukrainians; it is about 1370 people every day [7]. According to the State Statistics Service, about half of the deaths in 2016 in Ukraine had been caused by cardiovascular diseases. In comparison with 2015, the death rates have not changed in Ukraine. This shows low culture of prevention, diagnosis and treatment of cardiovascular disease among Ukrainians [7].
For the last 3 years the cardiovascular diseases make up 66 % in general structure of mortality among Ukrainians while in most European countries, this figure does not exceed 50 % [9].
Ukraine is among the countries of the international community, which set a goal to reduce mortality from cardiovascular diseases (CVD) in the quarter in 2025.
In our previous studies, we have selected the best excipients for "Angiolin" tableting by wet granulation method. "Angiolin" met all the requirements of State Pharmacopoeia of Ukraine in pharmaco-technological indices [5,6]. But due to the fact that some pharmaco-technological indices of selected tablet series were at threshold limit, we proposed to introduce disintegrant into these series [1].
Therefore, aim of our study is the selection of disin tegrants in "Angiolin" tableting by wet granulation method.

Materials and methods
We use the newest and modern equipment to determine the uniformity of the tablet mass, friability, hardness, disintegration time and the production of tablets.

Single-balanced plan and the study results of powder masses and tablets (S)-2,6-diaminohexane acid 3-methyl-1,2,4-triazolyl-5-thioacetate
The experimental design matrix for one-way balanced plan scheme and the study results of powder and tablets mass are shown in Table 1. The analysis of variance was conducted according to the experimental studies results (Table 1) [4].
On the basis of the analysis of variance we came to the conclusion about the effect of the studied disintegrants on pharmaco-technological properties of the powder mass and "Angiolin" tablets [8].
The figure shows the effect of disintegrants on the uniformity of "Angiolin" tablet mass.
The best indexes were observed using potato starch, which takes precedence over MCC burst, carboxymethyl sodium, polyplasdone XL 10, likotab P, croscarmellose sodium. It should be noted that the uniformity of obtained tablets mass met the pharmacopoeia standards for all species of studied disintegrants (Fig. 1).
Next, we considered the effect of disintegrants the on the tablet hardness.
The analysis of figure showed that the effectiveness of disintegrants can be illustrated by the following several advantages: likotab P, MCC burst, sodium carboxymethyl, potato starch, polyplasdone XL 10, croscarmellose sodium. The likotab P is the leader among the substances of the studied group (Fig. 2).
The study of the effect of disintegrants on tablet friability was conducted.
The analysis of figure showed that studied excipients can be placed according to the effect on tablet friability in the following sequence: MCC burst> likotab P> polyplasdone XL 10>sodium carboxymethyl>potato starch>croscarmellose sodium. MCC burst showed the best results, while sodium croscarmellose showed the highest percentage of tablet friability (Fig. 3).
Next, we considered the effect of disintegrants the on the disintegration.
«Angiolin» tablets, which contain croscarmellose sodium, were fastest disintegrated. The mentioned disintegrant has a significant advantage over others such as likotab P, MCC burst, sodium carboxymethyl, starch potato, polyplasdone XL 10 (Fig. 4). Findings: 1. The effect of disintegrants on the technological characteristics of "Angiolin" tablets was studied and the possibility of their production by wet granulation was confirmed.
2. The selected disintegrant, namely sodium croscarmellose showed better results and will be used for "Angiolin" tableting by wet granulation method in the future.
Challenges for further study: in future we will select and develop quantitative formula of the "Angiolin" tablets.
Conflicts of Interest: аuthors have no conflict of interest to declare.  Fig. 4. The effect of disintegrants on the "Angiolin" tablet disintegration.  Fig. 1. The effect of disintegrants on the uniformity of "Angiolin" tablet mass.