STUDY OF THE INFLUENCE OF EXCIPIENTS ON THE PHARMACO-TECHNOLOGICAL INDICATORS OF THE TABLETS OF BISOPROLOL FUMARATE AND INDAPAMIDE
DOI:
https://doi.org/10.11603/2312-0967.2023.4.14368Keywords:
antihypertensive drugs, tablets, direct compression, bisoprolol fumarate, indapamide, excipients, pharmaco-technological indicatorsAbstract
The aim of the work. Study of the influence of excipients on the pharmaco-technological parameters of powder masses and tablets of bisoprolol fumarate with indapamide.
Materials and Methods. Bisoprolol fumarate and indapamide powders; 27 excipients from the groups of disintegrants, sliding agents, lubricants, diluents based on microcrystalline cellulose (MCC) and multifunctional fillers were chosen for the pharmaceutical development of tablets. A five-factors experiment based on the Graeco-Latin cube of the second order was used to study the influence of excipients.
Tablets were obtained by direct compression. The study of the properties of the powder mixtures and the quality indicators of the tablets was carried out in accordance with the requirements of the State Pharmacopoeia of Ukraine. The process of pressing tablets and their appearance were also evaluated. Conclusions regarding the selection of optimal excipients were made using the desirability function.
Results and Discussion. The results of the study show that the flowability, bulk and tapped density, the angle of repose of the powder mixtures and the evaluation of the pressing process were most affected by sliding agents, namely Neusilin US 2, as well as samples of multifunctional fillers (MagGran or Cellactose 80) and fillers based on MCC (Vivapur 200 or 302). Better indicators of hardness testing and friability of tablets were provided by sliding substances, namely Syloid 244 FP. Disintegrants, namely sodium croscarmellose, had a decisive effect on the time of disintegration of tablets. To make a decision on the selection of optimal excipients used a generalized indicator - the desirability function.
Conclusions
The influence of the 27th excipients on the pharmaco-technological indicators of powder masses and tablets of bisoprolol fumarate with indapamide was studied. It was established that the optimal quality indicators of tablets with bisoprolol fumarate and indapamide were obtained when using sodium starch glycolate type VivaStar, Neusilin US 2, PEG-6000, Prosolv EASY tab SP and SacheLac 80. The results of this study are the basis for determining the optimal quantitative ratio of excipients in composition of tablets using regression analysis.
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