Romanian Society of Pharmaceutical Sciences
 

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PREFORMULATION STUDIES OF TABLETS CONTAINING RIVAROXABAN – NIACINAMIDE COCRYSTALLIZATION COMPOUNDS

CRISTINA SOLOMON 1, IULIAN SÂRBU 1, VALENTINA ANUȚA 2, EMMA ADRIANA OZON 1, ADINA MAGDALENA MUSUC 3, ANCUȚA CĂTĂLINA FIȚA 1*, DENISA TEODORA NITĂ 1, MIRELA ADRIANA MITU 1

1 Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, 6 Traian Vuia Street, 020956, Bucharest, Romania
2 Innovative Therapeutic Structures Research and Development Centre (InnoTher), “Carol Davila” University of Medicine and Pharmacy, 6 Traian Vuia Street, 020956, Bucharest, Romania
3 Institute of Physical Chemistry – Ilie Murgulescu, Romanian Academy, 060021, Bucharest, Romania

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Preformulation is the first phase in which physicochemical data on pharmacological compounds are collected, their potential compounds are evaluated and the acceptability of excipients is determined prior to manufacture. It also provides a roadmap for formulation development. A lot of drug performance factors, such as absorption, dissolution rate, and manufacturability, are significantly influenced by the size of the drug particles. Optimizing the particle size distribution guarantees that the drug may be produced successfully and absorbed in the body. While smaller particles could provide difficulties during manufacture, larger particles might dissolve too slowly, decreasing bioavailability. The present study aims to determine the pharmaco-technical properties of some RIV-NIA cocrystals in 1:1 and 1:2 molar ratios before and after mixing with the excipients for direct compression. A strong correlation between the particle size, moisture content, flowability and compressibility of the powders was identified. Due to the increase in particle size and the reduction in surface area after the addition of excipients, the direct compression blends for all formulations for direct compression exhibited better flow properties compared to the original binary systems. All four binary systems exhibited poor flowability and high compressibility, but they were notably improved after the addition of the excipients for direct compression process.