PREFORMULATION STUDIES OF TABLETS CONTAINING RIVAROXABAN – NIACINAMIDE COCRYSTALLIZATION COMPOUNDS

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 pharmacotechnical 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 excipien ts, 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. RezumatPreformularea este prima faz n care se colecteaz date fizico-chimice despre compuii farmacologici, se evalueaz potenialii lor derivai i se determin acceptabilitatea excipienilor nainte de fabricaie.De asemenea, ofer o hart pentru dezvolta rea formulrii.Muli factori de performan a medicamentelor, cum ar fi absorbia, viteza de dizolvare i productibilitatea, sun t influenai semnificativ de dimensiunea particulelor de medicament.Optimizarea distribuiei dimensiunii particulelor garanteaz c medicamentul poate fi produs cu succes i absorbit n organism.n timp ce particulele mai mici ar putea crea dificulti n timpul fabricaiei, particulele mai mari s-ar putea dizolva prea lent, reducnd biodisponibilitatea.Prezentul studiu i propune s determine proprietile farmacotehnice ale unor cocristale RIV-NIA n raporturi molare 1:1 i 1:2 nainte i dup amestecarea cu excipienii pentru compresie direct.A fost identificat o corelaie puternic ntre dimensiunea particulelor, coninutul de umiditate, curgerea i compresibilitatea pulberilor.Datorit creterii dimensiunii particulelor i reducerii suprafeei dup adugarea excipienilor, amestecurile pentru comprimarea direct pentru toate formulrile au prezentat proprieti de curgere mai bune n comparaie cu sistemele binare originale.Toate cele patru sisteme binare au prezentat o curgere slab i o compresibilitate ridicat, dar acestea s-au mbuntit semnificativ dup adugarea excipienilor.