PHYSICHOCHEMICAL CHARACTERISATION OF TICAGRELOR AMORPHOUS SOLID DISPERSIONS PREPARED BY SPRAY-DRYING PROCESS

Solid dispersions are widely used in the pharmaceutical industry in order to enhance the oral bioavailability of poorly solub le active pharmaceutical ingredients (APIs).Ticagrelor (TICA) exhibits limited water solubility and poor permeability through biological membranes.Dosage forms present on the market contain TICA in a crystalline state.However, the amorphous state of a drug is preferred because it requires less energy to dissolve.Thus, the dissolution kinetics is favourable compared to its crystalline counterpart.The aim of this study was to prepare and characterise 1:1 mass ratio of ticagrelor amorphous polymer solid dispersions obtained by spray-drying method.The systems were characterised by employing standard Differential Scanning Calorimetry (DSC), Fourier transform-infrared spectroscopy (FTIR) and Powder X-ray Diffraction (PXRD).The results demonstrate that amorphous solid dispersions of TICA with two polymers -hydroxypropyl cellulose (HPC) and Soluplus (SLP) -were successfully prepared using the spray-drying process. RezumatDispersiile solide sunt utilizate pe scar larg n industria farmaceutic pentru a accelera biodisponibilitatea oral a substanelor active farmaceutic (APIs) cu solubilitate redus.Ticagrelorul (TICA) prezint o solubilitate sczut n ap i o permeabilitate slab prin membranele biologice.Formele farmaceutice prezente pe pia conin TICA n stare cristalin.Totui, forma amorf a unui medicament este preferat, deoarece necesit o energie mai mic pentru dizolvare.Astfel, cinetica dizolvrii este favorabil n comparaie cu omologul su cristalin.Scopul acestui studiu a fost prepararea i caracterizarea unor dispersii solide amorfe formate din ticagrelor i polimer, n raport masic 1:1, obinute prin tehnica de uscare prin pulverizare.Sistemele au fost caracterizate utiliznd urmtoarele tehnici analitice: calorimetrie diferenial de scanare (DSC), spectroscopie n infrarou cu transformare Fourier (FTIR) i difracia de raze X pe pulberi (PXRD).Rezultatele obinute demonstreaz formarea cu succes a dispersiilor solide amorfe de TICA cu doi polimeri testai, hidroxi-propil celuloz (HPC) i soluplus (SLP).