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Razvoj koprocesiranega mezoporoznega silicijevega dioksida z disaharidi, polioli in polimeri za direktno tabletiranje
ID Dovjak, Jernej (Author), ID Planinšek, Odon (Mentor) More about this mentor... This link opens in a new window

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Abstract
Silicijev dioksid je široko uporabljena pomožna snov v farmaciji, največkrat kot dodatek k zmesem praškov za boljše pretočne lastnosti. Kot nosilec zdravilnih učinkovin za izdelavo trdnih disperzij težko vodotopnih zdravilnih učinkovin je do sedaj proučevan le na področju raziskav, kjer pa raziskovalci po navadi ne izdelujejo končne farmacevtske oblike, kapsule ali tablete. V magistrski nalogi smo izdelovali granule silicijevega dioksida z različnimi pomožnimi snovmi z metodo hitrovrtečega granulatorja z namenom izboljšanja stisljivosti delcev. Uporabili smo šest različnih na trgu dostopnih mezoporoznih silicijevih dioksidov (Syloid AL-1FP, Syloid XDP 3050, Aeroperl, Syloid 72FP, Syloid 3150, Syloid 244) s katerimi lahko izdelujemo trdne disperzije težko vodotopnih zdravilnih učinkovin. Granulate smo izdelali s pomočjo 11 različnih veziv (Sladkorji oziroma polioli: Laktoza, Izomalt, Maltitol, Manitol, Ksilitol. Polimeri: PVP K25, Avicel PH101, Vivapur 102, Hidroksipropil celuloza, PVP F90, Eudragit EPO). Granulatom smo merili pretočni čas, Carrov indeks, Hausnerjevo razmerje, izgubo mase pri sušenju, porazdelitev velikosti delcev in stisljivost. Na osnovi rezultatov teh analiz in lastnosti izdelanih tablet smo ugotavljali katero razmerje med silicijevim dioksidom in izbrano pomožno snovjo je najbolj optimalno. Granulate smo tabletirali in za vsako skupino pomožnih snovi (polimeri in polioli oziroma sladkorji), izbrali najboljšo. Najbolj optimalno razmerje silicijevega dioksida glede na vezivo iz obeh skupin je bilo 2:1. Pri tem razmerju smo najenostavneje stiskali tablete. Iz skupine polimerov je bilo najboljše vezivo PVP-K25 in iz skupine sladkorjev oziroma poliolov Izomalt. Končnim tabletam smo določili še čas razpadnosti. Vse tablete so razpadle v manj, kot 3 minutah in ustrezajo definiciji orodisperzibilnih tablet.

Language:Slovenian
Keywords:mezoporozni silicijev dioksid, granuliranje, tabletiranje, farmacevtska tehnologija, tablete
Work type:Master's thesis/paper
Organization:FFA - Faculty of Pharmacy
Year:2022
PID:20.500.12556/RUL-136795 This link opens in a new window
Publication date in RUL:21.05.2022
Views:761
Downloads:147
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Secondary language

Language:English
Title:Development of co-processed mesoporous silica with disaccharides, polyols and polymers for direct tableting
Abstract:
Silicon dioxide is a widely used excipient in pharmacy, most often as an additive to powder mixtures for better flow properties. As a carrier of active substances for the production of solid dispersions of poorly water-soluble active substances, it has so far been studied only in the field of research, where the researchers usually do not produce the final pharmaceutical form, capsule or tablet. In the Master's thesis, we produced granules of silicon dioxide with different excipients using the method of a high-shear granulator in order to improve the compressibility of particles. We used six different commercially available mesoporous silicon dioxides (Syloid AL-1FP, Syloid XDP 3050, Aeroperl, Syloid 72FP, Syloid 3150, Syloid 244) with which we can produce solid dispersions of poorly water-soluble active substances. The granules were made using eleven different binding agents (Sugars or polyols: Lactose, Isomalt, Maltitol, Mannitol, Xylitol. Polymers: PVP K25, Avicel PH101, Vivapur 102, Hydroxypropyl cellulose, PVP F90, Eudragit EPO). We measured flow time, Carr’s index, Hausner ratio, loss of mass on drying, and particle size distribution and compressibility of the tablets. Based on the results of these analyses and properties of the produced tablets, we established which ratio of silicon dioxide to the individual excipient is the most optimal. The granules were tableted and we selected the most appropriate one for each group of excipients (polymers and polyols or sugars). The most optimal ratio of silicon dioxide to binding agent from both groups was 2:1. This ratio produced tablets with the best properties. From the group of polymers, the best binder was PVP K25 and from the group of sugars or polyols was Isomalt. We also measured the disintegration time of the final product. All tablets disintegrated in less than 3 minutes so they meet the definition of orodispersible tablets.

Keywords:mesoporous silicon dioxide, granulation, tableting

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