Priprava dozirnih oblika s čvrstim disperzijama poli(etilen-glikola)

master's thesis

• Title (english): Preparation of solid dispersion dosage forms with poly(ethylene-glycol)
• Author: Iva Andrić
• Mentor: Krunoslav Žižek (mentor)
• Committee member: Krunoslav Žižek (predsjednik povjerenstva)
• Committee member: Domagoj Vrsaljko (član povjerenstva)
• Committee member: Juraj Šipušić (član povjerenstva)
• Granter: University of Zagreb; Faculty of Chemical Engineering and Technology; Zagreb
• Defense date and country: 2020-09-30, Croatia
• Scientific / art field, discipline and subdiscipline: TECHNICAL SCIENCES; Chemical Engineering

Abstract

Lurasidon-hidroklorid (LRS HCl) je djelatna tvar izrazito male topljivosti u vodenom mediju što otežava njegovu primjenu u liječenju psihičkih poremećaja. S ciljem povećanja njegove topljivosti, procesnom tehnologijom sušenja raspršivanjem pripravljene su čvrste disperzije djelatne tvari u matrici hidrofilnih polimera, poli(vinil-pirolidona) (PVP) i poli(etilen-glikola) (PEG). Dobivene čvrste disperzije karakterizirane su diferencijalnom pretražnom kalorimetrijom i rendgenskom difrakcijskom analizom praha. U pripravi raspadljivih tableta promjera 8 mm korištene su pripravljene čvrste disperzije i pomoćne tvari: manitol, natrijeva kroskarmeloza te mikrokristalna celuloza. Karakterizacija raspadljivih tableta podrazumijevala je ispitivanje ujednačenosti masa raspadljivih tableta, testiranje njihove raspadljivosti i tvrdoća, te određivanje sadržaja djelatne tvari. Vrijeme raspadljivosti za sve tablete manje je od 3 minute. In vitro ispitivanjima određena je topljivost djelatne tvari te su utvrđeni profili njezina oslobađanja iz raspadljivih tableta. Profili oslobađanja u laboratorijskom okruženju i uz prisutnosti McIlvaineovog pufera (pH = 3,8) ukazuju na bolju topljivost i brže oslobađanje djelatne tvari iz raspadljivih tableta pripravljenih iz čvrstih disperzija u odnosu na one koje sadrže čisti netretirani lurasidon-hidroklorid.

Abstract (english)

Lurasidone hydrochloride (LRS HCl) is an active pharmaceutical ingredient with extremely low aqueous solubility that makes this drug difficult to use for the treatment of psychotic disorders. For the purpose of drug solubility enhancement, solid dispersions were prepared by spray drying process technology in a matrix of hydrophilic polymers, poly(vinyl pyrrolidone) (PVP) and poly (ethylene glycol) (PEG). Derived solid dispersions were characterized by differential scanning calorimetry and X-ray powder diffraction analysis. Orally disintegrating tablets with 8 mm in diameter were prepared using solid dispersions and excipients: mannitol, sodium croscarmellose and microcrystalline cellulose. Characterization of orally disintegrating tablets (ODTs) implied testing the mass uniformity, its disintegration and hardness, and detecting the drug content. The disintegration time for all tablets is less than 3 minutes. Drug solubility and its release profiles were detected as well using in vitro dissolution tests. In vitro release profiles in the presence of McIlvaine buffer (pH = 3.8) indicate faster release of drug from disintegrating tablets prepared from solid dispersions in comparison to those containing pure and untreated lurasidone hydrochloride.

• Keywords: lurasidon-hidroklorid; poboljšanje topljivosti lijeka; čvrsta disperzija; sušenje raspršivanjem; raspadljiva tableta za usta; oslobađanje djelatne tvari
• Keywords (english): lurasidone hydrochloride; drug solubility enhancement; solid dispersion; spray drying; orally disintegrating tablet; drug release
• Language: croatian
• URN:NBN: urn:nbn:hr:149:121233
• Study programme: Title: Applied Chemistry - Graduate study; specializations in: Environmental chemistry and green technologies, Advanced materials and technologies, Applied organic chemistry; Course: Applied organic chemistry; Study programme type: university; Study level: graduate; Academic / professional title: magistar/magistra primijenjene kemije (magistar/magistra primijenjene kemije)
• Type of resource: Text
• File origin: Born digital
• Access conditions: Open access
• Created on: 2022-02-28 14:20:39