Poboljšanje topljivosti cinarizina u prisutnosti β-ciklodekstrina i njegovih derivata

master's thesis

• Title (english): Improvement of cinnarizine solubility in the presence of β-cyclodextrin and its derivatives
• Author: Morena Mikulec
• Mentor: Nives Galić (mentor)
• Committee member: Nives Galić (predsjednik povjerenstva)
• Committee member: Ines Primožič (član povjerenstva)
• Committee member: Davor Kovačević (član povjerenstva)
• Committee member: Sanda Rončević (član povjerenstva)
• Granter: University of Zagreb; Faculty of Science; (Department of Chemistry); Zagreb
• Defense date and country: 2023-12-12, Croatia
• Scientific / art field, discipline and subdiscipline: NATURAL SCIENCES; Chemistry

Abstract

Cinarizin je derivat piperazina koji posjeduje antihistaminsku aktivnost te djeluje kao blokator
kalcijevih kanala. Prema biofarmaceutskom sustavu klasifikacije djelatnih tvari cinarizin se
svrstava u drugu klasu koju karakteriziraju lijekovi slabe topljivosti i visoke permeabilnosti
kroz biološku membranu. Topljivost ovakvih djelatnih tvari poboljšava se ukoliko se
kompleksiraju s ciklodekstrinima. U sklopu ovog diplomskog rada provođenjem
solubilizacijskih ispitivanja istražen je utjecaj β-ciklodekstrina te njegova tri derivata
(hidroksipropil-β-ciklodekstrina, sulfobutileter-β-ciklodekstrina i nasumično metiliranog β-
ciklodekstrina) na topljivost cinarizina u vodenom mediju pri vrijednosti pH od 4,5 (simulirani
duodenalni medij). Razvijena je UV/Vis spektrofotometrijska metoda za kvantitativno
određivanje cinarizina u prisutnosti navedenih ciklodekstrina. Metoda je validirana prema
smjernicama koje propisuje Međunarodna konferencija o usklađivanju tehničkih zahtjeva za
registraciju farmaceutskih proizvoda za primjenu kod ljudi.

Abstract (english)

Cinnarizine is a piperazine derivative that acts as an antihistaminic and calcium channel
blocker. According to the biopharmaceutical classification system of active substances,
cinnarizine belongs to the second class, which is characterized by drugs with low solubility and
high permeability through the biological membrane. The solubility of these active substances
improves if they are complexed with cyclodextrins. The influence of β-cyclodextrin and its
three derivatives (hydroxypropyl-β-cyclodextrin, sulfobutylether-β-cyclodextrin, and randomly
methylated β-cyclodextrin) on the solubility of cinnarizine in aqueous medium at pH 4.5
(simulated duodenal medium) was investigated by conducting phase solubility analyses. An
UV/Vis spectrophotometry method was developed for the quantitative determination of
cinnarizine in the presence of the mentioned cyclodextrins. The method was validated
according to the guidelines prescribed by the International Conference on the Harmonization
of Technical Requirements for the Registration of Pharmaceutical Products for Human Use.

• Keywords: inarizin; ciklodekstrini; inkluzijski kompleksi; topljivost
• Keywords (english): cinnarizine; cyclodextrins; inclusion complexes; solubility
• Language: croatian
• URN:NBN: urn:nbn:hr:217:478399
• Study programme: Title: Graduate university studies in chemistry; specializations in: Graduate university studies in chemistry; Course: Graduate university studies in chemistry; Study programme type: university; Study level: graduate; Academic / professional title: sveučilišni/a magistar/magistra kemije (sveučilišni/a magistar/magistra kemije)
• Type of resource: Text
• File origin: Born digital
• Access conditions: Embargoed access; Embargo expiration date: 2025-12-12
• Created on: 2024-01-09 15:26:19