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Pregled izsledkov raziskav prenasičenja in vitro in in vivo ter opredelitev vpliva lastnosti hidroksipropilmetilceluloze na zaviranje obarjanja učinkovin
ID Gorenc, Natalija (Author), ID Bogataj, Marija (Mentor) More about this mentor... This link opens in a new window, ID Felicijan, Tjaša (Comentor)

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Abstract
Prenasičenje je stanje, pri katerem je koncentracija učinkovine v raztopini višja od njene topnosti. To stanje lahko pozitivno vpliva na povečanje biološke uporabnosti zdravilnih učinkovin, ki so v vodi slabo topne. Za vzdrževanje prenasičenega stanja in preprečevanje obarjanja učinkovin se uporabljajo različne pomožne snovi, kot so polimeri, površinsko aktivne snovi in ciklodekstrini. Hidroksipropilmetilceluloza, ki spada v skupino celuloznih polimerov, predstavlja enega od pogosto uporabljenih zaviralcev obarjanja. Pri pregledu literature smo se osredotočili na vpliv hidroksipropilmetilceluloze na podaljševanje in vzdrževanje prenasičenega stanja različnih učinkovin, še posebej tistih z nizko topnostjo, ki spadajo v BCS razred II in IV. Predhodno raztopljeni HPMC dodan v medij za raztapljanje podaljšuje in povečuje stopnjo prenasičenja natrijevega ibuprofenata, v primerjavi s trdnim HPMC ali formulacij brez HPMC. Učinek HPMC je še posebej izrazit pri lipofilnih učinkovinah z višjim logP, kjer znatno izboljša absorpcijo in najvišje plazemske koncentracije. Različni tipi in koncentracije HPMC lahko vplivajo na doseganje višjih koncentracij in stopnje prenasičenja učinkovin v formulacijah. Mehanizmi, kot so tvorba vodikovih vezi, sterične ovire, viskoznost in vpliv molekulske mase pa so ključni pri zaviranju obarjanja in vzdrževanje prenasičenega stanja.

Language:Slovenian
Keywords:HPMC, prenasičenje, zaviralci obarjanja, test raztapljanja
Work type:Master's thesis/paper
Organization:FFA - Faculty of Pharmacy
Year:2024
PID:20.500.12556/RUL-164713 This link opens in a new window
Publication date in RUL:08.11.2024
Views:75
Downloads:10
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Secondary language

Language:English
Title:Examination of in vitro and in vivo supersaturation studies’ results and assessment of the hydroxypropyl methylcellulose properties effects on drugs precipitation inhibition
Abstract:
Supersaturation is a condition in which the concentration of the drug in the solution is higher than its solubility. This situation can have a positive effect on increasing the bioavailability of drugs that are poorly soluble in water. To maintain a supersaturated state and prevent precipitation of drugs, various excipients are used, such as polymers, surfactants and cyclodextrins. Hydroxypropylmethylcellulose, which belongs to the group of cellulose polymers, is one of the commonly used precipitation inhibitor. When reviewing the literature, we focused on the effect of hydroxypropylmethylcellulose on prolonging and maintaining the supersaturated state of various drugs, especially those with low solubility, which belong to BCS class II and IV. Predissolved HPMC added to the dissolution medium prolongs and increases the degree of supersaturation of ibuprofen sodium, compared to solid HPMC or formulations without HPMC. The effect of HPMC is particularly pronounced for lipophilic drugs with a higher logP, where it significantly improves absorption and peak plasma concentrations. Different types and concentrations of HPMC can influence the achievement of higher concentrations and degrees of supersaturation of drugs in formulations. Mechanisms such as hydrogen bonding, steric hindrance, viscosity and effect of molecular weight are key in inhibiting precipitation and maintaining the supersaturated state.

Keywords:HPMC, supersaturation, precipitation inhibition, dissolution test

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