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Izdelava in vrednotenje hitro disperzibilnih praškastih formulacij slabo vodotopnih antioksidantov koencima Q10 in resveratrola
ID Hren, Anja (Author), ID Zvonar Pobirk, Alenka (Mentor) More about this mentor... This link opens in a new window

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Abstract
Nizka peroralna biološka uporabnost kot posledica nizke topnosti učinkovin v vodi predstavlja vedno večji izziv. Eden izmed pristopov, kako izboljšati raztapljanje in s tem biološko uporabnost slabo vodotopnih učinkovin, je tudi izdelava različnih formulacij na osnovi lipidov. Slednje so lahko v obliki emulzij ali talin, za pretvorbo v trdno stanje pa lahko uporabimo pristope, kot so (mikro)kapsuliranje, direktna adsorpcija na mezoporozne nosilce, granuliranje in druge. Namen magistrske naloge je bil izdelati trdno formulacijo slabo vodotopnih antioksidantov resveratrola in koencima Q10, ki se bo hitro dispergirala v vodnem mediju in izboljšala topnost vgrajenih antioksidantov. Tako resveratrol kot tudi koencim Q10 po biofarmacevtskem klasifikacijskem sistemu uvrščamo v II. razred, saj imata oba slabo vodotopnost in dobro permeabilnost. Za izboljšanje dispergiranja obeh antioksidantov v vodni fazi smo uporabili metodo emulgiranja, in sicer smo resveratrol vgradili v emulzije tipa olje-v-vodi, ki so kot oljno fazo vsebovale srednje- (Captex 355) ali dolgoverižni (olivno olje) triglicerid. Pri koencimu Q10 smo zaradi nizke temperature tališča kot oljno fazo uporabili talino koencima Q10. Kot najboljši emulgator se je v obeh sistemih izkazal Tween 80. Vse emulzije smo pretvorili v hitro disperzibilne prahove, pri čemer smo kot trdni nosilec uporabili mezoporozni Syloid 244 FP. Emulzije z resveratrolom smo solidificirali s pomočjo sušenja z razprševanjem. Pri formulacijah s koencimom Q10 pa smo uporabili tudi ročno granuliranje s talino ter granuliranje s talino v hitro vrtečem mešalniku.

Language:Slovenian
Keywords:disperzibilne formulacije, emulgiranje, sušenje z razprševanjem, granuliranje s talinami, koencim Q10, resveratrol
Work type:Master's thesis/paper
Organization:FFA - Faculty of Pharmacy
Year:2022
PID:20.500.12556/RUL-141030 This link opens in a new window
Publication date in RUL:22.09.2022
Views:431
Downloads:49
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Secondary language

Language:English
Title:Production and characterisation of rapidly dispersible powders with poorly water-soluble antioxidants coenzyme Q10 and resveratrol
Abstract:
Low oral bioavailability as a consequence of the low solubility of active compounds in water poses an increasing challenge. One of the approaches how to improve the dissolution and thus the bioavailability of poorly water-soluble active compounds is also the production of various lipid-based formulations. The latter can be in the form of emulsions or melts. Different approaches can be used for conversion to a solid state, such as (micro)encapsulation, direct adsorption on mesoporous carriers, granulation, and others. The purpose of the master's thesis was to produce a solid formulation of poorly water-soluble antioxidants of resveratrol and coenzyme Q10 which will disperse rapidly in an aqueous medium and improve the solubility of embedded antioxidants. According to the biopharmaceutical classification system, both resveratrol and coenzyme Q10 are classified in II. class because both have poor water solubility and good permeability. To improve the dispersibility of both antioxidants in the aqueous phase, we used the emulsification method, namely resveratrol was incorporated into oil-in-water emulsions which contained medium- (Captex 355) or long-chain (olive oil) triglyceride as the oil phase. Because of the low melting point of coenzyme Q10, the melt of coenzyme Q10 was used as the oil phase in its case. Tween 80 proved to be the best emulsifier in both systems. All emulsions were converted to fast dispersible powders using mesoporous Syloid 244 FP as a solid support. Resveratrol emulsions were solidified by spray drying. In coenzyme Q10 formulations, we used also manual melt granulation and melt granulation in a high-shear mixer.

Keywords:dispersible formulations, emulsification, spray drying, melt granulation, coenzyme Q10, resveratrol

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