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Primerjalno vrednotenje sproščanja ibuprofena in naproksena iz različnih trdnih farmacevtskih oblik
ID Keršmanc, Lina (Author), ID Bogataj, Marija (Mentor) More about this mentor... This link opens in a new window, ID Felicijan, Tjaša (Co-mentor)

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Abstract
Sproščanje učinkovine iz trdne farmacevtske oblike je prva in pomembna stopnja v procesih LADME sistema in ga delimo na takojšnje ter prirejeno (zakasnelo, pulzirajoče in podaljšano) sproščanje. V sklopu raziskovalnega dela smo vrednotili različne vplive na sproščanje ibuprofena in naproksena iz na trgu dostopnih tablet s takojšnjim (ibuprofen 400 in 600 mg tablete in naproksen 375 mg tablete), zakasnelim (naproksen 500 mg tablete) in podaljšanim (ibuprofen 800 mg tablete – ogrodne tablete) sproščanjem v napravi z veslastimi mešali (USP 2), napravi s pretočno celico (USP 4) in pretočnem sistemu s steklenimi kroglicami. Pri naproksen 500 mg tabletah omogoča zakasnelo sproščanje Eudragit L, medtem ko podaljšano sproščanje ibuprofena iz 800 mg tablet omogoča ksantanski gumi, ki ob stiku z molekulami vode močno nabreka in tvori gelsko plast, preko katere se z difuzijo ali erozijo sprošča učinkovina. Osnova za teste sproščanja so bile individualne monografije posameznih tablet iz Ameriške farmakopeje, ki pa smo jih, z namenom proučevanja različnih vplivov, v nadaljevanju ustrezno optimizirali. S primerjalnim vrednotenjem sproščanja ibuprofena in naproksena iz tablet s takojšnjim sproščanjem po farmakopejski metodi smo ugotovili, da je sproščanje ibuprofena bistveno hitrejše kot sproščanje naproksena, obe vrsti tablet pa ustrezata farmakopejskim zahtevam za ustreznost testa sproščanja. Pri vrednotenju različnih vplivov v napravi USP 2 smo ugotovili, da je pri sproščanju naproksena prisoten čas zakasnitve sproščanja in le-tega zmanjšajo povečanje koncentracije fosfatnega pufra, predhodno sproščanje v 0,1 M HCl ter povečanje hitrosti vrtenja mešal. Časa zadrževanja v 0,1 M HCl ne vpliva na sproščanje naproksena iz gastrorezistentnih tablet v USP 2, kot tudi ne na sproščanje ibuprofena iz tablet s takojšnjim sproščanjem v USP 4. Hitrost vrtenja mešal naprave USP 2 poveča hitrost sproščanja tako naproksena iz gastrorezistentnih tablet kot tudi ibuprofena iz ogrodnih tablet. Vpliv farmakopejskih metod za menjavo medija (metod A in B) v USP 2 je izražen pri ibuprofen ogrodnih tabletah, medtem ko izbira metode ne vpliva na sproščanje naproksena iz gastrorezistenitnih tablet. pH medija vpliva na nabrekanje ogrodnih tablet. Na sproščanje ibuprofena iz ogrodnih tablet se je kot najbolj učinkovit vpliv izkazala mehanska sila, in sicer tista, povzročena z gibanjem tablete po plasti steklenih kroglic v pretočnem sistemu. Z erozijo se gelska plast, v kateri je dispergirana učinkovina, odplavlja, zato je zaradi dodatne mehanske sile odstotek sproščenega ibuprofena iz ogrodnih tablet večji pri enakih testih v pretočnem sistemu kot v napravi USP 2.

Language:Slovenian
Keywords:ibuprofen, naproksen, sproščanje, ksantanski gumi
Work type:Master's thesis/paper
Organization:FFA - Faculty of Pharmacy
Year:2020
PID:20.500.12556/RUL-117440 This link opens in a new window
Publication date in RUL:10.07.2020
Views:1177
Downloads:420
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Secondary language

Language:English
Title:Comparative evaluation of ibuprofen and naproxen release from different solid dosage forms
Abstract:
Drug release from solid dosage form is first and important step in the process of LADME system. Release of drug can be either immediate or modified (delayed, pulsed and prolonged). In experimental work we were evaluating different influences on ibuprofen and naproxen release from commercially available tablets with immediate (ibuprofen 400 and 600 mg tablets and naproxen 375 mg tablets), delayed (naproxen 500 mg tablets) and prolonged (ibuprofen 800 mg tablets – matrix tablets) release by performing dissolution tests in paddle apparatus (USP 2), flow-through cell (USP 4) and flow-through system with glass beads. In naproxen 500 mg tablets delayed release is achieved by using polymer Eudragit L, while xanthan gum in ibuprofen 800 mg tablets prolongs drug release. In contact with water xanthan gum molecules highly swell and form gel layer from which drug is released either by diffusion or erosion. Dissolution tests were first performed as they are defined in each individual monograph in United States Pharmacopeia (USP) and then optimized with the purpose of evaluating different influences. With comparable evaluation of ibuprofen and naproxen release from immediate release tablets by pharmacopeial methods we determined that release of ibuprofen is much faster than release of naproxen and both types of tablets meet the pharmacopeial requirements for im-mediate release tablets. With evaluation of different influences in USP 2 lag time in naproxen dissolution profile was observed and it can be lowered by higher concentration of phosphate buffer, previous dissolution in 0,1 M HCl and increasing the speed of paddles in USP 2. Retention time in 0,1 M HCl does not influence naproxen release from delayed release tablets in USP 2 or ibuprofen release from immediate release tablets in USP 4. Paddle stirring speed in USP 2 increases release kinetics not only of naproxen from delayed release tablets but also of ibuprofen from matrix tablets. Difference between pharmacopeial methods of dissolution medium change (methods A and B) in USP 2 was observed in ibuprofen dissolution tests, while there was no difference between the two methods in release of naproxen from delayed release tablets. pH of medium has an impact on swelling of tablets with xanthan gum. The biggest influence on ibuprofen release from matrix tablets has mechanical stress, the one caused by glass beads in flow-through system with glass beads - glass beads cause erosion of gel layer in which drug is dispersed. Because of additional mechanical stress in flow-through system with glass beads percent of released ibuprofen is higher in flow-through system with glass beads than in USP 2.

Keywords:ibuprofen, naproxen, release, xanthan gum

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