Prikrivanje okusa tiaminijevega klorida, vgrajenega v mezoporozni silicijev dioksid z oblogo kopolimera metakrilne kisline

Prus, Barbara (author), Planinšek, Odon (mentor)

Tiamin spada v skupino vitaminov B, znan je tudi kot vitamin B1. Pomanjkanje tiamina lahko privede do različnih simptomov, ki se izražajo kot šibkost, utrujenost in težave z živci. Ker se ne shranjuje v telesu, je potrebno poskrbeti za zadosten vnos tega s hrano, če pa tudi to ni dovolj, lahko uporabljamo prehranska dopolnila ali zdravila. Tiamin tako najdemo v farmacevtskih oblikah, kot so kapsule, tablete, filmsko obložene tablete, peroralne raztopine in raztopine za injiciranje. Za izbrano učinkovino je značilno, da je grenkega okusa, zato smo ga v naši raziskavi skušali prikrivati. V ta namen smo izdelali dva osnovna vzorca, v katera smo vgradili tiaminijev klorid, nastale granule pa nato oblagali s polimerno oblogo za prikrivanje okusa. Pri prvem poskusu smo iz Syloid® 244FP in GALENIQ 800 naredili granule in jim vgradili učinkovino, v drugem poskusu pa smo učinkovino vgradili neposredno v Syloid® 244FP. Kot polimer za oblaganje smo izbrali kopolimer metakrilne kisline (Eudragit® E PO), ki smo ga na granule nanašali v različnih koncentracijah in količinah, tako da smo dobili granule, ki so bile bolj ali manj obložene. Po oblaganju granul smo vrednotili predvsem sproščanje učinkovine v mediju pH 1,2, v katerem se uporabljena polimerna obloga raztaplja, in v mediju pH 6,8, v katerem se polimerna obloga ne raztaplja. Na tak način smo preverili, ali je bilo naše oblaganje učinkovito in ali smo uspeli prikriti grenek okus učinkovine. Za bolj optimalen proces se je z vidika oblaganja izkazal poskus, ko smo učinkovino vgradili v Syloid® 244FP in dodali večji delež obloge, še vedno pa zakasnitev sproščanja učinkovine ni bila popolna, kar je bilo razvidno tudi iz posnetkov, ki smo jih naredili z vrstičnim elektronskim mikroskopom. Konvencionalne farmacevtske oblike niso primerne za pediatrične in geriatrične bolnike, raztopine za injiciranje pa so pogosto zelo invazivna metoda aplikacije zdravila, zato smo se odločili, da bomo iz obloženih granul skušali narediti orodisperzibilno tableto s tiaminijevim kloridom. Z vidika fizikalnih lastnosti narejenih vzorcev smo si za izdelavo orodispezibilne tablete izbrali vzorec, ki je bil narejen iz granul Syloid® 244FP in GALENIQ 800 učinkovine ter obložen z dvema različnima koncentracijama nanešene polimerne obloge. Na koncu nam je uspelo narediti orodisperzibilno tableto, ki je poleg osnovnih granul vsebovala še razgrajevalo in vezivo.

• Language: Slovenian
• Keywords: prikrivanje okusa, oblaganje, tiaminijev klorid, orodisperzibilna tableta
• Work type: Master's thesis/paper
• Organization: FFA - Faculty of Pharmacy
• Year: 2023
• PID: 20.500.12556/RUL-151138
• Publication date in RUL: 30.09.2023

Secondary language

• Language: English
• Title: Taste masking of thiamine chloride embedded in mesoporous silicon dioxide coated with methacrylic acid copolymer

Abstract

Thiamine is a B vitamin, also known as vitamin B1. A deficiency of thiamine can lead to a range of symptoms, including weakness, fatigue and nerve problems. As it is not stored in the body, it is important to ensure that adequate thiamine intake is obtained from food, and if this is not enough, dietary supplements or medication can be used. Thiamine can be found in pharmaceutical forms such as capsules, tablets, film-coated tablets, oral solutions and injectable solutions. The selected active substance is characterised by its bitter taste, which is why we tried to mask it in our study. For this purpose, two primary samples were produced, in which thiamine chloride was incorporated and the resulting granules were then coated with a polymeric coating to mask the taste. In the first experiment, Syloid® 244FP and GALENIQ 800 were made into granules and the active ingredient was incorporated, while in the second experiment the active ingredient was incorporated directly into Syloid® 244FP. The coating polymer chosen was a methacrylic acid copolymer (Eudragit® E PO), which was applied to the granules in different concentrations and quantities to obtain granules that were more or less coated. After coating the granules, the release of the active substance was evaluated mainly in pH 1,2 medium, in which the applied polymeric coating dissolves, and in pH 6,8 medium, in which the polymeric coating does not dissolve. In this way, we checked whether our coating was effective and whether we were able to mask the bitter taste of the active substance. The experiment where we incorporated the active substance into the Syloid® 244FP itself and added a higher proportion of the coating proved to be a more optimal process from the point of view of the coating, but still the delay in the release of the active substance was not perfect, as was also evident from the images we took with the in-line electron microscope. As conventional dosage forms are not suitable for pediatric and geriatric patients, and injectable solutions are often a very invasive method of drug administration, we decided to try to make an orodispersible thiamine chloride tablet from coated granules. In terms of the physical properties of the samples made, we chose a sample made from Syloid® 244FP and GALENIQ 800 granules of the active substance and coated with two different concentrations of the polymer coating to produce an orodispersible tablet. In the end, we managed to produce an orodispersible tablet that contained, in addition to the primary granules, a disintegrant and a binder.

• Keywords: taste masking, coating, thiamine chloride, orodispersible tablet