Razvoj zrnc ibuprofena in paracetamola za uporabo v slamicah

Farina, Tilen (author), Planinšek, Odon (mentor)

Pediatrični in geriatrični bolniki se pogosto srečujejo z oteženim jemanjem peroralnih zdravil. Njihova nezmožnost požiranja večjih farmacevtskih oblik in potreba po individualizaciji odmerjanja je pripeljala do razvoja nove farmacevtske oblike - slamice. Slamico, v kateri se nahaja odmerek zdravila, omejujeta dva nepovratna ventila, odmerek pa zaužijemo z vlekom tekočine v smeri ust. V magistrskem delu smo oblagali kristale paracetamola in granule ibuprofena z dvojnimi oblogami, ki so imele vlogo prekrivanja neprijetnega okusa zdravilnih učinkovin in olajšanja praznjenja odmerka iz slamice. Kristale paracetamola smo obložili s primarno oblogo iz dimetilaminoetilnega metakrilatnega kopolimera (Eudragit® E PO), ki naj bi dobro prekrival neprijeten okus paracetamola. Za sekundarno oblogo, katere funkcija je bila olajšano praznjenje odmerka iz slamice, pa smo uporabili polivinil alkohol-polietilen glikol premreženi kopolimer (Kollicoat® IR) in dodatek še enega polimera v razmerju 1:1. Sekundarne obloge, ki smo jih testirali so Kollicoat® IR, Kollicoat® IR z dodanim SDS, Kollicoat® IR in PEG 200000, Kollicoat® IR in Kollidon® 90F, Kollicoat® IR in PVA 89k-98k ter Kollicoat® IR in PVA 85k-124k. Obložene delce smo ponovno granulirali s hitro vodotopnimi sladkorji z namenom dodatnega olajšanja praznjenja slamice in nato merili potreben podtlak za praznjenje. Ugotovili smo, da se pod najnižjim podtlakom in z najnižjim porabljenim volumnom tekočine praznijo delci, obloženi z Eudragit® E PO in Kollicoat® IR ter PVA 89k-98k. Modificirano oblogo iz Eudragit® E PO ter oblogo Kollicoat® IR ter PVA 89k-98k smo aplicirali tudi na predhodno razvite granule ibuprofena, jih ponovno granulirali s hitro vodotopnimi sladkorji in jim merili podtlak in volumen praznjenja iz slamice. Ugotovili smo, da so bili rezultati praznjenja odmerka ibuprofena iz slamice primerljivi paracetamolu. Kakovost prekrivanja neprijetnega okusa zdravilne učinkovine smo testirali s testiranjem sproščanja učinkovine. Ugotovili smo, da primarna obloga uspešno prikrije neprijeten okus obeh zdravilnih učinkovin.

• Language: Slovenian
• Keywords: praznjenje slamice, oblaganje, prekrivanje okusa, paracetamol, ibuprofen
• Work type: Master's thesis/paper
• Organization: FFA - Faculty of Pharmacy
• Year: 2021
• PID: 20.500.12556/RUL-125704
• Publication date in RUL: 04.04.2021

Secondary language

• Language: English
• Title: Development of ibuprofen and paracetamol granules for their use in straws

Abstract

Oral application is often difficult for pediatric and geriatric patients. A new single dose drug delivery system was created due to incapability of swallowing bigger solid dose formulations. With larger demands for individual drug dosing and easier drug application we have created a drinking straw. Straw already contains a pre-filled solid drug dose and is bounded by two non-return valves. The drug dose is consumed by sucking the liquid through the straw. In the master’s thesis we have double coated crystals of paracetamol and granules of ibuprofen to cover the unpleasant taste of the APIs and to facilitate emptying of the dose out of the straw. The primary coating polymer for crystals of paracetamol was dimethylaminoethyl methacrylate-copolymer (Eudragit® E PO) and its function was to mask the unpleasant taste of the API. Using polymer ratio 1:1 we combined polyvinyl alcohol/polyethylene glycol graft copolymer (Kollicoat® IR) and an addition of another polymer to make secondary coating. Its main function was to facilitate emptying of the dose out of the straw. We have tested 6 different secondary polymer coatings such as Kollicoat® IR, Kollicoat® IR with addition of SDS, Kollicoat® IR and PEG 200000, Kollicoat® IR and Kollidon® 90F, Kollicoat® IR and PVA 89k-98k and lastly Kollicoat® IR and PVA 85k-124k. In order to additionally facilitate emptying of the dose out of the straw we granulated the double coated paracetamol crystals with highly water-soluble sugars. We came to conclusion that the most effective polymer for emptying of the straw was combination of Eudragit® E PO and Kollicoat® IR with addition of PVA 89k-98k. We have altered the primary coating formulation of Eudragit® E PO suspension and applied it with the same secondary coating formulation (Kollicoat® IR with addition of PVA 89k-98k) to pre-made granules of ibuprofen. After granulation with highly water-soluble sugars, we measured vacuum and volume of water used for emptying the straw once again and came to conclusion that emptying of the straw was similar using both APIs. Quality of taste masking of both APIs was conducted with the analysis of the dissolution profile of both APIs. We came to conclusion that primary polymer coating is very effective at taste masking both APIs.

• Keywords: straw emptying, coating, taste masking, paracetamol, ibuprofen