Vpliv pektina in saharoze na sproščanje paracetamola iz ogrodnih tablet : [enoviti magistrski študij farmacija]

Rus, Jasna (author), Bogataj, Marija (mentor)

Ogrodne tablete so peroralna farmacevtska oblika, s pomočjo katere doseţemo podaljšano sproščanje, najpogosteje z nabrekanjem hidrofilnega polimera v stiku s črevesnimi sokovi. Ob prehodu skozi gastrointestinalni trakt je taka tableta podvrţena različnim pogojem (pH, peristaltika), na sproščanje pa lahko vplivata tudi zauţita hrana in pijača. Namen te naloge je bil opredeliti vpliv kombinacije različnih koncentracij saharoze in pektina v mediju, na sproščanje iz ogrodnih tablet s hidroksipropilmetil celulozo (HPMC). Poskuse smo izvedli na dveh različnih vrstah tablet, ki smo jih izdelali sami. Tablete so vsebovale paracetamol (modelna učinkovina), mikrokristalno celulozo, magnezijev stearat ter HPMC. Polovica tablet je vsebovala HPMC vrste Metolose® 65SH-4000, druga polovica pa Metolose® 90SH-100 000 SR. Poskuse smo izvajali na pretočnem sistemu s kroglicami. Vodni mediji so vsebovali 0,002M HCl ter saharozo ali pektin v različnih koncentracijah ter kombinacijah. Mediji s saharozo so vsebovali saharozo v koncentracijah 150, 200, 250 ali 300 g/L, medij s pektinom je vseboval koncentracijo pektina 5 g/L, kombinirani mediji pa so vsebovali navedene koncentracije saharoze in koncentracije pektina 1, 2 ali 5 g/L. Ugotovili smo, da uporabljeni vrsti HPMC različno reagirata na povišanje koncentracije saharoze. HPMC Metolose® 65SH-4000 je na višanje koncentracije saharoze bolj občutljiva, do hitrega sproščanja iz tablet s to vrsto HPMC je prišlo ţe pri koncentraciji saharoze 200 g/L, medtem ko so tablete s HPMC (Metolose® 90SH-100 000 SR) izkazovale hitro sproščanje šele v mediju s koncentracijo saharoze 300 g/L. Koncentracija pektina 5 g/L v mediju na sproščanje iz tablet s HPMC Metolose® 65SH-4000 ni vplivala, pri tabletah s HPMC Metolose® 90SH-100 000 SR pa se je hitrost sproščanja nekoliko povečala. Sproščanje paracetamola v kombiniranih medijih, je bilo glede na profil sproščanja v mediju s saharozo spremenjeno pri obeh vrstah tablet enako. S povečevanjem koncentracije pektina do 2 g/L se je hitrost sproščanja paracetamola zmanjševala. Pri koncentraciji pektina 5 g/L pa se je sproščanje ţe občutneje upočasnilo.

• Language: Slovenian
• Keywords: pektin saharoza ogrodne tablete hidroksipropilmetil celuloza sproščanje
• Work type: Master's thesis/paper
• Typology: 2.09 - Master's Thesis
• Organization: FFA - Faculty of Pharmacy
• Place of publishing: Ljubljana
• Publisher: [J. Rus]
• Year: 2014
• Number of pages: III, 58 f.
• PID: 20.500.12556/RUL-121095
• UDC: 547.458.2+615.453(043.3)
• COBISS.SI-ID: 3616881
• Publication date in RUL: 30.09.2020

Secondary language

• Language: English
• Title: The influence of pectin and sucrose on the release of paracetamol from modified-release tablets

Abstract

Matrix tablet is an oral dosage form, which ensures prolonged release, most frequently by swelling of hydrophilic polymer when it comes in contact with gastric juice. While the tablet passes the gastrointestinal tract it is exposed to different conditions that could affect drug release. The release is also influenced by food and drinks one consumes. The main goal of this thesis was to define effects of different concentrations of sucrose and pectin in media on drug release from matrix tablets with hydroxypropylmethyl cellulose (HPMC). The experiments were performed on two different types of tablets, which we made ourselves. Tablets contained paracetamol as a model substance, microcrystalline cellulose, magnesium stearate and HPMC. One type of the tablets contained HPMC Metolose® 65SH-4000, and the other type contained HPMC Metolose® 90SH-100 000 SR. The experiments were performed on a flow-through system with glass beads. Aqueous medium contained 0,002 M HCl and sucrose and pectin in different concentrations and combinations. Media with sucrose contained sucrose in concentrations 150, 200, 250 or 300 g/L, the medium with pectin contained a concentration of pectin 5 g/L, and the combined media contained above cited concentrations of sucrose and pectin in concentrations 1, 2 or 5 g/L. We concluded that both types of HPMC react differently when the concentration of sucrose increases. HPMC Metolose® 65SH-4000 is more susceptible to increasing the concentration of sucrose; drug release from tablets was fast, starting at concentration of sucrose 200 g/L. HPMC Metolose® 90SH-100 000 SR tablets started to release faster at the concentration 300 g/L of sucrose in the medium. On one hand, adding only pectin to the medium at concentration 5 g/L did not affect the release from tablets with HPMC Metolose® 65SH-4000. On the other, this concentration of pectin slightly increased the release rate from tablets with HPMC Metolose® 90SH-100 000. The release of paracetamol in sucrose media was changed (for both types of tablets) when we added pectin. With increasing the concentration of pectin up to 2 g/L in sucrose media, the release rate of paracetamol decreased. Concentration 5 g/L of added pectin significantly slowed down the release.

• Keywords: pectin sucrose matrix tablets hydroxypropylmethyl cellulose release