| Avtor/Urednik | Klančar, Uroš; Legen, Igor; Kristl, Albin; Mrhar, Aleš | |
| Naslov | In vitro-in vivo korelacija (IVIVC) za učinkovine v pripravkih s podaljšanim sproščanjem, ki se intenzivno metabolizirajo ali absorbirajo s prenašalci v prebavilih | |
| Prevedeni naslov | In vitro in vivo correlation (IVIVC) for drugs in extended release formulations which are extensively metabolized or absorbed with transporters | |
| Tip | članek | |
| Vol. in št. | Letnik 61, št. 3 | |
| Leto izdaje | 2010 | |
| Obseg | str. 162-170 | |
| ISSN | 0014-8229 - Farmacevtski vestnik | |
| Jezik | slv | |
| Abstrakt | Na sproščanje učinkovin iz pripravkov s podaljšanim sproščanjem in absorpcijo iz prebavil vplivajo fizikalno kemijske lastnosti učinkovine, lastnosti farmacevtske oblike in fiziološke lastnosti gastrointestinalnega trakta (GIT). Nekatere učinkovine se v prebavilih lahko intenzivno metabolizirajo, ali pa na njih vplivajo razlioeni prenašalci. Oboje lahko znatno spremeni obseg absorpcije in posledioeno stopnjo in vitro-in vivo korelacije (IVIVC), ki predstavlja osnovo za napovedovanje plazemskih koncentracijskih profilov učinkovine na osnovi in vitro preskusov raztapljanja. V članku so glede na vrsto učinkovin, ki imajo različne lastnosti glede na biofarmacevtski sistem klasifikacije (BCS) in so vgrajene vpripravke s podaljšanim sproščanjem, opisani primeri vplivov metaboličnih procesov in prenašalcev na uspešnost doseganja IVIVC.The consumption of commercially available garlic supplements especially by chronic patients is continuously rising due to disease preventing effects, recognized in numerous preclinical and clinical studies. However, combining inconventional therapy utilized drugs with garlic phytochemicals can lead to serious pharmacokinetic and pharmacodynamic interactions. Namely, in some cases significant plasma profile changes of applied drugs and their metabolites, caused by intestinal and hepatic CYP inhibition and/or altered efflux membrane transporter activity, have been recognized in the presence of garlic phytochemicals leading to therapeutic failure or toxic side effects. There are also reports on pharmacodynamic interactions between drugs with narrow therapeutic window (i.e. warfarin) and garlic. Therefore combining garlic supplements and certain drugs should be closely monitored or in some cases even discontinued. | |
| Proste vsebinske oznake | IVIVC metabolizem prenašalci podaljšano sproščanje |