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Assessement and modulation of acamprosate intestinal absorption: comparative studies using in situ, in vitro (CACO-2 cell monolayers) and in vivo models

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Assessement and modulation of acamprosate intestinal absorption: comparative studies using in situ, in vitro (CACO-2 cell monolayers) and in vivo models

dc.contributor.author	Zornoza Sabina, Teodoro
dc.contributor.author	Cano Cebrián, María José
dc.contributor.author	Nalda Molina, Ricardo
dc.contributor.author	Guerri Sirera, Consuelo
dc.contributor.author	Granero Maciá, Luis
dc.contributor.author	Polache Vengut, Ana
dc.date.accessioned	2023-11-17T09:09:41Z
dc.date.available	2023-11-17T09:09:41Z
dc.date.issued	2004
dc.identifier.uri	https://hdl.handle.net/10550/91236
dc.description.abstract	The purpose of this study was to explore the intestinal absorption mechanism of acamprosate and to attempt to improve the bioavailability (BA) of the drug through modulation of its intestinal absorption using two enhancers (polysorbate 80 and sodium caprate) based on in situ, in vitro and in vivo models and comparing the results obtained. Intestinal transport of the drug, in the absence and in presence of polysorbate 80 (0.06, 0.28 and 9.6 mM) or sodium caprate (13 and 16 mM) was measured by using an in situ rat gut technique and Caco-2 cell monolayers. Additionally, the effect of sodium caprate on drug oral bioavailability, measured as urinary recovery, was quantified by performing in vivo experiments with the rat as animal model. Only sodium caprate was able to increase the absorption rate constant (ka) of acamprosate in the mid-intestine of the rats from 0.29 ± 0.07 h−1 in the absence of the promoter to 0.51 ± 0.19 h−1 in the presence of C10 16 mM, along with the apparent permeability (Papp) obtained in Caco-2 cells (around two-fold). However, the drug bioavailability in rats (around 20%) did not improve in the presence of any of the concentrations tested (13, 16 and 50 mM). It is concluded that acamprosate absorption likely occurs via paracellular pathway and can be enhanced by sodium caprate in situ and in vitro but not in vivo thus suggesting that although in situ and in vitro studies could be useful in early screening to select a potential promoter, in vivo studies in animal models are necessary to confirm the utility of the enhancer and to determine the influence of physiological variables.
dc.language.iso	eng
dc.relation.ispartof	European Journal of Pharmaceutical Sciences, 2004, vol. 22, num. 5, p. 347-356
dc.source	Zornoza Sabina, Teodoro Cano Cebrián, María José Nalda Molina, Ricardo Guerri Sirera, Consuelo Granero Maciá, Luis Polache Vengut, Ana 2004 Assessement and modulation of acamprosate intestinal absorption: comparative studies using in situ, in vitro (CACO-2 cell monolayers) and in vivo models European Journal of Pharmaceutical Sciences 22 5 347 356. https://doi.org/10.1016/j.ejps.2004.04.004
dc.subject	tecnologia farmacèutica
dc.subject	farmàcia
dc.title	Assessement and modulation of acamprosate intestinal absorption: comparative studies using in situ, in vitro (CACO-2 cell monolayers) and in vivo models
dc.type	journal article
dc.date.updated	2023-11-17T09:09:41Z
dc.identifier.doi	10.1016/j.ejps.2004.04.004
dc.identifier.idgrec	018992
dc.rights.accessRights	open access