2006
DOI: 10.1248/bpb.29.522
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Pharmacokinetic Analysis of Transcellular Transport of Quinidine across Monolayers of Human Intestinal Epithelial Caco-2 Cells

Abstract: Quinidine, a tertiary amine compound with a site of ionization with a pK a value of pH 8.8, is classified as a type IA antiarrhythmic drug, and has been used for the management of ventricular arrhythmias.1,2) The drug is absorbed rapidly and almost entirely after oral administration, and is detected in the plasma within 15 min.3) Quinidine binds to both albumin and a 1 -acid glycoprotein, and the proportion that binds to plasma protein is 70 to 95%. 4) However, its apparent volume of distribution is quite larg… Show more

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Cited by 22 publications
(27 citation statements)
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“…2,7) In the present study, to confirm the involvement of the cation transport system in intestinal absorption of quinidine, we investigated the membrane transport mechanism of quinidine using another intestinal epithelial cell line, LS180. This cell line possesses characteristics of the small intestine (e.g., expression of microvillus), and has also been used as an in vitro model of the intestine.…”
Section: Discussionmentioning
confidence: 98%
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“…2,7) In the present study, to confirm the involvement of the cation transport system in intestinal absorption of quinidine, we investigated the membrane transport mechanism of quinidine using another intestinal epithelial cell line, LS180. This cell line possesses characteristics of the small intestine (e.g., expression of microvillus), and has also been used as an in vitro model of the intestine.…”
Section: Discussionmentioning
confidence: 98%
“…2,7) The cellular uptake of quinidine in Caco-2 cells grown on plastic dishes was temperature-dependent, and markedly increased by alkalization of the apical medium at 37°C.…”
Section: Discussionmentioning
confidence: 99%
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“…12,13) In addition, several UGTs, such as UGT1A1, 1A6, and 2B7, are expressed in Caco-2 cells, and the expression of some UGTs is induced by aromatic hydrocarbon receptor (AhR) ligands, such as b-naphthoflavone (b-NF).…”
mentioning
confidence: 99%