In this study, fexofenadine was used as a putative P-gp probe substrate to investigate the possible interaction with diosmin in rats by using in vitro, in situ and in vivo animal models. Moreover, pharmacokinetics of fexofenadine primarily depends on the P-gp activity without involvement of metabolism by cytochrome P450.
|Cell lines||The human epithelial cells COLO205|
|Preparation method||Cells were pretreated with various concentrations of fexofenadine or with PBS and were stimulated with TNF-α.|
|Incubation time||90 min|
|Animal models||Male Wistar rats|
|Formulation||pH 7.4 isotonic Dulbecco’s PBS (D-PBS) containing 25 mM glucose|
|Dosages||10 mg/ kg|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||10 mM in DMSO|
Effect of diosmin on the intestinal absorption and pharmacokinetics of fexofenadine in rats.
Neerati P, et al. Pharmacol Rep. 2015 Apr;67(2):339-44. PMID: 25712660.
Fexofenadine regulates nuclear factor-κB signaling and endoplasmic reticulum stress in intestinal epithelial cells and ameliorates acute and chronic colitis in mice.
Koh SJ, et al. J Pharmacol Exp Ther. 2015 Mar;352(3):455-61. PMID: 25538104.
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