Orange juice increased the bioavailability of pravastatin, 3-hydroxy-3-methylglutaryl CoA reductase inhibitor, in rats and healthy human subjects

Concentration-Dependent Effect of Naringin on Intestinal Absorption of β1-Adrenoceptor Antagonist Talinolol Mediated by P-Glycoprotein and Organic Anion Transporting Polypeptide (Oatp)

“…Although intestinal mRNA and/or protein expression of various Oatp family members (e.g. Oatp1a1, Oatp1a4, Oatp1a5, Oatp2b1 and Oatp4a1) has been reported in rats, the localizations of these proteins have not been fully clarified yet, except for Oatp1a5 (38)(39)(40). We hypothesized that Oatp1a5, which is known to be expressed at the apical membrane, contributes to intestinal talinolol absorption in rats (40).…”

Differential Effect of Grapefruit Juice on Intestinal Absorption of Statins Due to Inhibition of Organic Anion Transporting Polypeptide and/or P-glycoprotein

“…However, because orange juice was reported to increase the bioavailability of pravastatin (100 mg/kg, same as the dose in our study) due to induction of Oatp in rats, pravastatin is likely absorbed by OATP/Oatp even at a high dose. 35 Pitavastatin reportedly showed no inhibition of P-gp-mediated digoxin transport even at 100 :M. 36 Therefore, the P-gp-mediated transport of pitavastatin is expected not to be saturated at high doses. Taken together, our results are expected to be consistent even if the concentrations of statins are different in the experiments.…”

Transporters and Drug-Drug Interactions: Important Determinants of Drug Disposition and Effects

“…By use of rats, it could be demonstrated in vivo that the AUC of celiprolol was decreased when hesperidin or orange juice was administered simultaneously into the duodenum (Uesawa and Mohri, 2008). In a study investigating the effects of orange juice on the pharmacokinetics of pravastatin in rats and healthy volunteers, Koitabashi et al (2006) demonstrated that the AUC of pravastatin was significantly increased in rats and humans treated with orange juice compared with the controls treated with water. The mechanism underlying this interaction remains to be elucidated.…”