Effects of capsaicin on pharmacokinetics of pitavastatin in rats

Abstract

1. Capsaicin (CAP) is the primary pungent principle in peppers and an inhibitor of CYP3A subfamily and P-gp. 2. Pitavastatin is mainly metabolized via glucuronidation and metabolism by hepatic CYPs is minimal. Pitavastatin is taken up by Oatp1b2 (encoded by Slco1b2) in rat. 3. The pharmacokinetics results showed that AUC and Cmax in the group pre-treated with 3 mg/kg/d CAP were increased by 1.2 fold and 1.6 fold; AUC and Cmax in the group pre-treated with 8 mg/kg/d CAP were increased by 2.1 fold (p<0.05) and 2.9 fold (p<0.05); AUC and Cmax in the group pre-treated with 25 mg/kg/d CAP were increased by 2.0 fold and 1.9 fold. The RT-PCR data indicated that pretreatment with CAP had little influence on the mRNA expression level of Slco1b2 in liver. These results demonstrated that chronic ingestion of CAP increases the bioavailability of pitavastatin in rat and that Oatp1b2 gene expression in rat liver is hardly effected by CAP.

Effect of Nanonized Chrysin on Fexofenadine Pharmacokinetics Mediated by P-Glycoprotein in Rats

“…These findings provide in vivo evidence that NCH might have increased the bioavailability of fexofenadine via the inhibition of P-gp mediated drug efflux during the absorption phase in the intestine. Moreover, the results obtained in our study were comparable to previous reports where piperine [6], diosmin [23] substantially enhanced the bioavailability of fexofenadine through the inhibition of P-gp mediated efflux in intestine of rats. We have limited data regarding the pharmacokinetics and drug interactions of chrysin in humans; however, animal experiments showed that chrysin can influence the pharmacokinetics of different compounds (e.g., caffeine, nitrofurantoin, and paracetamol) due to its interactions with CYP enzymes and BCRP [24,7,25,26].…”

Effects of Phytochemical P-Glycoprotein Modulators on the Pharmacokinetics and Tissue Distribution of Doxorubicin in Mice

“…In this study, the modulatory effects of the phytochemicals on P-gp were evaluated in vivo by using doxorubicin as a model P-gp substrate. Although alteration in oral bioavailabilities of various drugs by combination with the pungent phytochemicals have been well demonstrated [ 33 , 34 , 35 , 36 , 37 , 38 , 39 , 40 ], no information is available regarding their effects on tissue distribution of P-gp substrates. Therefore, the tissue distribution of doxorubicin after intravenous injection were evaluated in mice pretreated with piperine, capsaicin, or [6]-gingerol.…”