etoposide, a widely used anticancer drug, exhibits low and variable oral bioavailability mainly because of being substrate for the efflux transporter, p-glycoprotein (p-gp). therefore, the present study was aimed to investigate the effect of d-α-tocopherol polyethylene glycol 1000 succinate (tpgs) and peg 400 as p-gp inhibitors on the intestinal absorption of etoposide. everted sacs of rat smal...

This study attempted to clarify the material basis for the detoxification of Rhizoma Zingiberis (RZ) on aconitine, an analgesic drug, by quantitatively assessing the influence of RZ on the in vitro intestinal concentration of aconitine using an everted gut sac model and by qualitatively identifying the components in the RZ extract. To quantify aconitine in rat everted gut sacs, both an accurate...

The present study aimed at exploring the potential of the P-glycoprotein (P-gp) transporters as a barrier to the repaglinide (REG) epithelial permeability. In-vitro intestinal absorption models, the everted gut sac, and Caco-2 cell line, were used to study the possible role of P-gp in intestinal transport of REG. In the everted gut sacs, apparent permeability coefficients showed cargo concentra...

The present study aimed at exploring the potential of the P-glycoprotein (P-gp) transporters as a barrier to the repaglinide (REG) epithelial permeability. In-vitro intestinal absorption models, the everted gut sac, and Caco-2 cell line, were used to study the possible role of P-gp in intestinal transport of REG. In the everted gut sacs, apparent permeability coefficients showed cargo concentra...

PURPOSE The purpose of this study was to quantify the intestinal metabolism of midazolam, a CYP P450 substrate, usually used as a probe for the activity of the isoform CYP3A4/1 and to compare it with previous results obtained for other P450 substrates such as testosterone, dextromethorphan and bupropion, which show some specificities for different CYP isoforms. The aim was to shed light on the ...

Nicotinamide adenine dinucleotide (NADH) plays a major role in cellular metabolism and mitochondrial dysfunction and is thought that NAD+/NADH decrease neuronal degeneration and improve behavioral deficits. This potential use of NAD+ or NADH as neuroprotective drugs requires an insight on the pharmacokinetic properties of these compounds. For this reason, we assessed the absorption of NADH in t...

Cyclosporin A (CsA) is a P-glycoprotein (P-gp) inhibitor clinically used as an immunosuppressant. Itraconazole (ITZ) functions as an inhibitor of both the P-gp and CYP3A and is used as a fungistatic/fungicidal agent in human and veterinary medicine. The present studies were designed to investigate the effects of CsA and ITZ on 1) intestinal permeability of amlodipine (a calcium channel blocker ...