P-Glycoprotein (PGP) is nonuniformly distributed along the gastrointestinal (GI) tract; however, the data regarding regional differences in PGP function in the intestine are controversial. The aim of this work was to investigate the role of PGP efflux in region-specific absorption of talinolol from the GI tract in rats. Plasma talinolol concentrations were measured after several modes of admini...

Bioavailability of talinolol, a beta(1)-adrenergic receptor antagonist, was enhanced by coadministration with grapefruit juice (GFJ) in rats, whereas GFJ ingestion markedly reduced the absorption of talinolol in humans. Because our recent study indicated that the inhibitory effect of GFJ on organic anion-transporting polypeptide (Oatp)- and P-gp-mediated talinolol absorption depends on the conc...

The current study evaluates the ultra high performance liquid chromatography (UHPLC) method for the quantification of talinolol in lipid-based formulations. A simple, rapid, reliable and precise reversed phase UHPLC method has been developed and validated according to the regulatory guidelines, which was composed of isocratic mobile phase; acetonitrile and phosphate buffer saline (pH 4.5) with ...

Placental syncytiotrophoblasts are known to express the efflux transporter proteins P-glycoprotein (ABCB1) and multidrug resistance-associated protein 2 (ABCC2), which are supposed to be a functional part of the human placental barrier. With advancing gestational age, expression of ABCB1 decreases progressively, whereas ABCC2 is more expressed. To evaluate to which extent they contribute to pla...

In the present study, we successfully downscaled, for the first time, the in situ intestinal perfusion technique with mesenteric blood sampling from rat to mouse. To evaluate the feasibility of this approach, we assessed the apparent permeability (P(app)) of mouse intestine for a set of marker compounds [atenolol, paracellular transport; metoprolol, transcellular transport; talinolol, P-glycopr...

Talinolol is a beta1-selective adreno receptor antagonist well known for its Cardio protective and antihypertensive activity. beta blocker. In biopharmaceutical classification system the drugs which come under class II are characterized by more membrane permeability, less dissolution rate. poor aqueous solubility drug leads to bioavailability. So, aimed of this study was develop immediate relea...

To estimate the clinical impact of pharmacokinetic modulation via breast cancer resistance protein (BCRP), in vivo approaches in nonclinical settings are desired in drug development. Clinical observation has identified curcumin as a promising candidate for in vivo selectiveBCRP inhibition, in addition to several well-known inhibitors, such as lapatinib and pantoprazole. This study aimed to conf...

Membrane destabilizing properties and increased efflux of doxorubicin from liposomes caused by basic butylated methacrylate copolymer (BBMC), better known under its commercial trade name EUDRAGIT E, have been described in the scientific literature. Here, we investigated the effect of BBMC on suspended and filter-grown Caco2 cells with respect to apical-to-basal transport and membrane permeabili...