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- W2022885537 abstract "Background and Objective Surfactants used in pharmaceutical formulations can modulate drug absorption by multiple mechanisms including inhibition of intestinal P-glycoprotein (P-gp). Our objective was to analyze the effect of 2 surfactants with different affinity for P-gp in vitro on the intestinal absorption and bioavailability of the P-gp substrate talinolol in humans. Methods In vitro, the influence of surfactants on talinolol permeability was studied in Caco-2 cells. In vivo, an open-label 3-way crossover study with 9 healthy male volunteers was performed. Subjects were intubated with a 1-lumen nasogastrointestinal tube. The study solution, containing either talinolol (50 mg), talinolol and D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) (0.04%), or talinolol and Poloxamer 188 (0.8%), was administered through the tube. Results TPGS, but not Poloxamer 188, inhibited the P-gp-mediated talinolol transport in Caco-2 cells. In healthy volunteers TPGS increased the area under the plasma concentration-time curve with extrapolation to infinity (AUC0-∞) of talinolol by 39% (90% confidence interval, 1.10–1.75) and the maximum plasma concentration (Cmax) by 100% (90% confidence interval, 1.39–2.88). Poloxamer 188 did not significantly alter the AUC0-∞ or Cmax of talinolol. Conclusions This in vivo intraduodenal perfusion study showed that low concentrations of TPGS, close to the concentrations that showed P-gp inhibition in vitro, significantly increased the bioavailability of talinolol. The study design excluded modulation of solubility by TPGS and unspecific surfactant-related effects. The latter was supported by the absence of modulation of the talinolol pharmacokinetics by Poloxamer 188, which does not modulate P-gp. Therefore we consider intestinal P-gp inhibition by TPGS as the major underlying mechanism for the increase in talinolol bioavailability. Clinical Pharmacology & Therapeutics (2005) 77, 24–32; doi: 10.1016/j.clpt.2004.09.001" @default.
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- W2022885537 date "2005-01-01" @default.
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- W2022885537 title "P-glycoprotein and surfactants: Effect on intestinal talinolol absorption" @default.
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- W2022885537 doi "https://doi.org/10.1016/j.clpt.2004.09.001" @default.
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