Prediction of pharmacokinetic profile of valsartan in human based on in vitro uptake transport data.

Journal of Pharmacokinetics and Pharmacodynamics
Agnès PoirierThierry Lavé

Abstract

The aim of this study was to evaluate a strategy based on a physiologically based pharmacokinetic (PBPK) model for the prediction of PK profiles in human using in vitro data when elimination of compounds relies on active transport processes. The strategy was first applied to rat in vivo and in vitro data in order to refine the PBPK model. The model could then be applied to human in vitro uptake transport data using valsartan as a probe substrate. Plated rat and human hepatocytes, and cell lines overexpressing human OATP1B1 and OATP1B3 were used for in vitro uptake experiments. The uptake rate of valsartan was higher for rat hepatocytes (K (m,u) = 28.4 +/- 3.7 muM, V (max) = 1318 +/- 176 pmol/mg/min and P (dif) = 1.21 +/- 0.42 microl/mg/min) compared to human hepatocytes (K (m,u) = 44.4 +/- 14.6 microM, V (max) = 304 +/- 85 pmol/mg/min and P (dif) = 0.724 +/- 0.271 microl/mg/min). OATP1B1 and 1B3 parameters were correlated to human hepatocyte data using experimentally established relative activity factors (RAF). Resulting PBPK simulations using those in vitro data were compared for plasma (human and rat) and bile (rat) concentration-time profiles following i.v. bolus administration of valsartan. An uncertainty analysis indicated...Continue Reading

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