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Evaluation of the appropriate time range for estimating the apparent permeability coefficient (P(app)) in a transcellular transport study. | LitMetric

Evaluation of the appropriate time range for estimating the apparent permeability coefficient (P(app)) in a transcellular transport study.

Int J Pharm

Research Institute of Pharmaceutical Sciences, Musashino University, 1-1-20 Shinmachi, Nishitokyo-shi, Tokyo 202-8585, Japan. Electronic address:

Published: November 2015

AI Article Synopsis

  • - The study investigates how the apparent permeability coefficient (Papp) of a compound changes over time, specifically focusing on the lag phase and subsequent linear behavior in concentration profiles.
  • - A 3-compartment model is employed to describe the concentration in the receiver side (C3), revealing complexities in the relationship between time and concentration that include two steady states.
  • - The findings suggest that the optimal time range for evaluating Papp is between specific intervals defined by the rate constants α and β, indicating that the sink condition complicates uniform definitions of linearity in concentration measurements.

Article Abstract

In a transcellular transport study, the apparent permeability coefficient (Papp) of a compound is evaluated using the range by which the amount of compound accumulated on the receiver side is assumed to be proportional to time. However, the time profile of the concentration of the compound in receiver (C3) often shows a lag time before reaching the linear range and later changes from linear to steady state. In this study, the linear range needed to calculate Papp in the C3-time profile was evaluated by a 3-compartment model. C3 was described by an equation with two steady states (C3=A3(1-e(-αt))+B3(1-e(-βt)), α>β), and by a simple approximate line (C3=A3-A3×αt) in the time range of 3/α

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Source
http://dx.doi.org/10.1016/j.ijpharm.2015.09.035DOI Listing

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