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The novel in vitro method to calculate tissue-to-plasma partition coefficient in humans for predicting pharmacokinetic profiles by physiologically-based pharmacokinetic model with high predictability

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The novel in vitro method to calculate tissue-to-plasma partition coefficient in humans for predicting pharmacokinetic profiles by physiologically-based pharmacokinetic model with high predictability

Journal of Pharmaceutical Sciences

Fecha de publicación: 13 February 2020

DOI: https://doi.org/10.1016/j.xphs.2020.04.002

Autores: Kei Mayumi,, Miho Tachibana, Mei Yoshida, Shuichi Ohnishi, Takushi Kanazu, Hiroshi Hasegawa

Background: Proper prediction of human pharmacokinetic (PK) profiles can accelerate the compound selection in drug discovery. Recently, we reported a robust bottom-up physiologically-based pharmacokinetic (PBPK) approach (J Pharm Sci. 2019 Aug;108(8):2718-2727), which uses the in vivo rat distribution volume at the steady state (Vss) to determine human tissue-to-plasma partition coefficients (Kptissue).

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