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Purpose. To assess the degree to which the maximum unboundconcentration of inhibitor at the inlet to the liver (Iinlet,u,max), used in theprediction of drug-drug interactions, overestimates the unboundconcentration in the liver. Methods. The estimated value of Iinlet,u,max was compared with theunbound concentrations in systemic...
Purpose. To quantitatively predict the in vivo interaction betweentriazolam and erythromycin, which involves mechanism-basedinhibition of CYP3A4, from in vitro studies using human liver microsomes(HLM) and recombinant human CYP3A4 (REC). Methods. HLM or REC was preincubated with erythromycin in thepresence of NADPH and then triazolam was added. α- and 4-hydroxy(OH) triazolam were quantified...
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