Table 4

Interday variability of ER in modified Caco-2 cells

Experiment No.3-aIncubation timeTotal 1′-OH-MDZ3-bBasolateral MDZBasolateral MDZER3-c
min pmol pmol % of Apical Dose
13066.13749.115.1
22035.02649.911.7
33090.93758.319.5
41053.22805.216.0
52044.634710.011.4
62057.13748.913.2
Range11.4–19.5
Average14.5
SD3.1
CV21.1
  • 3-a Experiment number refers to experiments where 4.5 nmol of MDZ was dosed apically and 10% or less of this dose crossed into the basolateral compartment after the indicated incubation time.

  • 3-b Total 1′-OH-MDZ is the sum of the amount found in the apical and basolateral medium and the amount remaining in the cell at the end of the incubation time.

  • 3-c The first-pass ER was calculated by application of the total amount of 1′-OH MDZ formed and total MDZ in the basolateral medium to eq. 2.