Table 4

Estimation of metabolite recovery in urine4-a

Compound% Dose
10-N-Glucuronide4-b 13.2
N-Desmethyl-2-carboxy OLZ4-c 3.8
2-Carboxy OLZ4-b 3.5
N-Oxide OLZ4-b 3.4
N-Oxide-2-carboxy OLZ2.3
Glucuronide4-c , 4-d
4′-N-glucuronide4-c , 4-e 2.1
2-Carboxy OLZ glucuronide4-c , 4-d 2.1
2-Hydroxymethyl OLZ4-c 1.4
N-Desmethyl OLZ4-b 0.6
OLZ4-b 7.3
Total 39.7  
  • 4-a Based on total urinary recovery of ∼52%.

  • 4-b Mean value determined from urine samples from two subjects (subject 1, 8–16 hr; subject 4, 4–8 hr).

  • 4-c Based on urine samples from three subjects (subject 6, 16–72 hr; subject 1, 24–48 hr; subject 4, 24–72 hr).

  • 4-d Tentative structural assignment.

  • 4-e The amounts of 4′-N-glucuronide and 2-carboxy OLZ glucuronide were estimated after separation on an Inertsil C18 analytical column with a mobile phase of 1% acetic acid and acetonitrile.