TABLE 4

Pharmacokinetic parameters for DPC 681 dosed at 600 mg every 12 h for 14 days (except day 1 with a single 600 mg dose) in six healthy human volunteers

Parameter
Dose 1 Day 1, AM
Dose 14 Day 8, AM
Dose 15 Day 8, PM
Dose 26 Day 14, AM
Dose 27 Day 14, PM
Cmax (μM) 4.53±0.76a 1.34±0.36b 0.51±0.20b 1.25±0.57b 0.64±0.31b
Tmax (h) 1.0 (0.5-1.0) 1.0 (1.0-1.0) 1.0 (1.0-1.5) 1.0 (0.5-1.0) 0.75 (0.5-1.0)
AUC0-12h (μM·h) 9.15±1.92 2.34±0.63b 1.58±0.53b 2.27±0.97b 1.62±0.57b
t1/2 (h) 3.31±0.64 2.43±0.34 2.53±0.19c 3.13±0.60 2.86±0.52
CL/F (liters/h)
97±16
432±136b
672±312b
465±170b
621±199b

  • ↵ a All the parameters were expressed as mean ± S.D. (n = 6), except for Tmax (h) which was expressed as median (range)

  • ↵ b P < 0.05 and

  • ↵ c P < 0.001 when compared with the respective parameter at dose 1