TABLE 1.
Posaconazole pharmacokinetic parameters after single-dose i.v. administration in healthy volunteers
| Cohort | Posaconazole dose (mg) | No. of subjects | Arithmetic mean (%CV) or value as indicated fora: |
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|---|---|---|---|---|---|---|---|---|---|---|---|
| λz (h) | t1/2 (h) | tmax (h) [median (range)] | Cmax (ng/ml) | AUC0–last (ng · h/ml) | AUC0–∞ (ng · h/ml) | AUC% | Vz (liters) | CL (liters/h) | |||
| 2 | 50 | 9 | 0.0410 (34) | 18.7 (34) | 0.6 (0.5–0.7) | 313 (30) | 4,620 (31) | 4,890 (30) | 5.95 (62) | 294 (39) | 10.9 (25) |
| 3 | 100 | 9 | 0.0360 (14) | 19.6 (16) | 0.5 (0.5–0.5) | 1,330 (27) | 10,800 (27) | 11,200 (26) | 4.47 (47) | 262 (22) | 9.40 (23) |
| 4 | 200 | 9 | 0.0307 (23) | 23.6 (23) | 0.5 (0.5–24)b | 2,250 (29) | 34,600 (52) | 35,400 (50) | 2.75 (97) | 226 (38) | 6.54 (32) |
| 5 | 250 | 9 | 0.0279 (21) | 26.0 (23) | 0.5 (0.5–0.5) | 2,260 (26) | 40,600 (39) | 41,500 (41) | 1.84 (85) | 245 (33) | 6.68 (29) |
| 6 | 300 | 9 | 0.0292 (20) | 24.6 (20) | 0.5 (0.5–1.0) | 2,840 (30) | 45,500 (26) | 46,400 (26) | 1.74 (46) | 236 (17) | 6.90 (27) |
a
AUC0–∞, area under the concentration-time curve from time zero to infinity; AUC0–last, AUC from time zero to the time of the last measurable sample; AUC%, percentage of AUC0–∞ that is extrapolated; CL, total body clearance; Cmax, maximum observed plasma drug concentration; %CV, percent coefficient of variation; i.v., intravenous; tmax, time to Cmax; t1/2, terminal-phase half-life; λz, terminal-phase (elimination) rate constant; Vz, volume of distribution during the terminal phase.
b
One subject had a high concentration at the 24-h sample; therefore, tmax is 24 h for that subject.