TABLE 1

Posaconazole pharmacokinetic parameters after single-dose i.v. administration in healthy volunteers

CohortPosaconazole dose (mg)No. of subjectsArithmetic mean (%CV) or value as indicated fora:
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)
25090.0410 (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)
310090.0360 (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)
420090.0307 (23)23.6 (23)0.5 (0.5–24)b2,250 (29)34,600 (52)35,400 (50)2.75 (97)226 (38)6.54 (32)
525090.0279 (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)
630090.0292 (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.