Dose*
 
Cav (ng/mL)
 
AUC† (ng∙hr/mL)
 
CL/F (L/hr)
 
V/F (L)
 
t½ (hr)

Note: Cav based on observed data; other pharmacokinetic parameters based on estimates from population pharmacokinetic analyses
The variability in average plasma posaconazole concentrations in patients was relatively higher than that in healthy subjects.
* Oral suspension administration† AUC (0-24 hr) for 200 mg TID and AUC (0-12 hr) for 400 mg BID‡ HSCT recipients with GVHD§ Not done¶ Neutropenic patients who were receiving cytotoxic chemotherapy for acute myelogenous leukemia or myelodysplastic syndromes# Febrile neutropenic patients or patients with refractory invasive fungal infections, Cav n=24 
 
200 mg TID‡ (n=252) 1103 (67)
[21.5-3650] ND§ ND§ ND§ ND§
200 mg TID¶ (n=215) 583 (65)
[89.7-2200] 15,900 (62)
[4100-56,100] 51.2 (54)
[10.7-146] 2425 (39)
[828-5702] 37.2 (39)
[19.1-148]
400 mg BID# (n=23) 723 (86)
[6.70-2256] 9093 (80)
[1564-26,794] 76.1 (78)
[14.9-256] 3088 (84)
[407-13,140] 31.7 (42)
[12.4-67.3]

Absorption: When given orally in healthy volunteers, posaconazole delayed-release tablets are absorbed with a median Tmax of 4 to 5 hours. Steady-state plasma concentrations are attained by Day 6 at the 300 mg dose (QD after BID loading dose at Day 1). The absolute bioavailability of the oral delayed-release tablet is approximately 54%. The effect of food intake on the oral bioavailability of posaconazole following administration of posaconazole delayed-release tablets is not known. However, since the oral bioavailability of posaconazole is significantly increased when the oral suspension is administered with food or a nutritional supplement (see below), it is also recommended that posaconazole delayed-release tablets be taken with food.
 
Concomitant administration of posaconazole delayed-release tablets with drugs affecting gastric pH or gastric motility did not demonstrate any significant effects on posaconazole pharmacokinetic exposure (see Table 11).
 
Table 11: The Effect of Concomitant Medications that Affect the Gastric pH and Gastric Motility on the Pharmacokinetics of Posaconazole Delayed-Release Tablets in Healthy Volunteers

Coadministered Drug
 
Administration Arms
 
Change in Cmax
(ratio estimate*;
90% CI of the ratio estimate)
 
Change in AUC0-last
(ratio estimate*;
90% CI of the ratio estimate)

* Ratio Estimate is the ratio of coadministered drug plus posaconazole to posaconazole alone for Cmax or AUC0-last. 
 
Mylanta® Ultimate strength liquid (Increase in gastric pH) 25.4 meq/5 mL, 20 mL ↑6%
(1.06; 0.90 -1.26)↑ ↑4%
(1.04; 0.90 -1.20