Research Article

Formulation and Particle Size Reduction Improve Bioavailability of Poorly Water-Soluble Compounds with Antimalarial Activity

Table 5

Evaluations* of pharmacokinetics of WR299666 suspended in HECT at dose of 50 mg/kg following single oral administration in male ICR mice (n = 5).

PK ParametersWR299666 in Plasma
Microsuspension
(42.22 μm)
Microsuspension
(1.50 μm)

(ng/mL)145.20 ± 9.40245.20 ± 71.10
(hr)0.70 ± 0.080.79 ± 0.15
AUClast (ng · h/mL)387.40 ± 35.90718.60 ± 131.30
AUCinf. (ng · h/mL)405.10 ± 36.60732.40 ± 127.00
elimination (β, h)9.00 ± 0.907.94 ± 0.52
Vz/F (liter/kg)613.70 ± 39.40267.80 ± 79.20
CL/F (liter/hr/kg)1.97 ± 0.191.24 ± 0.27
MRT (h)5.81 ± 0.311.22 ± 0.20

Relative bioavailability (%)53.70100.00

The data was fitted with Phoenix/Win Nonlin (V6.1). PK: pharmacokinetics; MRT: mean residence time.