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 Parameters | WR299666 in Plasma | Microsuspension (42.22 μm) | Microsuspension (1.50 μm) |
| (ng/mL) | 145.20 ± 9.40 | 245.20 ± 71.10 | (hr) | 0.70 ± 0.08 | 0.79 ± 0.15 | AUClast (ng · h/mL) | 387.40 ± 35.90 | 718.60 ± 131.30 | AUCinf. (ng · h/mL) | 405.10 ± 36.60 | 732.40 ± 127.00 | elimination (β, h) | 9.00 ± 0.90 | 7.94 ± 0.52 | Vz/F (liter/kg) | 613.70 ± 39.40 | 267.80 ± 79.20 | CL/F (liter/hr/kg) | 1.97 ± 0.19 | 1.24 ± 0.27 | MRT (h) | 5.81 ± 0.31 | 1.22 ± 0.20 |
| Relative bioavailability (%) | 53.70 | 100.00 |
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The data was fitted with Phoenix/Win Nonlin (V6.1). PK: pharmacokinetics; MRT: mean residence time.
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