Table 2.
Main pharmacokinetic parameters of decoquinate in oily suspension with nano- and microparticle following single intramuscular injection at 120 mg/kg dose level in mice plasma (n = 2-3).
Main PK parameters following IM injection | Nano-DQ (0.43 µm) plasma |
CV% | Micro-DQ (8.31 µm) plasma |
CV% |
---|---|---|---|---|
C max (ng/ml) | 36.58 ± 3.56 | 9.74 | 45.35 ± 8.09 | 17.84 |
T max (hr) | 3.52 ± 0.13 | 3.82 | 3.22 ± 0.90 | 27.86 |
AUCinf. (ng·hr/ml) | 10,385 ± 405 | 3.91 | 18,311 ± 926 | 5.06 |
t1/2distribution (hr) | 4.84 ± 0.71 | 14.61 | 3.24 ± 1.51 | 46.59 |
t1/2elimination (hr) | 751.01 ± 28.72 | 3.82 | 1,444.90 ± 118.56 | 8.21 |
Vss/F (L/kg) | 12,155.69 ± 844.54 | 6.95 | 13,403.78 ± 447.67 | 3.34 |
CL/F (L/hr/kg) | 11.56 ± 0.45 | 3.91 | 6.57 ± 0.32 | 4.84 |
Minimum inhibitory concentration (MIC) (ng/ml)∗ | 5.12 ± 0.18 | 3.51 | 5.12 ± 0.18 | 3.51 |
T > MIC (hr) | 624.25 ± 60.74 (3.72 weeks) |
9.73 | 1375.00 ± 50.57 (8.18 weeks) |
3.68 |
∗Value was calculated based on full causal prophylaxis effect for 8 weeks. IM: intramuscular; DQ: decoquinate; CV: coefficient of variation.