Table 9.
Pharmacokinetic parameters for ELQ-300 in Male Sprague Dawley rats that were orally administered ELQ-331 SDD and SEDDS formulations
| Formulation | Tmax
(hr) |
Cmax
(ng/ml) |
t1/2
(hr) |
AUClast
(hr.ng/ml) |
AUCinf
(hr.ng/ml) |
Vz/F (ml/kg) |
Cl/F (ml/hr/kg) |
|---|---|---|---|---|---|---|---|
| Mean ± SD; n=3 per group | |||||||
| SDD | 4 ± 0 | 4130 ± 2280 | 14.2 ± 1.67 | 71200 ± 17700 | 72300 ± 18100 | 3020 ± 1130 | 145 ± 42 |
| SEDDS | 4 ± 0 | 6000 ± 591 | 13.7 ± 0.6 | 99600 ± 25500 | 100000 ± 25200 | 2050 ± 420 | 104 ± 24 |
Dose: 12.14 mg/kg ELQ-331 (equivalent to 10 mg/kg of ELQ-300); Tmax: Time at which Cmax was observed, Cmax: Maximum observed plasma concentration; t1/2: half-life; AUC last: Area under the plasma concentration-time curve up to the last measurable concentration; AUCinf: Area under the plasma concentration-time curve from time zero to infinity. Vz/F: Apparent volume of distribution during terminal phase after oral/extravascular administration; Cl/F: Apparent total plasma or serum clearance of drug after oral administration. SDD: Spray-dried Dispersion; SEDDS: Self-Emulsifying Drug Delivery System.