Table 6.

Pharmacokinetic studies in rats and dogs with compound 4c in 20% HP-β-CD aqueous solution (i.v. administration) or in microcrystalline cellulose (oral administration).

PK Parameter (unit)	Rat		Dog
	I.V. 2 mg/kg (N = 4)	Oral 50 mg/kg (N = 4)	I.V. 5 mg/kg (N = 4)	Oral 20 mg/kg (N = 4)
k (1/h)	0.16 ± 0.01	0.31 ± 0.01	0.13 ± 0.03	0.13 ± 0.03
AUC0→t (h*ng/mL)	3168 ± 492	4763 ± 1080	24516 ± 1918	11019 ± 2975
AUC0→∞ (h*ng/mL)	3170 ± 492	4610 ± 1053	24641 ± 1936	11561 ± 3210
T1/2 (h)	4.3 ± 0.28	2.2 ± 0.08	5.65 ± 1.30	5.50 ± 1.20
CL/F (L/h/kg)	0.64 ± 0.09	–	3.40 ± 0.27
Vd/F (L/kg)	0.33 ± 0.03	–	0.341 ± 0.015
MRT (h)	0.5 ± 0.03	5.6 ± 0.23	1.52 ± 0.139	5.12 ± 0.694
F (%)	100	6.0 ± 1.4	100	11.2 ± 2.73
Cmax (ng/mL)	–	482 ± 153	–	2423 ± 591
Tmax (h)	–	3.7 ± 3.9	–	1.50 ± 0.577