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. Author manuscript; available in PMC: 2013 Oct 25.
Published in final edited form as: J Med Chem. 2012 Oct 12;55(20):8657–8670. doi: 10.1021/jm3008486

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