Table 7. Pharmacokinetics (PK) of Compounds 86 and 91.
compda | routeb | speciesc | Cmax (ng/mL)d | t1/2 (h) | AUC0–∞ (h·ng/mL) | Vss (L/kg) | CLp (mL/min/kg) | F (%) |
---|---|---|---|---|---|---|---|---|
86 | iv | mouse | 2350 | 0.3 | 1141 | 0.7 | 30 | |
86 | po | mouse | 1234 | 1.6 | 2518 | 44 | ||
91 | iv | mouse | 1997 | 1.3 | 1830 | 1.4 | 18 | |
91 | po | mouse | 1530 | 2.2 | 6980 | 76 | ||
91 | iv | rat | 2587 | 1.5 | 3160 | 0.7 | 11 | |
91 | po | rat | 1980 | 3.5 | 7536 | 48 |
n = 3. The compound was formulated as solution in 20% HP-β-CD in saline.
Dosage: 2 mg/kg for intravenous (iv) and 10 mg/kg for oral (po) administration. Plasma samples were measured for drug exposure by LC–MS/MS.
CD-1 mouse or Sprague-Dawley rat were used.
The maximum drug concentration (Cmax) was observed at t = 5 min, the first sampling time point after iv administration.