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. 2018 May 16;61(11):4883–4903. doi: 10.1021/acs.jmedchem.8b00270

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
a

n = 3. The compound was formulated as solution in 20% HP-β-CD in saline.

b

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.

c

CD-1 mouse or Sprague-Dawley rat were used.

d

The maximum drug concentration (Cmax) was observed at t = 5 min, the first sampling time point after iv administration.