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Table 1 The intrinsic clearance of PQ and its enantiomers in human hepatocytes

From: Differential kinetic profiles and metabolism of primaquine enantiomers by human hepatocytes

  (±)-PQ (+)-PQ (−)-PQ
Time interval (min) for calculation of elimination rate constant 0–60 0–60 0–60
λ (h−1)a 0.34 0.19 0.64
t½ (h)b 2.03 3.62 1.09
t½ (min) 121.8 217 65
CLint in vitro [(mL/h)/million cellsc] 0.273 0.153 0.509
CLint in vitro [(µL/min)/million cells] 4.55 2.55 8.49
CLint in vivo [(L/h)/kg body mass]d 0.69 0.39 1.30
CLint in vivo [(mL/min)/kg body mass] 11.58 6.49 21.60
CLh,b [(L/h)/kg body mass]e 0.45 0.30 0.63
CLh,b [(mL/min)/kg body mass] 7 5 11
CLh,b (% hepatic blood flow)f 36 24 51
  1. λ elimination rate constant, Clint intrinsic clearance, CL h,b hepatic blood clearance
  2. aλ is taken as the -slope of the linear portion of the log-linear regression (0-60 min)
  3. bHalf-lives computed from \({\lambda}({\text{t1}}/2 = {\text{ln}}(2)/\lambda\)
  4. c \(({\text{ln2/T1/2}})/{\text{mio viable cells}} \times 1000\)
  5. d \(( {\text{CLint}} /1000) * ({\text{cells/g/liver}})* ({\text{g liver / kg body weight}})\). Hepatocellularity is given as 99 million cells/g liver; average human liver weight is 25.7 g/kg body mass
  6. e \({\text{CLh}} = ( {\text{Qh}} * {\text{CLint}},{\text{scaled}})/ ( {\text{Qh}} + {\text{CLint}},{\text{scaled}})\) Qh hepatic blood flow (well-stirred liver model) is given as 20.7 (mL/min)/kg body mass
  7. fQh (mL/min/kg body weight): 55 (rat); 30.9 (dog); 43.6 (monkey); 20.7 (human)