Parameter | Loxoprofen | Reduced trans-alcohol metabolite of loxoprofen |
---|---|---|
Model input parameters | ||
Molecular weight | 246 | 248 |
Octanol–water partition coefficient | 1.97 | 2.23 |
Plasma unbound fraction | 0.0681 | 0.0559 |
Blood–plasma concentration ratio | 0.799 | 0.782 |
Liver–plasma concentration ratio | 1.15 | 1.49 |
Fraction absorbed × intestinal availability | 1 | – |
Absorption rate constant, 1/h | 6.17 ± 0.27 a | – |
Volume of systemic circulation, L | 4.67 ± 0.17 a | 11.4 ± 0.3 a |
Hepatic intrinsic clearance, L/h | 76.3 ± 0.3 a | 215 ± 1 a |
Hepatic clearance, L/h | 4.93 | 10.7 |
Renal clearance, L/h | 0.10 | 1.1 |
Estimated values c | ||
Cmax in plasma, ng/mL | 6940 (0.97) b | 770 (0.86) b |
AUC in plasma, ng h/mL | 11,400 (1.1)b | 2380 (0.90) b |
Reported levels | ||
Cmax in plasma, ng/mL d | 7160 | 896 |
AUC in plasma, ng h/mL d | 10,700 | 2650 |
Bioavailability d | 1 | – |
Urinary excretion of unchanged drug d | 0.02 | – |