Tissue/ Compound | AUC0–240 | AUC0–∞ | Cmax | Tmax | Absorption/Formation | Redistribution | Elimination | ||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|
C | γ | t1/2 | A | α | t1/2 | B | β | t1/2 | |||||
Brain | |||||||||||||
R-2HMP | 298523 | 332872 | 6204 ± 912 | 15 | 38351 | 0.10 | 7 | 37503 | 0.067 | 10 | 848 | 0.0059 | 117 |
R-2HMA | 47756 | 51483 | 704 ± 194 | 15 | 16377 | 0.066 | 10 | 16044 | 0.061 | 11 | 333 | 0.0094 | 74 |
R-2HPA | 17153 | 18593 | 286 ± 36 | 30 | 9462 | 0.046 | 15 | 9409 | 0.043 | 16 | 53 | 0.0069 | 100 |
R-2HA | 3730 | 5445 | 32 ± 13 | 30 | 360 | 0.051 | 13 | 336 | 0.046 | 15 | 24 | 0.0047 | 149 |
Liver | |||||||||||||
R-2HMP | 263584 | 427977 | 2755 ± 306 | 30 | 141341 | 0.054 | 13 | 140234 | 0.052 | 13 | 1107 | 0.0032 | 220 |
R-2HMA | 31244 | 51940 | 420 ± 89 | 30 | 9043 | 0.043 | 16 | 8977 | 0.039 | 17 | 66 | 0.0020 | 350 |
R-2HPA | 12303 | 14343 | 191 ± 24 | 15 | 5070 | 0.058 | 12 | 5030 | 0.053 | 13 | 40 | 0.0054 | 129 |
R-2HA* | 13083 | 14193 | 114 ± 19 | 30 | 213 | 0.050 | 14 | 213 | 0.013 | 54 | |||
Plasma | |||||||||||||
R-2HMP | 35338 | 40886 | 1125 ± 409 | 5 | 1306 | 3.92 | 0.2 | 1128 | 0.068 | 10 | 178 | 0.0068 | 101 |
R-2HMA | 15940 | 17688 | 194 ± 16 | 15 | 268 | 0.29 | 2.5 | 150 | 0.030 | 23 | 118 | 0.0086 | 81 |
R-2HPA | 4980 | 5363 | 54 ± 11 | 15 | 69 | 0.36 | 2 | 20 | 0.025 | 28 | 49 | 0.010 | 66 |
R-2HA* | 1493 | 2061 | 13 ± 7 | 5 | 12 | 3.71 | 0.2 | 12 | 0.0069 | 100 |
Values were calculated by MOR with a triexponential model, followed by variance-weighted nonlinear regression.
∗, biexponential model was used.
Units: AUC, nanogram · minutes per gram; A, B, C,Cmax, nanograms per gram; α, β, γ, min.−1; Tmax, t1/2, min.