Table 4.
Pharmacokinetic parameters of 4-HPR and metabolites after repeated administration of oral BNF (A) and free 4-HPR (B).
| (A) BNF | ||||||
|---|---|---|---|---|---|---|
| Parameter | Cmax ± SD (µg/mL) |
Tmax (h) |
AUC0–last
(h*µg/mL) |
R% * | HL (h) |
|
| 4-HPR | 8.14 | ±1.029 | 2 | 86.28 | - | 7.5 |
| oxo-4-HPR | 2.88 | ±0.809 | 2 | 43.40 | 50% | 6.1 |
| MPR | 0.98 | ±0.179 | 4 | 14.82 | 17% | 16.6 |
| DH-4-HPR | 0.38 | ±0.125 | 2 | 4.73 | 5% | 6.2 |
| (B) Free 4-HPR | ||||||
| Parameter |
Cmax ± SD
(µg/mL) |
Tmax
(h) |
AUC0–last
(h*µg/mL) |
R% * |
HL
(h) |
|
| 4-HPR | 4.76 | ±0.205 | 4 | 60.94 | - | 6.6 |
| oxo-4-HPR | 2.72 | ±0548 | 4 | 34.30 | 56% | 5.3 |
| MPR | 0.59 | ±0.193 | 2 | 9.60 | 16% | 21.7 |
| DH-4-HPR | 0.33 | ±0.068 | 4 | 4.09 | 7% | 5.3 |
* R = AUC0–last metabolite/AUC0–last 4-HPR.