Table 2.
Pharmacokinetic Parameters of MGN, HNK, MHNK and Their Respective Metabolites (Glucuronides and Sulfates) After I.V. Administration of 5 mg ME/kg (n = 5)
| Parameters | Tmax (hr) | Cmax (ng/mL) | AUC0–24 (hr*ng/mL) | AUC0−∞ (hr*ng/mL) | Half-life (hr) | V (L/kg) | CL (L/hr/kg) | MRT0–24 (hr) |
|---|---|---|---|---|---|---|---|---|
| MGN | - | 2284.4 ± 700.5 | 1232.2 ± 649.6 | 1234.1 ± 651.2 | 1.0 ± 0.3 | 1.0 ± 0.4 | 0.8 ± 0.6 | 0.8 ± 0.5 |
| MGN_Glucuronide | 0.2 ± 0.1 | 137.0 ± 21.6 | 171.7 ± 39.4 | 173.3 ± 39.6 | 0.9 ± 0.2 | - | - | 1.1 ± 0.2 |
| MGN_Sulfate | 0.1 ± 0.1 | 17.4 ± 3.5 | 41.7 ± 12.1 | 49.0 ± 14.6 | 2.2 ± 0.7 | - | - | 2.1 ± 0.5 |
| HNK | - | 2400.5 ± 1041.4 | 1150.6 ± 719.3 | 1151.3 ± 719.1 | 0.7 ± 0.04 | 1.3 ± 1.0 | 1.2 ± 0.9 | 0.6 ± 0.1 |
| HNK_Glucuronide1 | 0.2 ± 0.1 | 102.7 ± 17.5 | 156.9 ± 36.6 | 158.3 ± 37.1 | 0.8 ± 0.3 | - | - | 1.2 ± 0.3 |
| HNK_Glucuronide2 | 0.3 ± 0.1 | 83.0 ± 15.7 | 164.2 ± 39.1 | 186.4 ± 57.3 | 2.7 ± 1.1 | - | - | 2.1 ± 0.3 |
| HNK_Sulfate | 0.1 ± 0.1 | 2.8 ± 1.2 | 2.3 ± 1.1 | 4.0 ± 2.3 | 2.0 ± 1.0 | - | - | 1.0 ± 0.4 |
| MHNK | - | 824.3 ± 309.5 | 623.2 ± 358.8 | 631.1 ± 360.0 | 2.9 ± 2.1 | 5.5 ± 1.7 | 2.0 ± 1.6 | 1.5 ± 0.6 |
| MHNK_Glucuronide | 0.2 ± 0.1 | 95.6 ± 17.4 | 180.5 ± 62.2 | 191.3 ± 63.7 | 1.4 ± 0.6 | - | - | 1.7 ± 0.6 |
| MHNK_Sulfate | - | - | - | - | - | - | - | - |