Table 5.
Pharmacokinetic parameters of rhynchophylline, isorhynchophylline, corynoxeine, isocorynoxeine, hirsutine, and hirsuteine after oral (po) and intravenous (iv) administration in mice (mean ± SD, n = 8).
| Parameters | Unit | Rhynchophylline | Isorhynchophylline | Corynoxeine | Isocorynoxeine | Hirsutine | Hirsuteine | ||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| iv | po | iv | po | iv | po | iv | po | iv | po | iv | po | ||
| AUC(0 − t) | ng/mL∗h | 168.6 ± 41.8 | 416.7 ± 82.9 | 142.0 ± 37.2 | 209.2 ± 48.1 | 191.4 ± 99.7 | 260.9 ± 66.7 | 179.2 ± 67.3 | 293.1 ± 95.7 | 261.3 ± 122.8 | 899.7 ± 157.8 | 200.7 ± 49.8 | 511.3 ± 83.3 |
| AUC(0-∞) | ng/mL∗h | 169.4 ± 41.6 | 459.6 ± 122.7 | 142.2 ± 37.2 | 212.1 ± 51.5 | 191.8 ± 99.7 | 261.8 ± 67.1 | 180.4 ± 66.5 | 299.1 ± 91.1 | 261.7 ± 122.5 | 908.4 ± 158.3 | 202.4 ± 49.5 | 518.2 ± 81.1 |
| MRT(0 − t) | h | 0.5 ± 0.2 | 1.7 ± 0.6 | 0.2 ± 0.1 | 1.2 ± 0.1 | 0.2 ± 0.1 | 0.9 ± 0.2 | 0.3 ± 0.1 | 1.6 ± 0.4 | 0.9 ± 0.4 | 1.8 ± 0.3 | 0.9 ± 0.3 | 1.6 ± 0.3 |
| MRT(0-∞) | h | 0.6 ± 0.4 | 3.8 ± 4.9 | 0.2 ± 0.1 | 1.4 ± 0.4 | 0.2 ± 0.1 | 0.9 ± 0.2 | 0.5 ± 0.3 | 1.8 ± 0.2 | 1.0 ± 0.4 | 1.9 ± 0.5 | 1.0 ± 0.5 | 1.9 ± 0.5 |
| t 1/2z | h | 2.2 ± 1.4 | 4.4 ± 6.0 | 0.6 ± 0.3 | 2.5 ± 2.1 | 0.5 ± 0.2 | 0.7 ± 0.4 | 3.2 ± 2.7 | 1.6 ± 0.7 | 1.1 ± 0.6 | 2.0 ± 0.9 | 2.2 ± 1.4 | 2.4 ± 2.0 |
| Vz | L/kg | 20.0 ± 13.4 | 60.1 ± 67.1 | 6.8 ± 4.0 | 84.5 ± 57.5 | 4.4 ± 1.5 | 19.3 ± 9.1 | 28.7 ± 26.2 | 45.7 ± 36.1 | 8.3 ± 6.5 | 16.8 ± 9.0 | 15.9 ± 9.8 | 36.1 ± 33.2 |
| CLz/F | L/h/kg | 6.2 ± 1.5 | 11.6 ± 3.2 | 7.4 ± 1.8 | 24.7 ± 6.1 | 6.2 ± 2.3 | 20.2 ± 5.2 | 6.1 ± 1.9 | 18.2 ± 6.1 | 4.4 ± 1.7 | 5.6 ± 1.0 | 5.2 ± 1.5 | 9.8 ± 1.5 |
| C max | ng/mL | 199.3 ± 34.3 | 508.0 ± 71.9 | 184.6 ± 29.3 | 305.3 ± 68.8 | 230.7 ± 58.1 | 374.8 ± 65.1 | 221.2 ± 47.8 | 373.2 ± 58.3 | 222.6 ± 87.6 | 524.5 ± 124.5 | 188.4 ± 44.7 | 360.8 ± 77.2 |
| Bioavailability | 49.4% | 29.5% | 27.3% | 32.7% | 68.9% | 51.0% | |||||||