Table 2.
Pharmacokinetics of glycyrrhetic acid (8) and liquiritigenin (27) in volunteers orally receiving LianhuaQingwen.
| Pharmacokinetics | Male (m1‒m5) | Male (m6‒m8) | Female (f9‒f12) | Female (f13‒f14) |
|---|---|---|---|---|
| Glycyrrhetic acid (8) on day 1 | ||||
| Cmax (nmol/L) | 88.2 ± 21.2 | 48.5 ± 16.5 | 51.2 ± 32.4 | 236 / 227 |
| Tpeak (h) | 15.4 ± 5.6 | 21.3 ± 4.6 | 18.0 ± 4.0 | 9.0 / 16.0 |
| Lag time (h) | 3.6 ± 2.5 | 10.0 ± 1.7 | 4.3 ± 3.9 | 1.0 / 3.0 |
| AUC0-48h (h ∙ nmol/L) | 1491 ± 736 | 623 ± 175 | 709 ± 431 | 3835 / 2576 |
| AUC0-∞ (h ∙ nmol/L) | 1645 ± 904 | 805 ± 175 | 766 ± 420 | 4516 / 2583 |
| MRT (h) | 22.7 ± 7.0 | 28.2 ± 5.4 | 32.8 ± 20.2 | 32.4 / 17.2 |
| t1/2 (h) | 7.3 ± 4.3 | 7.0 ± 1.8 | 5.5 ± 2.6 | 14.5 / 1.9 |
| Cum.Ae-U,0-48h (nmol/kg) | 0.03 ± 0.02 | 0.02 ± 0.01 | 0.02 ± 0.02 | 0.08 / 0.06 |
| CLR (mL·h−1·kg−1) | 0.02 ± 0.01 | 0.02 ± 0.0 | 0.02 ± 0.01 | 0.02 / 0.02 |
| Glycyrrhetic acid (8) on day 8 | ||||
| Cmax (nmol/L) | 41.6 ± 26.1 | 17.0 ± 0.7 | 41.5 ± 40.6 | 102 / 52.1 |
| Tpeak (h) | 8.9 ± 8.1 | 16.1 ± 13.8 | 10.0 ± 6.9 | 12.0 / 24.0 |
| AUC0-48h (h ∙ nmol/L) | 575 ± 642 | 193 ± 37 | 538 ± 639 | 1496 / 1103 |
| AUC0-∞ (h ∙ nmol/L) | 741 ± 888 | 193 ± 37 | 607 ± 671 | 1614 / 1289 |
| MRT (h) | 17.6 ± 9.6 | 18.9 ± 0.5 | 48.1 ± 31.9 | 79.7 / 29.8 |
| t1/2 (h) | 6.8 ± 5.6 | 5.9 ± 1.9 | 5.9 ± 0.8 | 5.6 / 13.0 |
| Cum.Ae-U,0-48h (nmol/kg) | 0.02 ± 0.02 | 0.01 ± 0.01 | 0.03 ± 0.02 | 0.1 / 0.02 |
| CLR (mL·h−1·kg−1) | 0.04 ± 0.03 | 0.05 ± 0.03 | 0.1 ± 0.0 | 0.04 / 0.02 |
| Liquiritigenin (27) on day 1 | ||||
| Cmax-1 (nmol/L) | 4.2 ± 2.2 | ― | 3.8 ± 1.0 | 5.6 / 2.9 |
| Cmax-2 (nmol/L) | 10.3 ± 6.4 | 6.1 ± 2.7 | 7.0 ± 2.5 | 10.8 / 10.0 |
| Tpeak-1 (h) | 3.4 ± 3.3 | ― | 1.0 ± 0.0 | 1.0 / 3.0 |
| Tpeak-2 (h) | 9.0 ± 2.4 | 10.0 ± 1.7 | 11.3 ± 1.5 | 6.0 / 9.0 |
| AUC0-48h (h ∙ nmol/L) | 47.7 ± 36.2 | 36.4 ± 21.5 | 49.0 ± 29.7 | 50.2 / 37.7 |
| AUC0-∞ (h ∙ nmol/L) | 54.7 ± 37.3 | 60.3 ± 29.5 | 64.3 ± 44.2 | 57.2 / 40.1 |
| MRT (h) | 14.3 ± 11.9 | 23.3 ± 26.3 | 13.6 ± 1.5 | 35.9 / 7.8 |
| t1/2 (h) | 2.3 ± 1.0 | 4.5 ± 2.1 | 3.9 ± 2.1 | 1.6 / 1.1 |
| Cum.Ae-U,0-48h (nmol/kg) | 2.7 ± 2.1 | 2.0 ± 0.4 | 2.3 ± 1.5 | 1.3 / 1.5 |
| CLR (mL·h−1·kg−1) | 46.6 ± 9.3 | 39.1 ± 16.6 | 58.7 ± 51.8 | 22.2 / 36.4 |
| Liquiritigenin (27) on day 8 | ||||
| Cmax-1 (nmol/L) | 2.0 ± 0.9 | ― | 3.7 ± 2.1 | 7.7 / ― |
| Cmax-2 (nmol/L) | 5.7 ± 3.6 | 3.6 ± 1.5 | 6.0 ± 3.4 | 4.8 / 2.4 |
| Tpeak-1 (h) | 2.8 ± 2.4 | ― | 1.0 ± 0.0 | 1.0 / ― |
| Tpeak-2 (h) | 9.6 ± 2.5 | 11.0 ± 1.7 | 6.8 ± 2.9 | 9.0 / 9.0 |
| AUC0-48h (h ∙ nmol/L) | 36.7 ± 36.3 | 21.8 ± 12.1 | 48.3 ± 32.5 | 25.8 / 17.8 |
| AUC0-∞ (h∙nmol/L) | 51.6 ± 48.3 | 26.7 ± 11.1 | 58.4 ± 39.0 | 38.3 / 42.2 |
| MRT (h) | 20.6 ± 23.5 | 11.2 ± 3.6 | 8.4 ± 3.8 | 18.5 / 7.6 |
| t1/2 (h) | 5.5 ± 3.0 | 3.0 ± 1.2 | 3.8 ± 0.5 | 4.3 / 8.9 |
| Cum.Ae-U,0-48h (nmol/kg) | 3.8 ± 4.3 | 2.5 ± 0.5 | 2.6 ± 1.7 | 1.1 / 1.4 |
| CLR (mL·h−1·kg−1) | 63.7 ± 39.6 | 101 ± 25 | 38.5 ± 18.3 | 28.3 / 32.4 |
Cmax maximum plasma concentration, Tpeak the time taken to achieve the peak plasma concentration, AUC area under the plasma concentration-time curve after dosing, MRT mean residence time, t1/2 terminal half-life, Cum.Ae-U cumulative amount excreted into urine, CLR renal excretory clearance.