TABLE 1.
Pharmacokinetic parameters of silybin A, silybin B, isosilybin A, isosilybin B, silychristin, silydianin, and taxifolin after single oral doses of milk thistle capsules (Legalon)
The Tmax values are expressed as median (range) and others are the mean ± S.D. (n = 13).
| One Capsule |
Two Capsules |
Three Capsules |
|
|---|---|---|---|
| Silybin A (21.2 mg/capsule) | |||
| Tmax (h) | 1.5 (0.5–8.0) | 1.0 (0.5–4) | 1.0 (0.5–4) |
| Cmax (ng/ml) | 106.9 ± 49.2 | 200.5 ± 98.3 | 299.3 ± 101.7 |
| t1/2 (h) | 1.6 ± 0.5 | 1.8 ± 0.5 | 1.9 ± 0.5 |
| AUC0–24h (ng×h/ml) | 231.2 ± 91.6 | 462.3 ± 222.2 | 737.3 ± 270.0 |
| AUC0–∞ (ng×h/ml) | 233.5 ± 92.1 | 466.1 ± 222.4 | 744.3 ± 269.7 |
| CL/F (l/h) | 108.9 ± 53.5 | 109.9 ± 45.2 | 96.9 ± 37.3 |
| V/F (l) | 244.5 ± 108.2 | 281.8 ± 130.9 | 259.4 ± 127.0 |
| Silybin B (29.5 mg/capsule) | |||
| Tmax (h) | 1.5 (0.5–6.0) | 1.0 (0.5–4) | 1.0 (0.5–4) |
| Cmax (ng/ml) | 30.5 ± 16.3 | 74.5 ± 45.7 | 121.0 ± 52.2 |
| t1/2 (h) | 2.4 ± 0.7 | 2.6 ± 0.8 | 2.2 ± 0.8 |
| AUC0–24h (ng×h/ml) | 63.6 ± 27.3 | 150.4 ± 94.0 | 279.1 ± 129.7 |
| AUC0–∞ (ng×h/ml) | 65.6 ± 27.1 | 155.2 ± 96.2 | 285.8 ± 130.8 |
| CL/F (l–/h) | 554.6 ± 298.5 | 514.8 ± 252.5 | 377.6 ± 130.8 |
| V/F (l) | 1944.0 ± 1307.7 | 1945.4 ± 1171.3 | 1190.8 ± 676.4 |
| Isosilybin A (11.4 mg/capsule) | |||
| Tmax (h) | 1.0 (0.5–6.0) | 1.0 (0.5–3.0) | 1.0 (0.5–3.0) |
| Cmax (ng/ml) | 6.1 ± 2.9 | 18.2 ± 13.5 | 24.7 ± 11.8 |
| t1/2 (h) | ND | 3.2 ± 1.5 | 2.8 ± 1.3 |
| AUC0–24h (ng×h/ml) | ND | 33.6 ± 21.0 | 57.2 ± 28.7 |
| AUC0–∞ (ng×h/ml) | ND | 36.4 ± 21.6 | 61.1 ± 28.6 |
| CL/F (l/h) | ND | 899.8 ± 560.1 | 675.6 ± 297.6 |
| V/F (l) | ND | 3781.1 ± 1961.4 | 2883.4 ± 2281.9 |
| Isosilybin B (8.2 mg/capsule) | |||
| Tmax (h) | 1.5 (0.5–8.0) | 1.0 (0.5–4.0) | 1.0 (0.5–4.0) |
| Cmax (ng/ml) | 22.0 ± 10.7 | 46.4 ± 31.0 | 75.8 ± 32.3 |
| t1/2 (h) | 1.9 ± 0.6 | 2.0 ± 0.7 | 1.9 ± 0.6 |
| AUC0–24h (ng×h/ml) | 40.4 ± 17.7 | 90.1 ± 53.6 | 158.6 ± 72.1 |
| AUC0–∞ (ng×h/ml) | 42.8 ± 17.6 | 91.9 ± 54.0 | 162.1 ± 72.5 |
| CL/F (l/h) | 237.9 ± 138.7 | 236.3 ± 119.3 | 183.5 ± 85.6 |
| V/F (l) | 662.0 ± 430.5 | 677.2 ± 353.9 | 506.4 ± 251.4 |
| Silychristin (31.5 mg/capsule) | |||
| Tmax (h) | ND | 1.5 (0.5–4.0) | 1.5 (0.5–4.0) |
| Cmax (ng/ml) | ND | 4.6 ± 1.1 | 8.5 ± 3.4 |
| t1/2 (h) | ND | ND | 2.7 ± 1.5 |
| AUC0–24h (ng×h/ml) | ND | ND | 32.9 ± 14.3 |
| AUC0–∞ (ng×h/ml) | ND | ND | 36.6 ± 14.6 |
| CL/F (l/h) | ND | ND | 2987.6 ± 1158.0 |
| V/F (l) | ND | ND | 11,079.9 ± 5506.1 |
| Silydianin (36.4 mg/capsule) | |||
| Tmax (h) | ND | ND | 1.5 (0.5–9.0) |
| Cmax (ng/ml) | ND | ND | 6.4 ± 3.8 |
| t1/2 (h) | ND | ND | ND |
| AUC0–24h (ng×h/ml) | ND | ND | ND |
| AUC0–∞ (ng×h/ml) | ND | ND | ND |
| CL/F (l/h) | ND | ND | ND |
| V/F (l) | ND | ND | ND |
| Taxifolin (5.9 mg/capsule) | |||
| Tmax (h) | ND | ND | 1.0 (0.5–3.0) |
| Cmax (ng/ml) | ND | ND | 5.1 ± 2.7 |
| t1/2 (h) | ND | ND | ND |
| AUC0–24h (ng×h/ml) | ND | ND | ND |
| AUC0–∞ (ng×h/ml) | ND | ND | ND |
| CL/F (l/h) | ND | ND | ND |
| V/F (l) | ND | ND | ND |
ND, not determined due to the plasma concentrations were below the low limits of quantification.