Estimation of portal vein concentrations for individual parent flavonolignans
A bold [I]/IC50 number indicates that the value is above the cutoff of 0.1.
| Variable | Silybin A | Silybin B | Reference | ||
|---|---|---|---|---|---|
| Dose of silymarin (mg) | 700 | 140 | 700 | 140 | (Hawke et al., 2010) |
| [Dose of individual flavonolignans (mg)] | [116] | [23.2] | [160] | [32] | |
| Cmax (µg/ml) | 0.58 | 0.04 | 0.22 | 0.008 | (Hawke et al., 2010) |
| ka (Absorption rate constant; min−1) | 0.1 | (Ito et al., 1998) | |||
| Q (Hepatic blood flow; ml/min) | 1500 | (Wynne et al., 1989) | |||
| fu (Fraction unbound) | 0.05 | Dr. Mengs, Madaus GmbH, Germany | |||
| fa (Fraction absorbed) | 0.2 | 0.62 | From rat (Pade, 2007) | ||
| Cu,max,in (unbound portal vein conc.; µM) | 0.22 | 0.04 | 0.70 | 0.13 | Calculated |
| [I]/IC50 ratio OATP1B1 | 0.02 | 0.004 | 0.08 | 0.02 | Calculated |
| [I]/IC50 ratio OATP1B3 | 0.08 | 0.01 | 0.14 | 0.03 | Calculated |
| [I]/IC50 ratio OATP2B1 | 0.05 | 0.01 | 0.88 | 0.16 | Calculated |