Table 1.
The half-maximum inhibitory concentration (IC50) of the samples on CYP3A4 and the ratios of the titer to grapefruit juice.
| Name of crude drug or formula | Lot number | Extracting ratio (%) | Extract (g) in one time dosage of crude drugs or Kampo formula(a) | Estimated concentration when taken(a) (mg/ml) | IC50 (mg/ml) | Ratio of inhibitory titer to grapefruit juice (%) |
|---|---|---|---|---|---|---|
| Grapefruit juice | 18.5.20 CK/3B | – | – | 100 | 0.96 | 100 |
|
| ||||||
| Moutan Bark | 5I11M | 43 | 0.43 | 2.2 | 0.10 | 21 |
| Glycyrrhiza | 6B22 | 27 | 0.27 | 1.3 | 0.11 | 12 |
| Mentha Herb | 2F18M | 43 | 0.43 | 2.1 | 0.66 | 3.1 |
| Peony Root | 5D08M | 41 | 0.41 | 2.1 | 0.81 | 2.4 |
| Ginger | 5J16M | 22 | 0.22 | 1.1 | 0.62 | 1.7 |
| Cinnamon Bark | 5B23M | 9.3 | 0.09 | 0.47 | 0.42 | 1.1 |
| Bupleurum Root | 3I05M | 15 | 0.15 | 0.76 | 0.67 | 1.1 |
| Gardenia Fruit | 9I11M | 25 | 0.25 | 1.3 | 1.1 | 1.1 |
| Japanese Angelica Root | 7B06M | 41 | 0.41 | 2.1 | 1.9 | 1.0 |
| Atractylodes Lancea Rhizome | 5G13M | 26 | 0.47 | 2.3 | 2.4 | 0.94 |
| Alisma Tuber | 6C07M | 6.9 | 0.07 | 0.35 | 0.39 | 0.85 |
| Cindium Rhizome | 1F08M | 47 | 0.26 | 1.3 | 2.0 | 0.63 |
| Peach Kernel | 3I18M | 9.8 | 0.10 | 0.49 | 7.0 | 0.067 |
| Poria Sclerotium | 5H18M | 3.1 | 0.03 | 0.16 | 3.0 | 0.050 |
|
| ||||||
| Tokishakuyakusan | – | 39 | 2.8 | 14 | 3.1 | 4.4 |
| Kamishoyosan | – | 32 | 2.4 | 12 | 0.38 | 30 |
| Keishibukuryogan | – | 17 | 0.82 | 4.1 | 0.25 | 16 |
|
| ||||||
| Tokishakuyakusan (Tsumura) | 2150023010 | 18 | 1.3 | 6.7 | 1.1 | 5.8 |
| Kamishoyosan (Tsumura) | 2160024010 | 18 | 1.3 | 6.7 | 0.40 | 16 |
| Keishibukuryogan (Tsumura) | 2150025010 | 12 | 0.58 | 2.9 | 0.72 | 3.9 |
(a) One-time dosages for crude drugs were set as 1 g. One time dosages for Kampo formula were set as one-third of daily dosage.
(b) Estimated concentration when one-time dosage extract was taken with 200 ml H2O.