TABLE 1.
The PK parameters of six ingredients in rat plasma after i.v., administration of SI with low and high dosages (Mean ± SD).
| Analyte | Group | t 1/2 | Cmax | AUC0-t | AUC0-∞ | Vd | Cl | MRT0-t | MRT0-∞ |
|---|---|---|---|---|---|---|---|---|---|
| (h) | (ng/ml) | (h·ng/ml) | (h·ng/ml) | (L/kg) | [L/(h·kg)] | (h) | (h) | ||
| SYR | Low | 0.25 ± 0.09 | 259.50 ± 59.35 | 100.67 ± 57.37 | 115.88 ± 70.51 | 0.21 ± 0.07 | 0.69 ± 0.43 | 0.27 ± 0.10 | 0.38 ± 0.16 |
| Medium | 0.61 ± 0.25 | 465.33 ± 42.92 | 363.24 ± 81.55 | 367.67 ± 78.73 | 0.31 ± 0.20 | 0.34 ± 0.07 | 0.69 ± 0.07 | 0.75 ± 0.14 | |
| High | 0.53 ± 0.23 | 925.33 ± 38.55 | 585.69 ± 94.42 | 591.71 ± 96.56 | 0.31 ± 0.11 | 0.41 ± 0.07 | 0.67 ± 0.21 | 0.71 ± 0.23 | |
| HSYA | Low | 0.47 ± 0.07 | 2,624.50 ± 660.17 | 2,479.11 ± 1,312.76 | 2,490.30 ± 1,317.76 | 0.09 ± 0.04 | 0.13 ± 0.07 | 0.76 ± 0.19 | 0.78 ± 0.19 |
| Medium | 0.64 ± 0.08 | 5,628.33 ± 405.14 | 5,074.18 ± 328.93 | 5,461.77 ± 202.42 | 0.09 ± 0.01 | 0.10 ± 0.00 | 0.79 ± 0.14 | 0.97 ± 0.06 | |
| High | 0.46 ± 0.12 | 14,077.33 ± 17.21 | 11,015.37 ± 1,025.71 | 11,453.34 ± 668.38 | 0.06 ± 0.02 | 0.09 ± 0.01 | 0.70 ± 0.09 | 0.78 ± 0.11 | |
| p-CA | Low | 0.08 ± 0.05 | 305.00 ± 147.31 | 62.45 ± 50.04 | 67.71 ± 57.20 | 0.11 ± 0.03 | 1.21 ± 0.76 | 0.10 ± 0.05 | 0.12 ± 0.07 |
| Medium | 0.22 ± 0.06 | 715.00 ± 85.75 | 265.09 ± 89.73 | 277.26 ± 84.05 | 0.13 ± 0.07 | 0.40 ± 0.13 | 0.27 ± 0.03 | 0.33 ± 0.01 | |
| High | 0.21 ± 0.05 | 1,255.00 ± 69.07 | 432.92 ± 44.53 | 469.10 ± 38.10 | 0.14 ± 0.03 | 0.45 ± 0.04 | 0.25 ± 0.04 | 0.32 ± 0.04 | |
| SCU | Low | — | — | — | — | — | — | — | — |
| Medium | 2.58 ± 1.84 | 162.20 ± 17.41 | 89.76 ± 21.01 | 104.73 ± 31.46 | 0.05 ± 0.02 | 0.01 ± 0.01 | 1.46 ± 0.64 | 2.90 ± 2.42 | |
| High | 2.84 ± 1.19 | 327.33 ± 60.05 | 305.74 ± 12.47 | 358.05 ± 33.97 | 0.03 ± 0.01 | 0.01 ± 0.00 | 1.57 ± 0.68 | 2.96 ± 1.49 | |
| p-HBA | Low | — | — | — | — | — | — | — | — |
| Medium | 0.48 ± 0.11 | 44.67 ± 5.13 | 20.15 ± 4.40 | 23.41 ± 5.21 | 0.35 ± 0.04 | 0.53 ± 0.11 | 0.43 ± 0.04 | 0.67 ± 0.11 | |
| High | 0.39 ± 0.35 | 74.33 ± 2.52 | 35.19 ± 31.15 | 44.04 ± 45.17 | 0.34 ± 0.09 | 0.99 ± 0.66 | 0.32 ± 0.25 | 0.53 ± 0.53 | |
| RU | Low | — | — | — | — | — | — | — | — |
| Medium | — | — | — | — | — | — | — | — | |
| High | 0.24 ± 0.04 | 39.33 ± 1.53 | 12.38 ± 1.37 | 15.10 ± 2.23 | 0.30 ± 0.02 | 0.86 ± 0.13 | 0.22 ± 0.03 | 0.36 ± 0.06 | |
| Con.sum | Low | 0.47 ± 0.07 | 3,167.75 ± 816.03 | 2,652.33 ± 1,429.09 | 2,663.49 ± 1,433.99 | 0.12 ± 0.06 | 0.18 ± 0.10 | 0.73 ± 0.18 | 0.75 ± 0.18 |
| Medium | 0.67 ± 0.03 | 7,028.20 ± 327.77 | 6,118.67 ± 358.43 | 6,121.59 ± 360.32 | 0.12 ± 0.01 | 0.13 ± 0.01 | 0.92 ± 0.06 | 0.93 ± 0.06 | |
| High | 0.61 ± 0.19 | 16,654.00 ± 83.47 | 12,888.28 ± 601.42 | 12,905.39 ± 600.72 | 0.10 ± 0.04 | 0.12 ± 0.01 | 0.76 ± 0.05 | 0.77 ± 0.05 | |
| AUC integrated | Low | 0.47 ± 0.07 | 2,479.02 ± 623.45 | 2,331.72 ± 1,235.38 | 2,342.22 ± 1,240.07 | 0.09 ± 0.04 | 0.13 ± 0.07 | 0.76 ± 0.19 | 0.78 ± 0.19 |
| Medium | 0.64 ± 0.08 | 4,977.67 ± 350.18 | 4,314.31 ± 162.32 | 4,651.87 ± 328.87 | 0.09 ± 0.01 | 0.10 ± 0.01 | 0.79 ± 0.15 | 0.98 ± 0.05 | |
| High | 0.45 ± 0.13 | 12,613.33 ± 15.31 | 9,842.06 ± 914.28 | 10,231.64 ± 594.87 | 0.06 ± 0.02 | 0.09 ± 0.01 | 0.69 ± 0.09 | 0.78 ± 0.11 | |
| Effect weighting integrated | Low | 0.47 ± 0.07 | 2,565.28 ± 644.69 | 2,419.83 ± 1,281.52 | 2,430.74 ± 1,286.40 | 0.09 ± 0.04 | 0.13 ± 0.07 | 0.76 ± 0.19 | 0.78 ± 0.19 |
| Medium | 0.80 ± 0.18 | 5,498.98 ± 395.38 | 5,178.98 ± 544.93 | 5,337.30 ± 637.82 | 0.11 ± 0.02 | 0.10 ± 0.01 | 0.91 ± 0.11 | 1.03 ± 0.13 | |
| High | 0.58 ± 0.20 | 13,737.03 ± 17.63 | 11,273.38 ± 1,221.77 | 11,861.16 ± 262.38 | 0.07 ± 0.02 | 0.09 ± 0.00 | 0.70 ± 0.09 | 0.83 ± 0.17 |
Low dose group, n = 4; medium and high groups, n = 3, respectively. The plasma drug concentration was low, so the PK, parameters could not be calculated.