Table 2.
PK parameter | t-Quercetin | t-Kaempferol | t-Isorhamnetin | Ginkgolide A | Ginkgolide B | Ginkgolide C | Ginkgolide J |
---|---|---|---|---|---|---|---|
ShuXueNing injection (15 min i.v. infusion at 1 mL·kg−1) | |||||||
C15min (nM) | 732 ± 107 | 1022 ± 186 | 163 ± 23 | 161 ± 25 | 64.5 ± 6.6 | 223 ± 29 | 68.4 ± 6.5 |
AUC0-t (h·nM) | 687 ± 125 | 1116 ± 192 | 379 ± 57 | 72.8 ± 10.9 | 31.7 ± 4.6 | 114 ± 11 | 28.1 ± 4.4 |
MRT (h) | 14.3 ± 4.4 | 15.0 ± 9.8 | 22.3 ± 5.2 | 0.46 ± 0.20 | 0.63 ± 0.08 | 0.67 ± 0.09 | 0.23 ± 0.05 |
t1/2-(1) (h) | 1.86 ± 0.19 | 1.34 ± 0.11 | 2.91 ± 0.46 | 0.62 ± 0.21 | 0.77 ± 0.06 | 0.92 ± 0.07 | 0.31 ± 0.04 |
t1/2-(2) (h) | 14.3 ± 3.8 | 21.5 ± 19.7 | 18.5 ± 4.2 | N.A. | N.A. | N.A. | N.A. |
CLtot,p (L·h−1·kg−1) | 0.46 ± 0.08 | 0.45 ± 0.24 | 0.23 ± 0.04 | 3.85 ± 0.61 | 2.96 ± 0.42 | 1.63 ± 0.13 | 3.40 ± 0.54 |
VSS (L·kg−1) | 6.55 ± 1.68 | 8.42 ± 3.75 | 4.99 ± 1.20 | 2.20 ± 0.72 | 2.22 ± 0.27 | 1.30 ± 0.17 | 1.19 ± 0.15 |
ShuXueNing injection (15 min i.v. infusion at 2 mL·kg−1) | |||||||
C15min (nM) | 1326 ± 275 | 1785 ± 420 | 293 ± 73 | 331 ± 28 | 120 ± 16 | 438 ± 72 | 154 ± 25 |
AUC0-t (h·nM) | 1660 ± 266 | 2400 ± 401 | 927 ± 77 | 185 ± 17 | 72.5 ± 7.4 | 298 ± 16 | 87.3 ± 11.1 |
MRT (h) | 23.9 ± 11.0 | 32.6 ± 4.0 | 25.4 ± 4.0 | 0.54 ± 0.04 | 0.62 ± 0.01 | 0.71 ± 0.10 | 0.41 ± 0.03 |
t1/2-(1) (h) | 1.62 ± 0.19 | 1.86 ± 0.31 | 2.88 ± 0.45 | 0.73 ± 0.05 | 0.69 ± 0.01 | 0.88 ± 0.07 | 0.47 ± 0.09 |
t1/2-(2) (h) | 20.8 ± 10.3 | 27.4 ± 4.2 | 18.0 ± 2.6 | N.A. | N.A. | N.A. | N.A. |
CLtot,p (L·h−1·kg−1) | 0.32 ± 0.08 | 0.31 ± 0.08 | 0.29 ± 0.02 | 3.05 ± 0.20 | 2.68 ± 0.10 | 1.21 ± 0.08 | 2.09 ± 0.33 |
VSS (L·kg−1) | 7.33 ± 2.04 | 10.1 ± 1.4 | 2.78 ± 0.21 | 2.01 ± 0.03 | 2.00 ± 0.09 | 1.01 ± 0.15 | 1.11 ± 0.12 |
ShuXueNing injection (15 min i.v. infusion at 4 mL·kg−1) | |||||||
C15min (nM) | 3607 ± 426 | 5113 ± 589 | 881 ± 86 | 884 ± 11 | 330 ± 8 | 1159 ± 40 | 407 ± 27 |
AUC0-t (h·nM) | 3274 ± 482 | 6275 ± 330 | 2087 ± 240 | 429 ± 38 | 174 ± 20 | 622 ± 106 | 211 ± 19 |
MRT (h) | 10.5 ± 4.2 | 34.7 ± 17.3 | 19.3 ± 4.6 | 0.57 ± 0.09 | 0.60 ± 0.08 | 0.54 ± 0.03 | 0.56 ± 0.06 |
t1/2-(1) (h) | 1.91 ± 0.26 | 1.80 ± 0.13 | 3.13 ± 0.60 | 0.77 ± 0.09 | 0.66 ± 0.05 | 0.78 ± 0.07 | 0.69 ± 0.03 |
t1/2-(2) (h) | 11.6 ± 3.3 | 30.2 ± 14.6 | 16.2 ± 3.7 | N.A. | N.A. | N.A. | N.A. |
CLtot,p (L·h−1·kg−1) | 0.44 ± 0.13 | 0.25 ± 0.08 | 0.19 ± 0.04 | 2.75 ± 0.17 | 2.32 ± 0.19 | 1.24 ± 0.17 | 1.78 ± 0.12 |
VSS (L·kg−1) | 4.26 ± 0.75 | 7.84 ± 2.73 | 3.56 ± 0.44 | 1.92 ± 0.30 | 1.68 ± 0.28 | 0.83 ± 0.07 | 1.22 ± 0.11 |
Because of its low content level in ShuXueNing injection (Table 1), a 15 min i.v. infusion dose of bilobalide at 1 mg·kg−1 was given to FAC rats to obtain the plasma PK parameters of the compound. The C15min, AUC0-t, MRT, t1/2, CLtot,p, and VSS value of bilobalide were 2696 ± 154 nM, 1619 ± 35 h·nM, 0.80 ± 0.05 h, 0.87 ± 0.06 h, 1.89 ± 0.04 L·h−1·kg−1 and 1.51 ± 0.11 L·kg−1 respectively.