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. 2013 Aug 27;170(2):440–457. doi: 10.1111/bph.12285

Table 2.

Plasma PK parameters of total flavonols and terpene lactones after an i.v. infusion dose of ShuXueNing injection in rats

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.