Table 37.
Pharmacokinetic parameters of ligustilide in rats after intravenous, intraperitoneal, and oral administration (n = 5).
| Pharmacokinetic parameter | Administration route and dose (mg/kg) |
||||
|---|---|---|---|---|---|
| i.v. |
i.p. |
p.o. |
|||
| 15.6 | 14.9a | 26 | 52 | 500 | |
| Tmax (h) | – | – | 0.05 ± 0.02 | 0.08 ± 0.01 | 0.36 ± 0.19 |
| Cmax (mg/L) | 13.19 ± 0.84 | 6.93 ± 0.60*** | 7.48 ± 1.10*** | 20.75 ± 2.55### | 0.66 ± 0.23*** |
| t1/2 (h) | 0.31 ± 0.12 | 0.22 ± 0.07 | 0.36 ± 0.05 | 0.44 ± 0.08# | 03.43 ± 1.01*** |
| AUC 0-μ (mg/L)b | 1.81 ± 0.24 | 0.79 ± 0.10** | 0.93 ± 0.07* | 1.77 ± 0.23# | 0.047 ± 0.012** |
| Vd/F (L/kg)c | 3.76 ± 1.23 | 5.62 ± 1.19 | 6.54 ± 1.56 | 6.32 ± 1.81 | 1641.9 ± 121.6*** |
| CL/F (L/h/kg)c | 9.14 ± 1.27 | 20.35 ± 3.05** | 16.90 ± 1.21** | 9.26 ± 1.04## | 411.1 ± 145.7*** |
| MRT (h) | 0.30 ± 0.07 | 0.19 ± 0.03 | 0.30 ± 0.05 | 0.41 ± 0.03 | 5.14 ± 1.56*** |
| F (%) | 45.7d | 51.7 | 97.7 | 2.6 | |
*p 0.05, **p 0.01, ***p 0.001, compared with i.v. dosing of the isolated ligustilide.
#p 0.05, ##p 0.01, ###p 0.001, compared with the lower i.p. dose of the isolated ligustilide.
AUC = area under the concentration-time curve; Cmax = peak plasma concentration; i.p. = intraperitoneal; i.v. = intravenous; MRT = mean residence time; p.o. = by mouth; Tmax = time of peak plasma concentration; CL = Clearance; Vd = Volume of Distribution; F = Absolute bioavailability; t1/2 = Half life; CL/F = apparent plasma clearance; Vd/F = apparent volume of distribution based on the terminal phase.
Dose of ligustilide in 100 mg/kg of Chuanxiong extract.
Normalized with dose.
Data represent Vd and CL in the case of i.v. dosing of the isolated ligustilide.
Relative bioavailability compared with that of i.v. dosing of the isolated ligustilide.