Abstract
The present study investigated the pharmacokinetics, excretion, and tissue
distribution of salidroside, a main active constituent in the roots of
Rhodiola species. The plasma concentration declined rapidly
following the intravenous dosing at 7.5, 15, and 30 mg/kg with a short
half-life time of about 1 h. The mean values of area under the
concentration-time curve (300.48 ± 36.73, 514.51 ± 134.99, and
1036.64 ± 101.67 mg · min/L), total body clearance (0.025 ± 0.003,
0.031 ± 0.008, and 0.029 ± 0.003 L/min/kg), and distribution value
(2.02 ± 0.80, 2.47 ± 1.09 and 2.58 ± 0.68 L/kg) suggested linear
pharmacokinetics between the three doses. After intravenous injection of
salidroside at 15 mg/kg, the total cumulative recovery of salidroside in
urine was 53.67 ± 12.03 % over 48 h, but only 0.09 ± 0.03 % and
0.18 ± 0.18 % of the dosage was excreted in bile and feces. Concentrations
of salidroside in 12 tissues as well as plasma were evaluated at 15, 40, and
120 min after dosing. At all time points, no higher concentration of
salidroside was detected in tissues than that in plasma, with the lowest
concentration of salidroside being observed in the brain, liver, fat, and
skeletal muscle were tissues with a higher concentration of salidroside. A
better distribution was also observed in the ovary and testis than that in
the kidney and spleen. This finding demonstrated that salidroside is
eliminated from plasma rapidly mainly by kidney clearance and conspicuously
penetrated well into the skeletal muscle, fat, ovary and testis. A total
recovered salidroside of about 54 % from excretion routes suggested that the
metabolism was likely to take an important role in its elimination.
Key words
salidroside - pharmacokinetics - excretion - distribution - HPLC-UV - LC-MS/MS -
Rhodiola
- Crassulaceae
