Pharmacokinetics Of Scutellarin In Animal

Aim: Pharmacokinetics of scutellarin in rat and dog after iv, and the distribution and elimination in rats, as well as the plasma protein binding capacity of scutellarin were studied. Method: Pharmacokinteic assays were carried out by HPLC, plasma protein binding capacity research was conducted by dialysis equilibrium and the sample assay was completed by HPLC also. Results: The concentration-time curve of rats after iv l,3,9mg/kg of scutellarin can be fitted to two-compartment model with the main pharmacokinetic parameters as follows: according to three dose-low, middle, high, t_1/2 α were 1.5min, 1.5min, 3min, t_1/2 β were 53min, 51min, 45min, AUC0-180 were 23.677,65.068,255.233 and the AUC_0-00 were 24.752,66.238,257.3692, the AUC exhibited linear kinetics over the dosage range of 1-9mg/kg. 5min after iv, scutellarin was found in tissues with high concentration in liver, kidney, small intestine, and low level in other tissues. After iv 9mg/kg, 3.38% and 1.97% were excreted from urine and feces in 48 hours. After iv 9mg/kg, 9.52% were excreted from bile in 24 hours. The rate of rat plasma binding of scutellarin was moderate level. The concentration-time curve of dogs after iv 1,3,9mg/kg of scutellarin can be also fitted to two-compartment model with the main pharmacokinetic parameters as follows: according to three dose-low, middle, high, t_1/2 α were 4.26min, 3.93min, 1.48min, tm p were 42.71min, 43min, 31min, AUC_0-108 were 17.78,62.468,216.605 and the AUC0-00 were 18.942,63.948,219.676, the AUC exhibited linear kinetics over the dosage range of 1-9mg/kg. Conclusion: The concentration of scutellarin in plasma declined rapidly after single dose of iv in animal, and were determined in most tissues with high level in liver, kidney, small intestine. Part of scutellarin was excreted from urine and bile. The protein binding ratio of scutellarin was moderate.