Pharmacokinetic Study on Luteolin and Cynaroside in Rats
10.6039/j.issn.1001-0408.2016.22.11
- VernacularTitle:木犀草素和木犀草苷在大鼠体内的药动学研究
- Author:
Xiaohua ZOU
;
Shuanghu WANG
;
Yunfang ZHOU
- Publication Type:Journal Article
- Keywords:
Luteolin;
Cynaroside;
Plasma concentration;
Pharmacokinetics;
UPLC-ESI-MS/MS
- From:
China Pharmacy
2016;27(22):3058-3061
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE:To establish the method for pharmacokinetic study of luteolin and cynaroside in rats and to determine pharmacokinetic parameters. METHODS:16 SD rats were randomly divided into luteolin group (sublingual iv,1.34 mg/kg) and cynaroside group(sublingual iv,0.64 mg/kg). 0.5 ml blood were collected before administration and 0,15,30 min and 1,2,3,4,6, 8,12,24,48 h after administration respectively to prepare plasma. UPLC-TQ-MS was adopted to determine plasma concentration, and pharmacokinetic parameters were calculated. A CORTECSTM UPLC? C18(100 mm×2.1 mm,1.6 μm)column was used with mobile phase consisted of acetonitrile-water (containing 0.1% formic acid) at a flow rate of 0.4 ml/min,the column temperature was set at 40 ℃,and quercetin was used as internal standard. RESULTS:The linear range of luteolin and cynaroside were 2.5-500 ng/ml (r=0.998 2) and 10-2 500 ng/ml (r=0.993 5). The lowest quantitation limits were 1 and 2.5 ng/ml,and extraction were 70.75%-87.72% and 75.40%-91.18%(n=6);RSD of inter-day and intra-day were all lower than 10%(n=3). Pharmacokinetic parameters as t1/2 were (1.88 ± 0.32) and (1.57 ± 0.08) h;CL were (0.77 ± 0.18) and (0.06 ± 0.01) L/(h·kg);AUC0-6 h were (189.60±40.04)and(1 093.14±187.36)ng·h/ml;AUC0-∞ were(195.18±38.37)and(1 097.11±188.07)ng·h/ml. CONCLU-SIONS:The method can be used for pharmacokinetic study of luteolin and cynaroside in rats,and the pharmacokinetics of them in rats are in line with two-compartment model.
