Objective:To study the absorption

distribution and excretion of hyperoside after intragastric administration to rats. Method: Hyperoside was fed to rats by intragastric and intravenous administration

respectively. Plasma

tissues and excretion samples were collected at different time. The samples were analyzed by HPLC for the detection of quercetin after enzymatic hydrolysis treatment with combined β-glucuronidase and sulphatase

using kaempferol as internal standard. Result: After intragastric administration of hyperoside (12.5

25

50 mg·kg-1) to rats

the main pharmacokinetic parameters t1/2e was (3.47±0.76)

(3.52±0.87)

(4.17±1.02) h-1

respectively; tmax was 0.5 h; Cmax was (0.528±0.230)

(1.136±0.451)

(2.033±1.147) mg·L-1

respectively; AUC was (2.67±0.28)

(4.11±0.37)

(6.72±0.83) mg·L-1·h-1

respectively. Based on the weighted regression analysis of the pooled data

Cmax and AUC values increased as the dose increased in a linear manner (r was 0.998 and 0.999

respectively)

consistent with the linear pharmacokinetics. As compared to the intravenous administration at a single dose of (25 mg·kg-1)

the absolute bioavailability after intragastric administration of hyperoside was estimated to be 26.0%. After intragastric administration to rats

the rank order of normalized tissue distribution was stomach>intestines>kidney

liver

muscle

lung

heart>cerebrum

uterus>spleen

testis>fat. After intragastric administration hyperoside (25 mg·kg-1)

excretion amount was only (0.71±0.13)% from urine and (2.04±0.36)% from faeces during 72 h

only (1.56±0.22)% from bile during 24 h

respectively. Conclusion: Hyperoside was rapidly absorbed in rats with a long t1/2e. There was no accumulation in blood and main tissues of hyperoside. The main excretion way of hyperoside was not prototype or glucoside forms from urine

faeces or bile excretion.