Objective:To establish a rapid RP-HPLC method for the determination and to study the pharmacokinetics of gentiopicroside after ig the total iridoid glucosides (TIG) extracted from Gentiana macophlla in rats and to assess the effect of other component in the TIG extracted from Gentiana macophlla. Method: The rats were orally treated with the TIG extracted from Gentiana macophlla. Plasma in centrifuge tube heparinized was separated by centifugation at 4 000 r·min-1 for 10 min

and five times acetonitrile in volume was added to deposit proteins. After centrifugalized

the concentration of gentiopicroside in plasma was determined by RP-HPLC. The pharmacokinetic parameters were calculated with Kinetic software. Result: A good linear relationship was obtained between the peak area and the concentration of gentiopicroside from 33.5 to 4 020.0 μg·L-1

and the lowest limit of detection of gentiopicroside in plasma was 6.7 μg·L-1. The mean extraction recoveries were 80.82%

97.38% and 89.10% for high

middle

low concentrations of the samples respectively. The concentration-time profiles of gentiopicroside were fit with noncompartment model. The main pharmacokinetics parameters t1/2

Tmax

Cmax

MRT

HVD

AUC(0~∞)

CL(s) were relatively stable. Conclusion: The method applied for determination of gentiopicroside content in blood was quick

simple

accurate

sensitive and feasible for the study of the gentiopicroside pharmacokinetics in rats.