OBJECTIVE To investigate pharmacokinetic differences of geniposide and paeoniflorin in normal and inflammatory rats after Xiao’er Chiqiao Qingre granules(XECQ) administration.

METHODS Twenty rats were randomly divided into two groups, rats in the model group were intraperitoneal injected with 0.5 mg·kg⁻¹ LPS every other day for six times and 1 mg·kg⁻¹ LPS at the last time. Rats in the control group received equal dose of physiological saline at all the same time. After two weeks model making, all rats were oral administration with 3.75 g·kg⁻¹ XECQ. Rat plasma samples were then collected at different time points and treated with protein precipitation-liquid-liquid extraction methods for LC-MS/MS analysis to obtain concentration data. The pharmacokinetic parameters were calculated by Phoenix Winnolin 6.3.

RESULTS After XECQ administration, the main pharmacokinetic parameters of geniposide in control and model group were obtained as follows: AUC_0-t was (293.36±59.96) and (379.57±194.96)μg·L⁻¹·h, C_max was (78.15±25.88) and (82.63±40.45)μg·L⁻¹, T_max was (0.60±0.32) and (0.73±0.38)h, t_1/2 was (1.72±0.70) and (1.56±0.53)h, CL_Z/F was (68.10±13.03) and (66.94±36.20)L·h⁻¹·kg⁻¹, V_Z/F was (168.41±77.55) and (153.51±106.9)L·kg⁻¹. The main pharmacokinetic parameters of paeoniflorin in control and model group were obtained as follows: AUC_0-t was (162.82±24.41) and (138.34±39.54)μg·L⁻¹·h, C_max was (35.85±4.31) and (30.39±8.94)μg·L⁻¹, T_max was (0.70±0.47) and (0.78±0.72)h, t_1/2 was (4.61±3.80) and (4.10±1.87)h, CL_Z/F was (72.52±19.40) and (87.57±21.88)L·h⁻¹·kg⁻¹, V_Z/F was (404.18±163.58) and (503.29±260.04)L·kg⁻¹. Compared with the control group, no significant differences in pharmacokinetic parameters of geniposide and paeoniflorin were observed in the model group.

CONCLUSION Inflammatory condition may have few effect on pharmacokinetic behaviors of geniposide and paeoniflorin in rats after XECQ administration.