Abstract： Objective： Based on the previous study that Guanxin Ⅱ has antidepressant effect， in order to reveal the material basis of antidepressant effect of Guanxin Ⅱ，the aim of the study was to evaluate the potential pharmacodynamic components of Guanxin Ⅱ in blood and brain tissue of rats by high performance liquid chromatography(HPLC). Methods：SD rats were administered oral Guanxin Ⅱ(2.5 g/kg) ，and were killed 30 minutes later. Collected the serum and brain tissue of rats and determined the three main active components of Guanxin Ⅱ(Hydroxysafflor yellow A，ferulic acid，salvianolic acid B) by HPLC，and calculated the permeability of blood-brain barrier(BBB) of each component. Chromatographic column：Agilent Zorbax SB- C18(250 mm×4.6 mm，5 μm)；mobile phase：acetonitrile(A)- 0.1% phosphoric acid(B)；column temperature： 35 ℃ ； flow rate： 1.0 mL/min. Results： The linear regression equations of hydroxysafflor yellow A， ferulic acid and salvianolic acid B in serum are Y=3.976 5X + 0.431 0(r=0.999 9)，Y=70.262X + 69.141 0(r=0.999 9)，Y=34.729X- 2.404 4(r= 0.999 6) ，respectively. The linear regression equations of hydroxysafflor yellow A，ferulic acid and salvianolic acid B in brain tissue are Y=4.586 9X-0.096 3(r=0.999 8)，Y=70.859X+100.040 0(r=0.998 1)，Y=42.176X+18.242 0(r=0.999 5)，respectively. There was no significant difference in the concentration of the three active monomers in serum and brain tissue(P＞0.05). Three of hydroxysafflor yellow A，ferulic acid and salvianolic acid B passed through the BBB，and the BBB penetration rates of them were 1.22% ， 1.27% and 0.87% ， respectively. Conclusion： Three active monomers， hydroxysafflor yellow A， ferulic acid and salvianolic acid B，were detected in serum and brain tissue，after administered oral Guanxin Ⅱ in rats. Three of them passed through the BBB，and three of them maybe the potential therapeutic components of Guanxin Ⅱ.