Abstract: To study the pharmacokinetics of blonanserin tablets in thirty Chinese healthy volunteers grouped into three single-dose levels of 4, 8 and 12 mg. The blood samples were collected up to 60 h after oral administration. The plasma concentration of blonanserin was determined by a validated LC-MS/MS method. The pharmacokinetic parameters were calculated by DAS 3. 2. 4 software. The main pharmacokinetic parameters of blonanserin after the single dose of 4, 8 and 12 mg were as follows: c_max were(539. 61±388. 74), (1 190. 39±736. 51)and(1 637. 34±481. 45)ng/L; t_max were(1. 00±0. 47), (1. 38 ±0. 79)and(1. 43±0. 94)h; t_1/2 were(12. 05±3. 49), (14. 76±3. 78)and(13. 68±3. 92)h; AUC_{0-60 h} were(4 692. 21±3 041. 75), (7 964. 42±3 988. 07)and(9 648. 22±2 565. 07)ng ·h/L; AUC_0-∞ were(5 060. 91±3 146. 10), (8 547. 61±4 209. 87)and(9 986. 15±2 659. 51)ng ·h/L, respectively. The main pharmacokinetic parameters of blonanserin positively correlated with the dose over the range of 4-12 mg.