OBJECTIVE： To study the pharmacokinetic characteristics of evodiamine liposome in rats and the tissue distribution and targeting in mice. METHODS： The rats were randomly divided into 2 group with 8 rats in each group； they were given evodiamine liposomes and solution （10 mg/kg by evodiamine） via tail vein respectively. 0.5 ml fundus venous plexus blood were sampled respectively at 0.083， 0.25， 0.5， 0.75， 1， 1.5 ，2， 3， 4 and 5 h after administration. The plasma concentration of evodiamine in rats were measured by HPLC. The pharmacokinetic parameters were calculated by DAS 2.1.1 software. The mice were randomly divided into 2 groups with 30 rats in each group； they were given evodiamine liposomes and solution （8 mg/kg by evodiamine） via tail vein respectively. The heart， liver， spleen， lung and kidney tissues were removed immediately after every 3 mice were sacrificed at 0.083，0.25，0.5，1，2，4，6，8，10，12 h after administration. The concentrations of evodiamine were measured by HPLC， and the distribution of evodiamine in each tissue was analyzed. RESULTS： The pharmacokinetics of evodiamine liposomes and solutions in rats were in line with non-compartment model； their pharmacokinetic parameters were as follows as t1/2 of （1.78±0.58） h and（1.06±0.40） h， AUC0-t of （4.63±0.33） μg·h/ml and （2.75±0.09） μg·h/ml （P＜0.01）. The concentrations of evodiamine in each tissue of mice were in descending trend as liver＞spleen＞lung＞heart＞kidney， and spleen＞liver＞kidney＞heart＞lung. CONCLUSIONS： Compared with solution， liposomes promote the absorption of evodiamine and the distribution of it in liver， showing good liver targeting.