Abstract: OBJECTIVE To prepare buddleoside-phospholipids complex, and then investigate its pharmacokinetic properties. METHODS The buddleoside-phospholipids complex was prepared by solvent evaporation method, and the compounding rate was used as the evaluation index. The preparation process was optimized by orthogonal experiment. After SD rats were administrated with drugs, the blood concentration of buddleoside was detected by HPLC. RESULTS The recombination ratio of buddleoside-phospholipids complex was near to 100% under the optimized preparations. The results of X-ray diffraction indicated that buddleoside showed an amorphous state in the complex. The solubility in water and octanol was enhanced greatly. Pharmacokinetic results in SD rats showed that the t_max, C_max, AUC_0-t and other parameters of the complex has significant difference compared to buddleoside suspension. The bioavailability of buddleoside was enhanced to 1.11 times by the complex. CONCLUSION The phospholipids complex improved the solubility property of buddleoside, and the oral bioavailability of buddleoside was improved significantly.