Abstract: Objective To compare the pharmacokinetic parameters of evodiamine hydroxypropyl-β-cyclodextrin inclusion complex and free evodiamine suspension in rats, and investigate the pharmacokinetic characteristics of evodiamine inclusion complex. Methods Both water solubility and cumulative release percentage of EHD were tested with evodiamine as the control. Blood samples were collected from the venous plexus of SD rats after intravenous administration with evodiamine inclusion complex and free evodiamine at 100 mg/kg (equivalent evodiamine dose). Plasma concentrations of evodiamine were determined by high-performance liquid chromatography (HPLC), and the pharmacokinetic parameters were calculated using DAS 2.1.1. Results The evodiamine inclusion complex showed a better water solubility (18.46 ± 0.36 μg/mL) and a higher cumulative release percentage [(76.8±4.9)%] than free evodiamine. The pharmacokinetic parameters of evodiamine inclusion complex and free evodiamine in rats were as follows: Cmax, 252.5±12.43 vs 161.3±3.45 μg/L; Tmax, 4.00±0 vs 4.07±0 h; MRT0-∞, 8.46± 0.91 vs 4.43±0.74 h; AUC0-t, 2266.40±28.64 vs 911.92±8.53 μg·L-1·h-1; AUC0-∞, 2359.76±31.58 vs 919.16±9.73 μg·L-1·h-1. The relative bioavailability of evodiamine inclusion complex was 256.73% . Conclusion Compared with free evodiamine, evodiamine inclusion complex has a higher bioavailability.