OBJECTIVE: To study the effects of borneol on the penetration of asiaticoside through the blood brain barrier in rats. METHODS: 144 SD rats were randomly divided into 4 groups,36 for each group. Group A was given asiaticoside 30 mg/kg intragastrcally; group B given asiaticoside 30 mg/kg via tail vein; group C given bornel 100 mg/kg intragastrcally and asiaticoside 30 mg/kg intragastrcally; group D given bornel 100 mg/kg intragastrcally and asiaticoside 30 mg/kg via tail vein. The concentrations of asiaticoside in brain tissue were determined by HPLC at 15, 30, 60, 90, 180, 300 min after medication, and pharmacokinetic parameters were calculated by DAS 2.0 software. RESULTS: Asiaticoside was not found in group A. The pharmacokinetic parameters of group B, C and D were that cmax were (0.61±0.03), (0.85±0.08), (0.99±0.08) mg/L; AUC0-300 min were (55.39±2.71), (89.88±7.30), (92.24±9.24) μg·min/ml; AUC0-∞ were (58.52±2.75), (92.90±7.08), (93.16±8.62) μg·min/ml, respectively. cmax, AUC0-300 min and AUC0-∞ of group C and D were obviously higher than those of group B (P<0.05 or P<0.01). CONCLUSIONS: Borneol can enhance the penetration of asiaticoside through blood brain barrier of rats, so as to increase the concentration of asiaticoside in the brain tissue.