OBJECTIVE: To study the pharmacokinetic change of albendazole (ABZ) in rats after nanocrystallization, and to lay a foundation for further study of ABZ nano-preparation. METHODS: 16 rats were randomly divided into ABZ raw material (ABZ suspension) group and ABZ nano-powder (ABZ nano-powder suspension) group, with 8 rats in each group. They were given relevant medicine 63 mg/kg intragastrically. 0.2-0.3 ml blood samples were collected from orbital cavity 0.5, 1, 2, 4, 8, 12, 24, 36, 48, 72 h after medication, respectively. Using mebendazole as internal standard, blood concentration of ABZ were determined by RP-HPLC, and pharmacokinetics parameters were calculated by using 3p97 software. RESULTS: The pharmacokinetics of ABZ raw material and ABZ nano-powder in rats were in line with two-compartment model. The main pharmacokinetic parameters of ABZ raw material group vs. ABZ nano-powder group were as follows as cmax (3.20±1.41) μg/ml vs. (6.11±0.74) μg/ml; tmax (3.42±0.91) h vs. (3.15±0.27) h; AUC0-72 h (49.90±15.50) μg·h/ml vs. (78.36±8.78) μg·h/ml; AUC0-∞ (52.30±10.10 ) μg·h/ml vs. (80.27±8.26) μg·h/ml. Compared with ABZ raw material group, cmax, AUC0-72 h and AUC0-∞ of ABZ nano-powder group were increased significantly (P<0.05). CONCLUSIONS: The nanocrystallization of ABZ can enhance the absorbability rate and improve the absorption of drugs to some extent, and it also improves oral bioavailability of ABZ.