AIM: To study the pharmacokinetics after oral administration of caudatin in rats. METHODS: Blood samples of rats were collected at predetermined intervals for the assay of caudatin after oral administration and the plasma concentration of caudatin was analyzed by LC/ESI-MS/MS method. The pharmacokinetic parameters were also calculated. RESULTS: The half-lives of caudatin were examined to be (1.59 ± 1.08), (0.99 ± 0.27), (1.92 ± 1.55) h after oral administration with caudatin at doses of 10, 20, 40 mg·kg-1. The AUC0-t were (220.6 ± 114.8), (539.1 ± 160.6), (1631.9 ± 915.9) μg·h·L-1, respectively. The cmax were (153.5 ± 79.1), (232.8 ± 119.3), (687.9 ± 245.7) μg·L-1, respectively. The tmax were (0.36 ± 0.35), (1.33 ± 0.61), (0.96 ± 0.68) h, respectively. The relationship between AUC0-t and dose was non-linear. CONCLUSION: The result suggested that the pharmacokinetics of caudatin in rats conform to non-linear kinetics.