OBJECTIVE: To study the pharmacokinetic characteristics of arotinoid ethyl ester (RO) in Beagle dogs in vivo. METHODS: 18 Beagle dogs were randomly divided into high-dose, medium-dose, low-dose groups (40, 20, 10 mg/kg), 6 in each group. Rats were intragastrically administrated related doses of RO. Blood sample 1 mL was taken after 0.5, 1.0, 2.0, 4.0, 6.0, 8.0, 12.0, 24.0, 36.0, 48.0, 60.0, 72.0 h of administration, and plasma was separated. RP-HPLC was used to determine the concentrations of RO and its metabolite arotinoid acetic acid (RA) in plasma. Using DAS 2.0 software for fitting, pharmacokinetic parameters were calculated. RESULTS: Both RO and RA showed a distribution in one-compartment model in dogs in vivo. The cmax of RO high-dose, medium-dose, low-dose groups in dogs in vivo were (0.42±0.87), (0.54±0.09), (0.31±0.05) μg/mL; t1/2z were (1.20±0.33), (1.14±0.45), (1.90±0.65) h; AUC0-72 h were (3.55±0.90), (0.87±0.50), (0.92±0.31) μg·h/mL; and CL/F were (11.99±4.01), (19.87±10.79), (12.29±7.57) L/(kg·h). The cmax of RA high-dose, medium-dose, low-dose groups in dogs in vivo were (32.51±4.04), (19.87±2.78), (16.55±4.06) μg/mL; t1/2z were (7.27±4.20), (7.17±4.20), (10.18±4.01) h; AUC0-72 h were (408.14±96.61), (333.39±61.28), (286.55±30.96) μg·h/mL; and CL/F were (1.30±0.53)、(0.76±0.87)、(0.54±0.10) L/(kg·h). CONCLUSIONS: Orally taking RO is easy to absorb with rapid elimination. Its active metabolite RA has longer accumulation time in vivo.