Abstract: AIM: To establish a method in determination of CPU-0213 in serum of mice and rats and to investigate the pharmacokinetics parameters after a single injection at the dose of 80 mg·kg^-1.METHODS: The concentration of CPU-0213 in serum was assayed by HPLC and the pharmacokinetics parameters were calculated by the program of 3P97.RESULTS: The linearity of CPU-0213 ranged from 0.4 to 200 mg·L^-1(r=0.9998) and the limit of quantity was 35 μg·L^-1.The RSD of intra-day was less than 2.7 %and that of inter-day was less than 6.3 %.The recovery was more than 95.9 %.The disposition was conformed to a two-compartment model. The T_1/2β of CPU-0213 in mice and rats were 83.0±1.8 and 96.6±11.5 min, respectively.CONCLUSION: The study provides a simple, stable and special method for determining of concentrations of CPU-0213 in serum of mice and rats.After intravenously injection of CPU-0213 at a single dose, there is no significantly difference in the pharmacokinetics patterns of CPU-0213 in mice and rats.

Key words: endothelin receptor antagonist, CPU-0213, HPLC, mice, rats, single intravenous injection, drug concentration in the serum, 3P97, pharmacokinetics, two-compartment model