Abstract: AIM: To study the pharmacokinetic profiles of ceptopril, a new ACE inhibitor, in Chinese healthy male and female volunteers. METHODS: 10 healthy volunteers (5 males and 5 females) were en- rolled and 30 mg ceptopril oral dose was given twice daily for 7 days. Another 10 healthy volunteers (5 males and 5 females) were treated with 60mg captopril in the fed and fasted conditions. With the analysis of HPLC for the concentrations of ceptopril in plasma, pharmacokinetic parameters were calculated by Win-Nonlin software. RESULTS: No significant difference was observed between the pharmacokinetic parameters of the 1st dose and the last dose (P >0.05), with values as follows: t_max (1.2±0.5) h and (1.2±0.3)h, C_max (279±100) μg L and (299±101) μg L, AUC0-t (421±107) μg·L^-1 ·h and (461±152)μg·L^-1 ·h, t_1/2 (1.3±0.9) h and (1.3±0.5) h. Compared with those in fasted condition, t_max was prolonged, and AUC and C_max were not significantly changed in fed condition. There was no significant difference between the male and female volunteers. CONCLUSION: There was no accumulation when ceptopril was given with multiple doses. Food affected the absorption rate of ceptopril, but did not decrease its exposure. No sex difference was observed.

Key words: ceptopril, HPLC, pharmacokinetics, food effect