Résumé
OBJECTIVE: To evaluate the pharmacokinetics characteristics and safety of antipsytrotic ziprasidone mesylate with single dose intramuscularly injected in healthy volunteers. METHODS: A total of 12 healthy Chinese volunteers(male 6 cases and female 6 cases) were received intramuscularly single dose of ziprasidone mesylate, the dosage was 10 mg.Blood samples were collected at different time after intramuscularly injection.The concentrations of ziprasidone in serum were determined by LC-MS/MS, and the pharmacokinetic parameters were calculated. RESULTS: The concentration-time curves of ziprasidone fitted to two-compartment model.The pharmacokinetic parameters were stated as follows, ρmax was (97.85± 29.24) ng·mL-1;tmax was (0.56±0.30)h;MRT was (5.35±0.96) h; t1/2 was (4.29±0.88)h; AUC0→t was (405.6±98.68) ng·h·mL-1, AUC0→∞was (413.3± 100.69)ng·h·mL-1; CL was (25.50±6.10)L·h-1; Vd was (157.48±47.60)L; Kel was (0.168±0.035)h. There were no significant differences of the parameters between the male and female subjects. The common adverse events were somnolence, nausea and weakness with the severity of mild to moderate. CONCLUSION: The pharmacokinetic parameters in 12 healthy volunteers after intramuscular injection of 10 mg ziprasidone mesylate are in line with that reported in the literature. This medicine has effect of sedation, so that it could be used to control the excited agitation.