Pharmacokinetics and Tolerability of Rufinamide in Healthy Chinese Subjects

This single- and multiple-dose, randomized, open-label study was conducted in healthy Chinese subjects. In the single-dose study, volunteers were randomly assigned to 4 dose groups and received a single dose of 200, 400, 800, 1200 mg rufinamide tablets under fasted condition. An additional food effect study was performed in the 200-mg dose group by assessing changes in PK parameters after high-fat diet. In the multiple-dose study, 10 subjects were administered 200-mg rufinamide formulation twice daily for 6 consecutive days. LC-MS/MS method was applied to determine plasma concentration of rufinamide. Tolerability was assessed based on investigator inquiries, spontaneous reports, and clinical evaluations such as standard laboratory tests, vital signs, physical examinations and 12-lead electrocardiography.

Inclusion criteria

• body mass index between19 and 24 kg/m2
• negative for HIV and hepatitis B
• had no clinicallyimportant findings on health tests
• thorax radiography and ECG with no abnormalities
• normal blood pressure values
• heart rate

Exclusion criteria

• any drug treatment within 2 weeks before starting the study
• participation in another clinical study within the previous 3 months
• alcoholism and smoking
• pregnancy
• breast-feeding
• hypocalcemia
• blood donation or participation in other clinical trials within 3 months before enrollment in the study
• sitting blood pressure <80/50 mm Hg or >140/100 mm Hg
• A ventricular rate <60 beats/min or >100 beats/min at rest