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Pharmacokinetics and Tolerability of Rufinamide in Healthy Chinese Subjects

Phase 1
Completed
Conditions
Seizures
Interventions
Registration Number
NCT02332174
Lead Sponsor
Wuhan Union Hospital, China
Brief Summary

The purpose of this study was to determine the pharmacokinetic (PK) and safety profile of single and multiple doses of rufinamide. The effects of food and sex on the PK properties of rufinamide in these Chinese volunteers were also evaluated.

Detailed Description

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.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
40
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

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
400-mg grouprufinamideTen healthy subjects were administered a single oral dose of 400 mg rufinamide tablets in fasted state.
200-mg grouprufinamideTen healthy subjects were administered a single oral dose of 200 mg rufinamide tablets in fasted and fed state at day 1 and then received repeated oral doses of rufinamide (200 mg) once daily for 6 days.
800-mg grouprufinamideTen healthy subjects were administered a single oral dose of 800 mg rufinamide tablets in fasted state.
1200-mg grouprufinamideTen healthy subjects were administered a single oral dose of 1200 mg rufinamide tablets in fasted state.
Primary Outcome Measures
NameTimeMethod
AUCthree days

the area under the concentration-time curve

Secondary Outcome Measures
NameTimeMethod
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