Pharmacokinetics of Licarbazepine in Healthy Volunteers: Single and Multiple Oral Doses and Effect of Food

¹ Novartis Pharma AG
² F. Hoffmann-LaRoche Ltd
³ Novartis Pharma SAS

^* To whom correspondence should be addressed. E-mail: claire.souppart{at}novartis.com.

	Abstract

Two studies characterized single- and multiple-dose pharmacokinetics of licarbazepine immediate-release tablets and food effects on single-dose pharmacokinetics. In 1 study, 12 volunteers received 500 mg licarbazepine on day 1, 500 mg bid on days 3 to 6, and 500 mg on day 7. In the second study, 12 subjects received one 500-mg licarbazepine dose under fasted and fed conditions. After multiple dosing, geometric mean (%CV) C^ss_max, C^ss_min, and AUC were 77.6 µmol/L (18), 45.3 µmol/L (25), and 747 h·µmol/L (19), respectively, with a t_max of 2 hours. Mean half-lives were 9.3 and 11.3 hours for single and multiple dosing, respectively. Food had no clinically significant effect on single-dose pharmacokinetics. Half-life (~10 hours) and low intersubject variability in main pharmacokinetic parameters were similar under fasted and fed conditions. Median t_max increased from 1.5 to 2.5 hours with food. Licarbazepine is well tolerated and has predictable pharmacokinetics.