A Pharmacokinetic Bioequivalence Study Comparing Sublingual Riluzole (BHV ‐0223) and Oral Tablet Formulation of Riluzole in Healthy Volunteers

This study assessed the bioequivalence between 40‐mg BHV‐0223 and standard 50‐mg oral riluzole tablets, and the food effect on BHV‐0223 pharmacokinetics in healthy volunteers. Overall, 133 healthy subjects received BHV‐0223 and riluzole tablets under fasted conditions. Geometric mean ratios for the area under the plasma concentration–time curve (AUC) from time zero to time of last nonzero concentration (AUC0 ‐t) (89.9%; confidence interval [CI], 87.3% –92.5%), AUC from time zero to infinity (AUC0 ‐∞) (89.8%; CI, 87.3% –92.4%), and maximum observed concentration (112.7%; CI, 105.5%–120.4%) all met bioequivalence criteria (80%–125%). Subsequently, 67 subjects received BHV‐0223 under fed conditions. The geometric mean ratios of AUC0 ‐t (91.2%; CI, 88.1 –94.3%), and AUC0 ‐∞ (92.0%; CI, 89.0 –95.1%) were similar, but maximum observed concentration ratios were not within bioequivalence criteria. BHV‐0223 was well tolerated. This study demonstrated that 40‐mg sublingual BHV‐0223 is bioequivalent to 50‐mg oral riluzole tablets.

Source: Clinical Pharmacology in Drug Development - October 13, 2019 Category: Drugs & Pharmacology Authors: Irfan Qureshi, Meghan Lovegren, Victoria Wirtz, Richard Larouche, Mario Tanguay, Matt S. Anderson, Sonja Hartmann, Vlad Coric, Robert M. Berman Tags: Original Manuscript Source Type: research