Influence of food on pharmacokinetics of zolpidem from fast dissolving sublingual zolpidem tartrate tablets

Abstract

Ingesting food can impact the pharmacokinetics of sedative‐hypnotic drugs. A buffered zolpidem sublingual tablet (ZST) recently became available for the treatment of middle‐of‐the‐night awakening. In this randomized, open‐label, single‐site study, the pharmacokinetic profile of ZST was evaluated when administered while fasting and following a standard high‐fat meal (fed state). Healthy adults aged 18–64 years received a single morning dose of 3.5 mg ZST in the fed or fasting state. From 20 min to 3 h post‐dose, zolpidem plasma levels were lower in the fed state compared to the fasting state. After 4 h post‐dose (corresponding to “morning wake time”), higher zolpidem plasma levels were evident in the fed state. Area under the concentration‐time curve (AUC) values for the 0–8 h interval were 160 ng/mL h in the fed state and 203 ng/mL h in the fasting state (P < .001). In the fed versus fasting states, C_max was 32.0 ng/mL versus 57.3 ng/mL (P < .001), respectively, and T_max was 3.0 h versus 0.92 h (P < .001), respectively. Together these data suggest that administration of ZST in the fed state is not optimal for maximizing the likelihood of therapeutic benefit and minimizing the probability of residual sedation.