Plasma Levels of lormetazepam after Sublingual and Oral Administration of 1 MG to Humans

Abstract

A new galenical formulation containing 1 mg lormeta-zepam (LMZ) for sublingual administration (“sleeping wafer”, see Figure 1) has been developed. In an open-cross over design the plasma lormetazepam levels were monitored radioimmunologically in 16 volunteers. Subjects received the sublingual formulation and an oral tablet (Noctamid^R-1) in a randomized sequence at weekly intervals. After sublingual administration the mean plasma lormetazepam levels were significantly higher between 7.5 and 25 minutes than after administration of the tablet. The earlier rise in plasma LMZ levels is also reflected in partial areas under the plasma level curve up to 45 minutes. LMZ was completely absorbed from both formulations as shown in total AUCs.

It is anticipated that sublingual administration of the new formulation will lead to a 40 - 50 % reduction of sleep latency. Possibilities for therapeutic application of the new formulation are discussed.