Safety and Pharmacokinetic Study of Sublingual Flumazenil (CRLS035) in Healthy Adults
Status:
Completed
Trial end date:
2012-08-01
Target enrollment:
Participant gender:
Summary
This study compare the pharmacokinetic (PK) profile of sublingual CRLS035 (two doses) to I.V
flumazenil administration.
Selection of study drug dosage: CRLS035 - sublingual Flumazenil will be administrated at a
final dosage of 1.1 mg per 100 µl and 2.2 mg (200 µl) in a sublingual spray administration.
Currently, Flumazenil is given as an IV drug with a repetitive administration of doses of 0.2
mg up to 3 mg per hour. As the bioavailability of Flumazenil is expected to be lower than the
IV administration, 1.1 mg and 2.2 mg will be tested in sublingual delivery. The suggested
doses in this study are very safe according to the following data: first, sublingual and
buccal administration of Flumazenil have been detailed previously with similar and higher
doses with no side effects, secondly, IV dose may reach 3 mg and thirdly, oral administration
has been reported as up to 600 mg/dose.
The purpose of this study is to determine the single dose PK profile of SL CRLS035. This
study is designed to collect short-term safety data and to monitor the PK profile of CRLS035.
Primary Objective The primary objective is to determine the single dose safety and PK profile
of SL CRLS035 using the marketed IV flumazenil formulation as the comparator.
Secondary Objectives The secondary objectives are to (1) characterize the concentration time
course of two dose levels of SL CRLS035 to support dose selection for Phase 2 and 3 studies
and to evaluate the safety and tolerability of flumazenil formulations; (2)To evaluate the
effect of high fat diet and water consumption on the PK profile.