alexa Pharmacokinetics and Safety of Sublingual Flumazenil (CRLS035) in Healthy Adults (Potential Therapy for Hepatic Encephalopathy)
ISSN: 2153-0645

Journal of Pharmacogenomics & Pharmacoproteomics
Open Access

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Research Letter

Pharmacokinetics and Safety of Sublingual Flumazenil (CRLS035) in Healthy Adults (Potential Therapy for Hepatic Encephalopathy)

Saadi T1, Kramskay R1, Zilberman Peled B2, Katz N3, Peled N2 and Baruch Y1,4*

1Liver Unit, Rambam Health Care Campus, Haifa, Israel

2Coeruleus Ltd, Israel

3Sleep Laboratory, Assuta Medical Center, Tel Aviv, Israel

4Bruce Rappaport Faculty of Medicine, Technion-Israel Institute of Technology, Haifa, Israel

*Corresponding Author:
Dr. Yaacov Baruch, MD
Liver Unit, Rambam Health Care Campus
POB 9602, Haifa 31096, Israel
Tel: +972-4-854-3049
Fax: +972-4-854-2477
E-mail: [email protected]

Received date: August 08, 2014; Accepted date: September 11, 2014; Published date: September 20, 2014

Citation: Saadi T, Kramskay R, Peled BZ, Katz K, Peled N, et al. (2014) Pharmacokinetics and Safety of Sublingual Flumazenil (CRLS035) in Healthy Adults (Potential Therapy for Hepatic Encephalopathy). J Pharmacogenomics Pharmacoproteomics 5:140. doi: 10.4172/2153-0645.1000140

Copyright: © 2014 Saadi T, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.



Flumazenil, a GABAA receptor antagonist, has a significant clinical benefit especially in overt hepatic encephalopathy patients, although it requires intravenous access. A novel highly concentrated sublingual spray formulation of flumazenil (CRLS035) was developed by Coeruleus Ltd. The aim of this study was to determine the single dose safety and pharmacokinetics of sublingual CRLS035 versus flumazenil intravenously (IV) in healthy volunteers.
Ten healthy adult volunteers participated in the study. CRLS035 was administered sublingually in two doses (1.1 mg and 2.2 mg) vs. IV flumazenil (0.2 mg). Subjects were evaluated after a high-fat diet and water consumption. Blood samples were collected pre- and post-dose at eight time points. Flumazenil levels were analyzed for Cmax, Tmax, Cmin, Tmin, AUC0-∞, AUC0-t and T1/2. Safety variables included local oral area and assessment of systemic adverse events.
The estimated bioavailability of the two sublingual doses was 14% and 11%, respectively. The bioequivalence of the 1.1 mg sublingual dose was similar to the 0.2 mg IV dose. Water consumption and the high-fat diet did not change the pharmacokinetic parameters significantly. No associated adverse events were reported across the study.
The pharmacokinetics of sublingual flumazenil is comparable to intravenous administration and the drug is safe. The sublingual approach allows convenient and better treatment availability for patients with hepatic encephalopathy.


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