The pharmacokinetic properties of deramciclane fumarate (EGIS-3886; (1R,2S,4R)-(-)-N,N-dimethyl-2-[(1,7,7-trimethyl-2-phenylbicyclo-[2,2,1]-hept-2 -yl)oxy]ethanamine-2-(E)-butendioate (1:1)), a new potential anxiolytic agent, were investigated in Beagle dogs after 0.5 and 3.0 mg kg-1 single oral doses. Plasma levels of deramciclane were determined by a highly sensitive, validated gas chromatograpic-nitrogen selective detection (GC-NPD) method using a solid-phase extraction (SPE) technique. The pharmacokinetics of deramciclane in dogs can be described by a two-compartment open model. Absorption was relatively fast and the maximum plasma concentrations (C(max) 7.3 ng mL-1; 99.9 ng mL-1) were reached at 2.17 h (t(max)) after the administration of 0.5 and 3.0 mg kg-1 doses, respectively. The biological half-life (t(β1/2)) were 9.32 and 8.46 h after 0.5 and 3.0 mg kg-1 oral doses, respectively. Comparison of the C(max) and AUC(0-∞) values indicated a tendency toward non-linear pharmacokinetics. The values of volume of distribution (Vd(ss)) (143.13; 44.10 L kg-1) suggested relatively marked tissue-binding by deramciclane.
|Number of pages||4|
|Publication status||Published - Dec 1 1997|
ASJC Scopus subject areas
- Pharmaceutical Science