Pharmacokinetics of deramciclane in dogs

E. Bojti, J. Leibinger, G. Grezal, I. Klebovich

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)503-506
Number of pages4
JournalPharmaceutical Sciences
Volume3
Issue number10
Publication statusPublished - 1997

Fingerprint

Pharmacokinetics
Dogs
Fumarates
Anti-Anxiety Agents
Solid Phase Extraction
Area Under Curve
Half-Life
Nitrogen
Gases
deramciclane

ASJC Scopus subject areas

  • Pharmaceutical Science

Cite this

Bojti, E., Leibinger, J., Grezal, G., & Klebovich, I. (1997). Pharmacokinetics of deramciclane in dogs. Pharmaceutical Sciences, 3(10), 503-506.

Pharmacokinetics of deramciclane in dogs. / Bojti, E.; Leibinger, J.; Grezal, G.; Klebovich, I.

In: Pharmaceutical Sciences, Vol. 3, No. 10, 1997, p. 503-506.

Research output: Contribution to journalArticle

Bojti, E, Leibinger, J, Grezal, G & Klebovich, I 1997, 'Pharmacokinetics of deramciclane in dogs', Pharmaceutical Sciences, vol. 3, no. 10, pp. 503-506.
Bojti E, Leibinger J, Grezal G, Klebovich I. Pharmacokinetics of deramciclane in dogs. Pharmaceutical Sciences. 1997;3(10):503-506.
Bojti, E. ; Leibinger, J. ; Grezal, G. ; Klebovich, I. / Pharmacokinetics of deramciclane in dogs. In: Pharmaceutical Sciences. 1997 ; Vol. 3, No. 10. pp. 503-506.
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