Inclusion of lignocaine base into a polar lipid formulation--in vitro release, duration of peripheral nerve block and arterial blood concentrations in the rat

Acta Anaesthesiologica Scandinavica
Henrik DyhreH Renck

Abstract

Slow-release formulations of local anaesthetics may produce nerve blocks of long duration. The present study aimed at investigating the in vitro and in vivo properties of a polar lipid formulation for slow release of lignocaine and the effects on nerve block duration by inclusion of dexamethasone into the system. In vitro release of lignocaine from the lipid formulation was studied in a US Pharmacopoeia rotating apparatus. Sciatic nerve blocks were induced in rats by 0.1 ml of test formulations containing lignocaine HCl 20 mg. ml-1 in aqueous solution, lignocaine base 20, 100 or 200 mg. ml-1 in lipid formulation or the last formulation with dexamethasone 0.05, 0.5 or 5 mg. ml-1. The durations of sensory and motor block and the arterial blood concentrations of lignocaine were investigated. In vitro there was a sustained release of lignocaine from the lipid formulation, with 50% release at around 48 h. In vivo lignocaine base 20 mg. ml-1 in lipid formulation produced sciatic nerve blocks of significantly shorter duration than lignocaine HCl 20 mg. ml-1 in aqueous solution, while lignocaine base 100 and 200 mg. ml-1 in lipid formulation produced blocks lasting two and three times longer, respectively, than the lignocaine HCl solut...Continue Reading

References

May 1, 1980·Journal of Pharmaceutical Sciences·G B ParkJ Edelson
Oct 1, 1994·Anesthesia and Analgesia·G J GrantL Langerman
May 1, 1996·Acta Anaesthesiologica Scandinavica·A Johansson

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Citations

Oct 5, 2006·Current Opinion in Anaesthesiology·Guy L Ludbrook, Richard N Upton
May 16, 2006·Journal of Controlled Release : Official Journal of the Controlled Release Society·Lars SöderbergSven Björkman
Jul 4, 2018·Journal of Liposome Research·Ana Cláudia Pedreira de AlmeidaEneida de Paula
Apr 22, 2003·European Journal of Anaesthesiology·K PayneG A McHugh
Apr 22, 2003·European Journal of Anaesthesiology·A Manohin, M Manohin
Apr 22, 2003·European Journal of Anaesthesiology·K HellwagnerF X Lackner
Apr 22, 2003·European Journal of Anaesthesiology·S GoelV K Grover
Apr 22, 2003·European Journal of Anaesthesiology·S WhiteK Henderson
Apr 22, 2003·European Journal of Anaesthesiology·K PayneG A McHugh
Apr 22, 2003·European Journal of Anaesthesiology·A P Klockgether-RadkeG Hellige
Apr 22, 2003·European Journal of Anaesthesiology·N W F Linton, R A F Linton
Apr 22, 2003·European Journal of Anaesthesiology·J DahnK Hörmann
Apr 22, 2003·European Journal of Anaesthesiology·M KayaD N Kadiogullari
Apr 22, 2003·European Journal of Anaesthesiology·M FattoruttoL Barvais

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