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British Journal of Anaesthesia, 1988, Vol. 60, No. 1 64-69
© 1988 The Board of Management and Trustees of the British Journal of Anaesthesia

research-article

COMPARATIVE IN VIVO AND IN VITRO ASSESSMENT OF THE PERCUTANEOUS ABSORPTION OF LOCAL ANAESTHETICS

D. F. MCCAFFERTY, B.SC., PH.D., M.P.S.N.I., A. D. WOOLFSON, B.SC., PH.D., M.P.S.N.I., K. H. MCCLELLAND, B.SC., M.P.S.N.I. and V. BOSTON, M.D., F.R.C.S.,

Department of Pharmacy, The Queen's University of Belfast, Medical Biology Centre 97 Lisburn Road, Belfast BT9 7BL.
Northern Ireland Paediatric Surgical Service, Royal Belfast Hospital For Sick Children Falls Road, Belfast BT12.

The percutaneous absorption of local anaesthetics in a standard formulation has been compared in vitro and in vivo. In vitro data were obtained with a modified Sartorius absorption system and silastic as a lipophilic barrier membrane. With this system the greatest steady-state flux values and permeability coefficients were obtained with amethocaine and lignocaine. These drugs also performed best in an in vivo volunteer trial. However, statistical analysis revealed that amethocaine was significantly better at producing full-depth anaesthesia to the challenge of insertion of a sterile needle. An optimized amethocaine formulation may therefore be expected to meet most closely the ideal profile for a percutaneous local anaesthetic preparation.


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