Comparative in vivo and in vitro assessment of the percutaneous absorption of local anaesthetics.

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.