McCafferty D F, Woolfson A D, McClelland K H, Boston V
Department of Pharmacy, Queen's University of Belfast, Northern Ireland.
Br J Anaesth. 1988 Jan;60(1):64-9. doi: 10.1093/bja/60.1.64.
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.
已对标准制剂中局部麻醉药的经皮吸收进行了体外和体内比较。体外数据是通过改良的赛多利斯吸收系统获得的，其中硅橡胶作为亲脂性屏障膜。使用该系统，丁卡因和利多卡因获得了最大的稳态通量值和渗透系数。在一项体内志愿者试验中，这些药物也表现最佳。然而，统计分析显示，在应对无菌针头插入的刺激时，丁卡因在产生全层麻醉方面明显更好。因此，预计优化的丁卡因制剂可能最接近经皮局部麻醉制剂的理想特性。
