Akerman B, Haegerstam G, Pring B G, Sandberg R
Acta Pharmacol Toxicol (Copenh). 1979 Jul;45(1):58-65. doi: 10.1111/j.1600-0773.1979.tb02361.x.
The percutaneous penetration of the local anaestetic lidocaine was investigated in the guinea-pig. Three different types of composition were employed: lidocaine hydrochloride in aqueous solution, lidocaine base in an aqueous alcoholic solvent mixture and lidocaine base in aqueous solutions of dipolar aprotic solvents. The latter solvents included simple tertiary aliphatic amides, amides related to dimethylacetamide, some cyclic amides as well as a number of miscellaneous compounds. The degree of dermal anaesthesia was noted in each case. In addition, the uptake and distribution of lidocaine in the skin and its absorption into the blood were studied using tritium-labelled drug. The results show that the percutaneous penetration of lidocaine is dependent on the concentration of the agent, the time of epicutaneous application of the composition, whether the agent was used as salt or free base, and the nature of the solvent medium. Lidocaine base in aqueous dimethylacetamide was most effective in producing percutaneous local anaesthesia.
在豚鼠身上研究了局部麻醉药利多卡因的经皮渗透情况。采用了三种不同类型的组合物：盐酸利多卡因水溶液、利多卡因碱在乙醇水溶液混合溶剂中以及利多卡因碱在偶极非质子溶剂的水溶液中。后一种溶剂包括简单的叔脂肪族酰胺、与二甲基乙酰胺相关的酰胺、一些环状酰胺以及许多其他化合物。记录每种情况下的皮肤麻醉程度。此外，使用氚标记药物研究了利多卡因在皮肤中的摄取、分布及其吸收入血情况。结果表明，利多卡因的经皮渗透取决于药物浓度、组合物表皮应用时间、药物是以盐还是游离碱形式使用以及溶剂介质的性质。二甲基乙酰胺水溶液中的利多卡因碱在产生经皮局部麻醉方面最有效。
