Sarpotdar P P, Zatz J L
J Pharm Sci. 1986 Feb;75(2):176-81. doi: 10.1002/jps.2600750216.
The effect of two nonionic surfactants (polyoxyethylene sorbitan monoesters) on percutaneous absorption of lidocaine in the presence of various concentrations of propylene glycol is reported. Comparisons were made in vitro using excised hairless mouse skin as the barrier membrane. Under infinite dose conditions, steady-state flux was enhanced by surfactants at high propylene glycol concentrations. The same trend was observed following application of a thin layer of formulation to the skin (finite-dose conditions). However, penetration behavior was complex due to: (a) changes in vehicle composition following application, (b) temperature changes resulting from evaporation or moisture uptake, and (c) depletion of lidocaine as a result of penetration with compositions that lost water by evaporation. Two peaks in the flux versus time curve were observed. Surfactant monomer concentration in the vehicles was increased in the presence of propylene glycol.
报告了两种非离子表面活性剂（聚氧乙烯山梨醇单酯）在不同浓度丙二醇存在下对利多卡因经皮吸收的影响。使用切除的无毛小鼠皮肤作为屏障膜进行体外比较。在无限剂量条件下，高丙二醇浓度时表面活性剂可增强稳态通量。在皮肤涂抹薄层制剂（有限剂量条件）后也观察到相同趋势。然而，渗透行为较为复杂，原因如下：(a) 涂抹后载体组成发生变化；(b) 蒸发或吸湿导致温度变化；(c) 因涂抹的组合物蒸发失水，利多卡因渗透后耗尽。通量与时间曲线中观察到两个峰值。丙二醇存在下载体中表面活性剂单体浓度增加。
