EVALUATION OF PENETRATION ENHANCEMENT OF LIDOCAINE BY NONIONIC SURFACTANTS THROUGH HAIRLESS MOUSE SKIN INVITRO
EVALUATION OF PENETRATION ENHANCEMENT OF LIDOCAINE BY NONIONIC SURFACTANTS THROUGH HAIRLESS MOUSE SKIN INVITRO
复制标题
DOI：
10.1002/jps.2600750216
复制
发表时间：
1986-02-01
影响因子：
3.8
通讯作者：
ZATZ, JL
中科院分区：
文献类型：
--
作者：
SARPOTDAR, PP;ZATZ, JL
报道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。体外比较采用切除的无毛小鼠皮肤作为屏障膜。在无限剂量条件下，高丙二醇浓度的表面活性剂增强了稳态通量。在将薄层制剂应用于皮肤（有限剂量条件）后观察到同样的趋势。然而，渗透行为是复杂的，原因是：(a)施用后载药成分的变化，(b)蒸发或吸湿导致的温度变化，以及(c)利多卡因因蒸发失水的成分渗透而耗损。在通量-时间曲线上观察到两个峰。载体中表面活性剂单体浓度在丙二醇存在下增加。
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 behaviour 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.