Effect of vehicles and penetration enhancers on the in vitro percutaneous absorption of tenoxicam through hairless mouse skin

被引:78
作者
Gwak, HS [1 ]
Chun, IK [1 ]
机构
[1] Dongduk Womens Univ, Coll Pharm, Lab Pharmaceut, Seoul 136714, South Korea
关键词
percutaneous absorption; tenoxicam; penetration enhancers; fatty acids; Amines;
D O I
10.1016/S0378-5173(02)00009-1
中图分类号
R9 [药学];
学科分类号
1007 [药学];
摘要
The effects of vehicles and penetration enhancers on the in vitro permeation of tenoxicam from saturated Solutions through dorsal hairless mouse skin were investigated. Various types of vehicles, including ester-, alcohol-, and ether-types and their Mixtures, were used as vehicles, and then a series of fatty acids and amines were employed as enhancers, respectively. Even though the fluxes of tenoxicam from saturated pure vehicles were generally low (0.1-1.1 mug/cm(2) per h), the skin permeability of tenoxicam was significantly increased by the combination of diethylene glycol monoethyl ether (DGME) and propylene glycol monolaurate (PGML) or propylene glycol monocaprylate (PGMC), the highest fluxes were achieved at 40%, of DGME in both of the two cosolvents. The marked synergistic enhancement was also obtained by using propylene glycol (PG)-oleyl alcohol (OA1) cosolvent. The greatest flux was attained by L the addition of unsaturated fatty acids at 3% concentration to PG. But saturated fatty acids failed to show a significant enhancing effect. The enhancement factors with the addition of oleic acid (OA) or linoleic acid (LOA) to PG were 348 and 238, respectively. Tromethamine (TM) showed an enhancing effect by the increased solubility; however, triethanolamine (TEA) did not show a significant enhancing effect. Rather, it decreased the fluxes of tenoxicam when added to PG with fatty acids. The above results indicate that the combinations of lipophilic vehicles like OA, LOA or OA1 and hydrophilic vehicles like PG can be used for enhancing the skin permeation of tenoxicam. (C) 2002 Elsevier Science B.V. All rights reserved.
引用
收藏
页码:57 / 64
页数:8
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