Kitagawa Shuji, Ikarashi Ai
Niigata University of Pharmacy and Applied Life Sciences, Faculty of Pharmaceutical Sciences, Japan.
Chem Pharm Bull (Tokyo). 2003 Oct;51(10):1183-5. doi: 10.1248/cpb.51.1183.
Using excised guinea pig dorsal skin, we examined the effects of three surfactants, anionic sodium dodecylsulfate (SDS), cationic n-dodecyltrimethylammonium bromide and non-ionic n-dodecyl-beta-D-maltoside, all of which commonly have an n-dodecyl group, on in vitro skin permeation of the cationic drug ketotifen. All these three surfactants increased the skin permeation of ketotifen. Among the surfactants tested, anionic SDS had the largest enhancement effects, and significantly increased the permeation at concentrations over 1 mM. The enhancement effect of the same anionic surfactant on the permeation of anionic salicylate was smaller and similar to that of cationic n-dodecyltrimethylammonium. The enhancement effects of SDS on ketotifen permeation were more marked than those of the cationic surfactant but differed from previous findings of their effects on other drugs permeation. Analysis of the retention of ketotifen in the skin suggested that SDS-induced increase in the transfer of hydrophilic ketotifen to the skin is the main reason for the marked increase in skin permeation.
我们使用切除的豚鼠背部皮肤，研究了三种表面活性剂，即阴离子型十二烷基硫酸钠（SDS）、阳离子型正十二烷基三甲基溴化铵和非离子型正十二烷基-β-D-麦芽糖苷（它们通常都含有一个正十二烷基）对阳离子药物酮替芬体外皮肤渗透的影响。这三种表面活性剂均增加了酮替芬的皮肤渗透。在所测试的表面活性剂中，阴离子型SDS的增强作用最大，在浓度超过1 mM时显著增加了渗透率。相同的阴离子表面活性剂对阴离子型水杨酸酯渗透的增强作用较小，与阳离子型正十二烷基三甲基溴化铵的作用相似。SDS对酮替芬渗透的增强作用比阳离子表面活性剂更显著，但与之前关于它们对其他药物渗透影响的研究结果不同。对酮替芬在皮肤中的滞留情况分析表明，SDS诱导亲水性酮替芬向皮肤转移增加是皮肤渗透显著增加的主要原因。
