Brand Rhonda M, Charron Anna R, Brand Randall E
Department of Internal Medicine, Evanston Northwestern Healthcare and Feinberg School of Medicine at Northwestern University, 1001 University Place, Evanston, IL 60201, USA.
Int J Pharm. 2005 Sep 14;301(1-2):48-53. doi: 10.1016/j.ijpharm.2005.05.023.
Head lice are the most common parasitic infestation in the United States requiring topical treatment with pediculicides. Ovide, the 0.5% malathion formulation used in treatment of head lice requires placement on dry hair for 8-12 h. Malathion, however, is effective at killing lice and nits in 10 min. Our concern of over exposing children to malathion has led us to examine whether significantly more malathion will penetrate transdermally when applied for the recommended 8 h than for a shorter but apparently equally effective period.
In vitro absorption studies were performed across haired rat skin and human abdominal skin to determine whether reducing malathion application time decreased skin absorption.
A 0.5 h exposure caused 0.36+/-0.14% of the donor malathion to penetrate through human skin after 24 h and 2.1+/-0.6% remained in the skin after washing with shampoo. After 8 h of topical applications penetration was approximately three-fold greater (1.02+/-0.41) and 3.4+/-0.5% remained in the skin (p<0.05 versus 0.5 h). The relationship between absorption and exposure time also occurred for haired rat skin (p<0.05). This differential continued for 72 h even after removal of the source.
Significantly less malathion penetrated from Ovide after 0.5 h versus the suggested 8 h application, without decreasing the product's efficacy. Further clinical studies in children are warranted to confirm the efficacy of this shortened application time.
头虱是美国最常见的寄生虫感染,需要使用杀虱剂进行局部治疗。用于治疗头虱的0.5%马拉硫磷制剂Ovide需要涂抹在干发上8至12小时。然而,马拉硫磷在10分钟内就能有效杀死虱子和虱卵。我们担心儿童过度接触马拉硫磷,因此研究了按照推荐的8小时使用时,经皮渗透的马拉硫磷是否会比使用更短但显然同样有效的时间显著增多。
通过有毛大鼠皮肤和人腹部皮肤进行体外吸收研究,以确定缩短马拉硫磷的涂抹时间是否会降低皮肤吸收。
暴露0.5小时后,24小时内有0.36±0.14%的供体马拉硫磷穿透人皮肤,用洗发水清洗后,2.1±0.6%的马拉硫磷留在皮肤中。局部涂抹8小时后,穿透率约增加了三倍(1.02±0.41),3.4±0.5%的马拉硫磷留在皮肤中(与0.5小时相比,p<0.05)。有毛大鼠皮肤也出现了吸收与暴露时间之间的这种关系(p<0.05)。即使去除源物质后,这种差异仍持续72小时。
与建议的8小时涂抹时间相比,Ovide在涂抹0.5小时后经皮渗透的马拉硫磷显著减少,且不降低产品疗效。有必要在儿童中进行进一步的临床研究,以证实这种缩短涂抹时间的疗效。