Riecke Birgit Falk, Bartels Else Marie, Torp-Pedersen Søren, Ribel-Madsen Søren, Bliddal Henning, Danneskiold-Samsøe Bente, Arendt-Nielsen Lars
The Parker Institute, Copenhagen University Hospital, Ndr. Fasanvej 57, 2000 Frederiksberg, Denmark.
The Parker Institute, Copenhagen University Hospital, Ndr. Fasanvej 57, 2000 Frederiksberg, Denmark ; Faculty of Health Sciences, Copenhagen University, Copenhagen, Denmark ; Center for Sensory-Motor Interaction, Aalborg University, Aalborg, Denmark.
Results Pharma Sci. 2011 Nov 4;1(1):76-9. doi: 10.1016/j.rinphs.2011.11.001. eCollection 2011 May.
Topical application of NSAIDs is an alternative route to systemic administration when a local anti-inflammatory effect of the underlying tissue is a treatment option. The aim of the present microdialysis study was to assess and compare plasma and tissue levels of diclofenac when topically applied with or without iontophoresis in healthy adults. Fourteen healthy adults (26±9.4 years) were randomized to diclofenac applied by iontophoresis, or by a gel, in a crossover design. Diclofenac concentrations were measured in plasma and in microdialysis perfusates from the underlying tissues. Iontophoretic application resulted in the highest plasma concentration of 3.4±0.5 ng/ml (SEM given) compared to 0.4 ng/ml (at the detection limit) with gel, whereas no differences were observed between tissue concentrations for the two application methods, both being very low, below or around the detection limit. Iontophoresis caused skin reactions in 25% of the participants. Iontophoresis of diclofenac as compared to traditional topical application was not superior in order to increase the NSAID concentration locally and appears to have a higher frequency of skin reactions.
当潜在组织的局部抗炎作用是一种治疗选择时，非甾体抗炎药的局部应用是全身给药的替代途径。本微透析研究的目的是评估和比较在健康成年人中，双氯芬酸在有或没有离子导入的情况下局部应用时的血浆和组织水平。14名健康成年人（26±9.4岁）采用交叉设计，随机分为接受离子导入或凝胶剂给药的双氯芬酸组。测量血浆和来自潜在组织的微透析灌注液中的双氯芬酸浓度。离子导入给药导致血浆浓度最高，为3.4±0.5 ng/ml（给出标准误），而凝胶剂给药时为0.4 ng/ml（在检测限），然而两种给药方法的组织浓度之间未观察到差异，均非常低，低于或接近检测限。离子导入在25%的参与者中引起皮肤反应。与传统局部应用相比，双氯芬酸离子导入在提高局部非甾体抗炎药浓度方面并不优越，且似乎有更高频率的皮肤反应。
