A microdialysis study of topically applied diclofenac to healthy humans: Passive versus iontophoretic delivery

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• 作者：Birgit Falk  ; Riecke^a ; Else Marie  ; Bartels^a ;   ; ^{Else.Bartels@frh.regionh.dk} ; S&oslash ; ren  ; Torp-Pedersen^a ; S&oslash ; ren  ; Ribel-Madsen^a ; Henning  ; Bliddal^a ;   ; ^b ;   ; ^c ; Bente  ; Danneskiold-Sams&oslash ; e^a ;   ; ^b ;   ; ^c ;   ; ^{bds@frh.regionh.dk} ; Lars  ; Arendt-Nielsen^c
• 关键词：NSAID ; Diclofenac ; Iontophoresis ; Drug transport ; Administration topical
• 刊名：Results in Pharma Sciences
• 出版年：2011
• 出版时间：May 2011
• 年：2011
• 卷：1
• 期：1
• 页码：76-79
• 全文大小：169 K

文摘

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¡À9.4 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¡À0.5 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.