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首页> 外文期刊>Skin research and technology: official journal of International Society for Bioengineering and the Skin (ISBS) [and] International Society for Digital Imaging of Skin (ISDIS) [and] International Society for Skin Imaging (ISSI) >Determination of the in vivo bioavailability of iontophoretically delivered diclofenac using a methyl nicotinate skin inflammation assay.
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Determination of the in vivo bioavailability of iontophoretically delivered diclofenac using a methyl nicotinate skin inflammation assay.

机译：使用烟酸甲酯皮肤炎症试验确定离子电渗入的双氯芬酸的体内生物利用度。

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摘要

In this study, we investigated the bioavailability of iontophoretically delivered diclofenac with the methylnicotinate (MN) test. The inhibition of an erythema provoked by MN is proportional to the bioavailability of diclofenac in the skin. It was our aim to use this procedure in the determination of the contribution of, respectively, passive diffusion, occlusion and electrically assisted delivery during an iontophoretic procedure as used in physiotherapy. A total of six application sites were marked on the volar forearms of each volunteer (n=12), for the following treatment and/or control modes: A=cathodal iontophoresis of 12 mg/cm(2) Voltaren Emulgel((R)) (diethylammonii diclofenac 1%) for 20 min; B=passive diffusion under a contact sponge; C=passive diffusion without any covering; D=current alone; E=standard MN response; and F=blanco site. Tristimulus surface colorimetry and Laser Doppler flowmetry were used to measure, respectively, the skin color and the perfusion of the microcirculation. Bioavailability was assessed by quantification of an MN-induced erythema under the different conditions. A significant reduction of the MN-induced erythema was observed with the Chromameter and Laser Doppler measurements for the following treatment modalities: (1) electrically assisted delivery: respectively, 65% and 100%, (2) application under a contact sponge: 66% and 97% and (3) passive diffusion without any covering: 32% and 65%. A significant reduction was equally observed for the site treated with the current alone: 19% and 42%. There was no significant difference between the response after iontophoretic-delivered diclofenac (mode A) and application of diclofenac under a contact sponge (mode B). The procedure used enabled us to evaluate the bioavailability of a non-steroidal anti-inflammatory drug in the skin. Under the conditions used, we did not find an increased bioavailability after electrically assisted delivery of diclofenac compared with the passive percutaneous penetration under the contact sponge.
机译：在这项研究中，我们调查了用烟酸甲酯（MN）测试离子电传递双氯芬酸的生物利用度。 MN引起的红斑的抑制与双氯芬酸在皮肤中的生物利用度成正比。我们的目的是在物理疗法中所用的离子电渗疗法过程中，使用该程序分别确定被动扩散，阻塞和电辅助递送的作用。对于以下治疗和/或控制方式，每个志愿者的前臂上总共标记了六个应用部位（n = 12）：A = 12 mg / cm的阴极离子电渗疗法（2）Voltaren Emulgel（R） （二乙胺双氯芬酸1％）20分钟; B =接触海绵下的被动扩散; C ＝无扩散的无源扩散; D =仅电流; E ＝标准MN响应;和F =空白站点。三刺激表面比色法和激光多普勒血流仪分别用于测量皮肤颜色和微循环的灌注。通过在不同条件下对MN引起的红斑进行量化来评估生物利用度。对于以下治疗方式，用色度计和激光多普勒测量可观察到MN引起的红斑明显减少：（1）电辅助输送：分别为65％和100％，（2）在接触海绵下的施加：66％ 97％;（3）无覆盖的被动扩散：32％和65％。对于仅使用电流处理的部位，同样可以观察到明显的减少：19％和42％。离子电渗疗法递送双氯芬酸后的反应（模式A）与在接触海绵下施用双氯芬酸后的反应（模式B）之间没有显着差异。使用的程序使我们能够评估皮肤中非甾体类抗炎药的生物利用度。在使用条件下，与接触海绵下的被动经皮穿透相比，在电辅助递送双氯芬酸后我们没有发现增加的生物利用度。

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