Acino AG, Miesbach 83714, Germany.
J Pharm Sci. 2012 Jan;101(1):245-55. doi: 10.1002/jps.22765. Epub 2011 Sep 23.
A new type of electrochemical transdermal patch has been investigated using release/permeation experiments with excised nude mouse skin. The patch comprises a drug-containing hydrogel sandwiched between two electrodes that are arranged parallel to the skin surface. The objective was to determine the mechanism of working of enhanced flux for the drug fentanyl when low voltages are applied. The results indicate that a voltage-induced hydrolysis of the water present in the patch's hydrogel occurs. This causes a pH shift that results in deprotonization of the fentanyl and hence enhanced release/permeation. The enhanced flux is up to approximately 30 μg/(cm(2) h) over 20 h and requires only a low-voltage application over a duration of just 60 s. Because the enhancement mechanism occurs in the patch and not in the skin, the potential for substantially reduced skin irritation compared with iontophoresis is given.
采用离体裸鼠皮肤的释放/渗透实验研究了一种新型电化学经皮贴片。该贴片由夹在两个平行于皮肤表面的电极之间的含药水凝胶组成。目的是确定在施加低电压时,药物芬太尼通量增强的工作机制。结果表明,贴片水凝胶中存在的水发生电压诱导水解。这导致 pH 值发生变化,导致芬太尼去质子化,从而增强释放/渗透。增强的通量在 20 小时内高达约 30 μg/(cm(2) h),并且仅需在 60 秒的持续时间内施加低电压。由于增强机制发生在贴片中而不是在皮肤中,与离子电渗法相比,皮肤刺激性大大降低的潜力。