Numajiri S, Sakurai H, Sugibayashi K, Morimoto Y, Omiya H, Takenaka H, Akiyama N
Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Josai University, Saitama, Japan.
J Pharm Pharmacol. 1993 Jul;45(7):610-3. doi: 10.1111/j.2042-7158.1993.tb05662.x.
A direct current (DC) system and a pulsed depolarization (PD) system were evaluated for their iontophoretic permeation of sodium benzoate, as a model drug, through hairless rat and human skin. Approximately the same initial permeation of sodium benzoate through the hairless rat skin was obtained at 0.1 mA for the DC device and at 3.0 mA for the PD device. Study of the drug's permeation was performed using a two-chamber iontophoretic diffusion cell, over two cycles of three successive on-off experimental conditions [stage I (off) 0-4 h, II (on) 4-6 h, III (off) 6-10 h, saline washing 10-24 h, IV (off) 24-28 h, V (on) 28-30 h and VI (off) 30-34 h]. Skin permeation rate during stage IV of the iontophoresis as compared with the control group through hairless rat or human skin for the DC system was 2-4 times that in stage I, whereas in the same stage using the PD system it was almost the same as in stage I. Impedance of skin decreased during the application of either system (stage II); however, the value significantly recovered during stage III only in the case of the PD system use on human skin. Histological observation revealed no tissue alteration in the hairless rat skin after using either system. When the DC or PD system was applied to volunteers, the minimum current density producing pain was 0.016 or 2.7 mA cm-2, respectively.(ABSTRACT TRUNCATED AT 250 WORDS)
评估了直流(DC)系统和脉冲去极化(PD)系统对苯甲酸钠作为模型药物通过无毛大鼠和人体皮肤的离子导入渗透情况。对于直流装置,在0.1 mA时通过无毛大鼠皮肤的苯甲酸钠初始渗透率与对于脉冲去极化装置在3.0 mA时大致相同。使用两室离子导入扩散池,在三个连续的开-关实验条件的两个周期内进行药物渗透研究[第一阶段(关)0-4小时,第二阶段(开)4-6小时,第三阶段(关)6-10小时,盐水冲洗10-24小时,第四阶段(关)24-28小时,第五阶段(开)28-30小时,第六阶段(关)30-34小时]。与对照组相比,直流系统通过无毛大鼠或人体皮肤在离子导入第四阶段的皮肤渗透速率是第一阶段的2-4倍,而在同一阶段使用脉冲去极化系统时,其与第一阶段几乎相同。在任一系统应用期间(第二阶段)皮肤阻抗均降低;然而,仅在对人体皮肤使用脉冲去极化系统的情况下,第三阶段阻抗值才显著恢复。组织学观察显示,使用任一系统后无毛大鼠皮肤均无组织改变。当将直流或脉冲去极化系统应用于志愿者时,产生疼痛的最小电流密度分别为0.016或2.7 mA/cm²。(摘要截于250字)