Murakami T, Ihara C, Kiyonaka G, Yumoto R, Shigeki S, Ikuta Y, Yata N
Department of Biopharmaceutics, Institute of Pharmaceutical Sciences, Hiroshima University School of Medicine, Hiroshima, Japan.
Skin Pharmacol Appl Skin Physiol. 1999 Jul-Aug;12(4):221-6. doi: 10.1159/000066246.
The usefulness of iontophoresis is restricted to highly water-soluble compounds, since drugs are generally applied as an aqueous solution in a drug electrode. In the present study, salicylic acid (SA) dissolved in ethanol-water mixture was loaded in a drug electrode, and the effect of ethanol on the iontophoretic transdermal delivery of SA was evaluated. Ethanol at a concentration of 10 or 30% showed no significant effect on the iontophoretic transdermal delivery of SA compared to that in the absence of ethanol, but 40 or 70% ethanol increased it significantly. The current density passing through in vivo during iontophoretic treatment decreased with increase in ethanol concentrations. These results suggested that the enhanced transdermal absorption of SA iontophoretically by the presence of ethanol in a drug solution is not due to the increased current density in vivo, but probably due to the direct action of ethanol on the stratum corneum. In conclusion, addition of ethanol to a drug solution at an appropriate concentration was proved to enhance the iontophoretic transdermal delivery of SA. A mixture of ethanol and water can dissolve many poorly water-soluble drugs, and therefore it would be able to expand the application of iontophoresis to include many drugs that are poorly soluble in water.
离子导入法的应用局限于高度水溶性的化合物,因为药物通常以水溶液的形式置于药物电极中。在本研究中,将溶解于乙醇 - 水混合物中的水杨酸(SA)装入药物电极,并评估乙醇对SA离子导入透皮给药的影响。与不存在乙醇的情况相比,浓度为10%或30%的乙醇对SA的离子导入透皮给药没有显著影响,但40%或70%的乙醇则显著增加了其离子导入透皮给药效果。离子导入治疗期间体内通过的电流密度随着乙醇浓度的增加而降低。这些结果表明,药物溶液中乙醇的存在使SA离子导入透皮吸收增强,并非由于体内电流密度增加,而可能是由于乙醇对角质层的直接作用。总之,向药物溶液中添加适当浓度的乙醇被证明可增强SA的离子导入透皮给药效果。乙醇和水的混合物可以溶解许多水溶性差的药物,因此它能够扩大离子导入法的应用范围,使其包括许多难溶于水的药物。