Thysman S, Préat V, Roland M
Laboratoire de Pharmacie Galénique, Ecole de Pharmacie, Université Catholique de Louvain, Brussels, Belgium.
J Pharm Sci. 1992 Jul;81(7):670-5. doi: 10.1002/jps.2600810717.
The effect of different factors on the iontophoretic transport of metoprolol was analyzed. In vitro experiments were first performed in a diffusion cell with a cellophane membrane. Comparison of different pH, buffers, and ionic strengths in the donor compartment showed that higher iontophoretic transport was obtained with phthalate buffer (0.01 M) at pH 3. When the current density increased, the flux of metoprolol also increased. A decrease in drug concentration or an increase in viscosity slowed down the iontophoretic transport of metoprolol. The fluxes of metoprolol through hairless rat skin were strongly enhanced compared with passive diffusion. Direct current seemed to be more efficient than pulse current. When the on:off ratio of the pulse current was reduced, the flux also decreased.
分析了不同因素对美托洛尔离子导入转运的影响。首先在具有玻璃纸膜的扩散池中进行体外实验。供体室中不同pH值、缓冲液和离子强度的比较表明,在pH 3时使用邻苯二甲酸盐缓冲液(0.01 M)可获得更高的离子导入转运。当电流密度增加时,美托洛尔的通量也增加。药物浓度降低或粘度增加会减缓美托洛尔的离子导入转运。与被动扩散相比,美托洛尔通过无毛大鼠皮肤的通量显著增强。直流电似乎比脉冲电流更有效。当脉冲电流的通断比降低时,通量也会降低。