Kadir R, Stempler D, Liron Z, Cohen S
Department of Physiology & Pharmacology, Tel Aviv University, Israel.
J Pharm Sci. 1989 Feb;78(2):149-53. doi: 10.1002/jps.2600780216.
A nonionic surfactant, diethyleneglycol lauryl ether (PEG-2-L), increases the flux of either theophylline or adenosine by a factor of 2.2-2.7, when these are delivered from propionic acid solutions into human skin samples, with respect to propionic acid alone. At the same time, the flux of propionic acid from the same vehicles is decreased. Significant expansion of the partial molal volumes vi of both purines occurs following incorporation of PEG-2-L into their propionic acid solution. Hence, the enhancing effect of this surfactant arises mainly from an increase in the excess free energy of these solutes in the donor phase ("push" effect). Paraffin oil increases the flux of either drug from propionic acid by an entirely different mechanism. It enhances the flux of propionic acid into the skin, thus promoting the partitioning of the purine solute in the modified skin barrier ("pull" effect). Indeed, the magnitude of vi of either purine in propionic acid:paraffin oil solution gives no indication of a significant interaction between paraffin oil and the purine solute. Finally, the penetration enhancing effects of PEG-2-L and paraffin oil combined together in the same propionic acid vehicle are additive, resulting in a flux which is approximately the sum total of fluxes obtained separately with PEG-2-L or paraffin oil.
一种非离子表面活性剂，二甘醇月桂醚（PEG - 2 - L），当从丙酸溶液向人体皮肤样本递送茶碱或腺苷时，相较于单独使用丙酸，其通量增加了2.2至2.7倍。与此同时，相同载体中丙酸的通量降低。将PEG - 2 - L加入到嘌呤的丙酸溶液中后，两种嘌呤的偏摩尔体积vi均显著增大。因此，这种表面活性剂的增强作用主要源于供体相中这些溶质的过量自由能增加（“推动”效应）。石蜡油通过完全不同的机制增加了两种药物从丙酸中的通量。它增强了丙酸进入皮肤的通量，从而促进嘌呤溶质在改性皮肤屏障中的分配（“拉动”效应）。实际上，丙酸：石蜡油溶液中任何一种嘌呤的vi大小都没有表明石蜡油与嘌呤溶质之间存在显著相互作用。最后，PEG - 2 - L和石蜡油在同一丙酸载体中共同产生的渗透增强作用是相加的，产生的通量大约是分别使用PEG - 2 - L或石蜡油时获得的通量总和。
