Vizserálek Gábor, Berkó Szilvia, Tóth Gergő, Balogh Réka, Budai-Szűcs Mária, Csányi Erzsébet, Sinkó Bálint, Takács-Novák Krisztina
Department of Pharmaceutical Chemistry, Semmelweis University, 9 Hőgyes Endre Street, H-1092 Budapest, Hungary.
Department of Pharmaceutical Technology, University of Szeged, 6 Eötvös Street, H-6720 Szeged, Hungary.
Eur J Pharm Sci. 2015 Aug 30;76:165-72. doi: 10.1016/j.ejps.2015.05.004. Epub 2015 May 7.
Using the skin as absorption site presents unique advantages that have facilitated the progression of transdermal drug delivery in the past decades. Efforts in drug research have been devoted to find a quick and reproducible model for predicting the skin permeation of molecules. The Parallel Artificial Membrane Permeability Assay (PAMPA) has been extended for prediction of transdermal permeation by developing a model with completely artificial membrane, which can mimic the permeation through the stratum corneum. The present study aims to extend the Skin PAMPA method for testing transdermal and local therapeutic patches. The original method was modified and seven commercially available transdermal and local therapeutic patches with four different active pharmaceutical ingredients (nicotine, fentanyl, rivastigmine and ketoprofen) were studied. Data were compared to the declared delivery rates that are indicated by the manufacturers. Ex vivo permeation study was also performed in order to compare the permeated amount of the released drugs obtained by the two methods. The flux across the artificial membrane as well as the human skin (ex vivo) has been calculated and compared to the in vivo flux deduced from the labelled delivery rate and the active area of the patches. The results suggest that Skin PAMPA system can serve as a useful tool for evaluation and classification of the transdermal patches.
将皮肤作为吸收部位具有独特的优势，在过去几十年中推动了透皮给药的发展。药物研究工作致力于寻找一种快速且可重复的模型来预测分子的皮肤渗透情况。平行人工膜通透性测定法（PAMPA）已通过开发一种具有完全人工膜的模型得到扩展，用于预测透皮渗透，该模型可模拟通过角质层的渗透。本研究旨在扩展皮肤PAMPA方法以测试透皮和局部治疗贴剂。对原始方法进行了改进，并研究了七种含有四种不同活性药物成分（尼古丁、芬太尼、卡巴拉汀和酮洛芬）的市售透皮和局部治疗贴剂。将数据与制造商标明的释放速率进行比较。还进行了体外渗透研究，以比较两种方法获得的释放药物的渗透量。计算了通过人工膜以及人体皮肤（体外）的通量，并与根据贴剂的标记释放速率和有效面积推导得出的体内通量进行比较。结果表明，皮肤PAMPA系统可作为评估和分类透皮贴剂的有用工具。
