Garren K W, Repta A J
Department of Pharmaceutical Chemistry, University of Kansas, Lawrence 66045.
J Pharm Sci. 1989 Feb;78(2):160-4. doi: 10.1002/jps.2600780218.
The in vitro diffusion of a series of substituted acetanilides across the hamster cheek pouch was studied. The keratinized epithelial layer of the cheek pouch appeared to provide the major barrier to diffusion of these compounds. Linear relationships were found for plots of log epithelial permeability (Pe) versus the log of the octanol-buffer partition coefficient (PCoct; r = 0.712), and log Pe versus the log of the isooctane-buffer partition coefficient (PCiso; r = 0.869). Comparison of the in vitro data with in vivo data obtained in humans using the buccal absorption test showed good correlation (r = 0.878) between Pe and percent buccal absorption in 5 min. These results suggest that diffusion across the hamster cheek pouch may have some utility in the prediction of human buccal absorption.
研究了一系列取代乙酰苯胺在仓鼠颊囊中的体外扩散情况。颊囊的角质化上皮层似乎是这些化合物扩散的主要屏障。对于对数上皮渗透率（Pe）与辛醇-缓冲液分配系数（PCoct；r = 0.712）的对数作图，以及对数Pe与异辛烷-缓冲液分配系数（PCiso；r = 0.869）的对数作图，均发现了线性关系。将体外数据与使用颊部吸收试验在人体中获得的体内数据进行比较，结果显示在5分钟内Pe与颊部吸收百分比之间具有良好的相关性（r = 0.878）。这些结果表明，仓鼠颊囊中的扩散情况在预测人体颊部吸收方面可能具有一定作用。
