Siegel I A
J Invest Dermatol. 1981 Feb;76(2):137-40. doi: 10.1111/1523-1747.ep12525477.
The in vitro permeability of oral mucosa from New Zealand rabbits to 17 nonelectrolytes was studied using radioactive tracer techniques. Calculated permeability coefficients were independent of solute concentration and were similar when measured from outer to inner surface or inner to outer surface. Generally, an increase in chain length and increased lipid solubility within a series of alcohols or diols resulted in increased permeability. However, the first member of each series displayed anomalous behavior in that it penetrated more rapidly than the second member of the series. Addition of one or more hydroxyl groups to a compound brings about a decrease in permeability. The addition of a second or third hydroxyl group has less of an effect in decreasing permeability if it is adjacent to an existing hydroxyl as compared to when it is further separated. Addition of a hydroxyl group to a compound decreases permeability to a greater extent than addition of a ketone. Also, replacement of a hydroxyl group with an amide results in decreased permeability. These results point out the importance of lipid solubility and ability to form hydrogen bonds to permeability.
采用放射性示踪技术研究了新西兰兔口腔黏膜对17种非电解质的体外渗透性。计算得到的渗透系数与溶质浓度无关，并且从外表面到内表面或从内表面到外表面测量时结果相似。一般来说，在一系列醇或二醇中，链长增加和脂溶性增加会导致渗透性增加。然而，每个系列的第一个成员表现出异常行为，即它比该系列的第二个成员渗透得更快。向化合物中添加一个或多个羟基会导致渗透性降低。如果第二个或第三个羟基与现有的羟基相邻，与它被进一步隔开时相比，其降低渗透性的效果较小。向化合物中添加一个羟基比添加一个酮更能降低渗透性。此外，用酰胺取代羟基会导致渗透性降低。这些结果指出了脂溶性和形成氢键的能力对渗透性的重要性。
