THAYSEN J H, SCHWARTZ I L
J Exp Med. 1953 Sep;98(3):261-8. doi: 10.1084/jem.98.3.261.
A series of sulfonamide compounds, para-aminohippurate, and inulin were used to study the permeability of the epithelium of human sweat glands. Inulin was not excreted in the sweat. The ratios of the concentrations in sweat to the concentrations in plasma, S/P, of sulfanilamide, sulfapyridine, sulfathiazole, sulfadiazine, and para-aminohippurate were found to be 0.69, 0.58, 0.13, 0.11, and 0.02 respectively, independent of the plasma concentrations and the sweating rates. The fact that the S/P ratios are thus unaffected by the absolute number of molecules transported suggests that these compounds enter into the sweat by simple diffusion and not via a specific secretory mechanism which could become saturated by increasing load. If this is so, the difference in the S/P ratios must be explained by an unequal permeability of the epithelium of the sweat gland to the various compounds and some explanation for these differences in the rate of excretion must exist in terms of physicochemical properties of the compounds. A comparison between the S/P ratios and the pK values of the various sulfonamides indicates that the differences in their rates of excretion in the sweat depend upon the degree of ionization of the various compounds at the physiological pH. Compounds which are mainly non-ionized are excreted with high S/P ratios, whereas ionized compounds appear with low ratios. A quantitative relationship was shown to exist between the S/P ratio for each compound and the percentage of the compound which is non-ionized at pH 7.4.
使用一系列磺胺类化合物、对氨基马尿酸盐和菊粉来研究人体汗腺上皮的通透性。菊粉不会随汗液排出。磺胺、磺胺吡啶、磺胺噻唑、磺胺嘧啶和对氨基马尿酸盐在汗液中的浓度与血浆中的浓度之比(S/P)分别为0.69、0.58、0.13、0.11和0.02,与血浆浓度和出汗速率无关。S/P比值不受转运分子绝对数量影响这一事实表明,这些化合物是通过简单扩散进入汗液的,而非通过可能因负荷增加而饱和的特定分泌机制。如果是这样,S/P比值的差异必须用汗腺上皮对各种化合物的通透性不同来解释,而且这些排泄速率差异的某些解释必须依据化合物的物理化学性质。各种磺胺类化合物的S/P比值与pK值之间的比较表明,它们在汗液中排泄速率的差异取决于各种化合物在生理pH值下的电离程度。主要以非离子形式存在的化合物以高S/P比值排泄,而离子化化合物则以低比值出现。结果表明,每种化合物的S/P比值与在pH 7.4时非离子化的化合物百分比之间存在定量关系。