Gardiner T H, Goodman F R
Am J Physiol. 1977 Mar;232(3):C132-7. doi: 10.1152/ajpcell.1977.232.3.C132.
The pulmonary absorption and uptake of (35S)phenol red ((35S)PR was measured in anesthetized rats with alpha-naphthylthiourea- (ANTU) induced lung edema. When (35S)PR solution was injected through a tracheal cannula in control animals and the percentage of the tracheal cannula in control animals and the percentage of the dose unabsorbed plotted semilogarithmically against time, an apparent first-order absorption rate was obtained. In contrast, in rats with ANTU-induced edema, the absorption time curve showed at least two different first-order components. Increasing the concentration of (35S)PR from 0.01 to 3 mM resulted in a decrease in the percentage absorption of the compound in controls compared with a relatively constant percentage absorption in edematous lungs. (35S)PR uptake by lung slices from ANTU-treated rats was decreased in the presence of IAA and a N2 atmosphere, and the dye accumulated at a faster rate and to a greater extent than in controls. The results suggest that although energy-dependent drug transport mechanisms remain intact, the porosity of the absorbing membranes and the extent of drug binding in the lung are increased markedly in the presence of edema.
在使用α-萘基硫脲(ANTU)诱导肺水肿的麻醉大鼠中,测定了(35S)酚红((35S)PR)的肺吸收和摄取情况。当在对照动物中通过气管插管注射(35S)PR溶液,并将对照动物中气管插管的百分比以及未吸收剂量的百分比对时间进行半对数绘图时,得到了明显的一级吸收速率。相比之下,在ANTU诱导水肿的大鼠中,吸收时间曲线显示至少有两个不同的一级成分。将(35S)PR的浓度从0.01 mM增加到3 mM,导致对照中该化合物的吸收百分比降低,而在水肿肺中吸收百分比相对恒定。在吲哚乙酸(IAA)存在和氮气环境下,ANTU处理大鼠的肺切片对(35S)PR的摄取减少,并且染料积累的速率比对照更快、程度更大。结果表明,尽管能量依赖的药物转运机制保持完整,但在存在水肿的情况下,吸收膜的孔隙率和肺中药物结合的程度显著增加。