Relationship between nasal absorption and physicochemical properties of quaternary ammonium compounds.
Relationship between nasal absorption and physicochemical properties of quaternary ammonium compounds.
复制标题
季铵化合物的鼻吸收与理化性质的关系。
DOI：
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发表时间：
1991
影响因子：
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通讯作者：
S. Yamada
中科院分区：
文献类型：
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作者：
R. Kimura;M. Miwa;Y. Kato;M. Sato;S. Yamada
本文研究了一系列与四乙基氯化铵相关的脂肪族季铵盐化合物在大鼠体内的鼻腔吸收及其与其理化性质(相对分子质量和分配系数)的关系。所考察的10种季铵盐化合物均被大鼠鼻粘膜吸收。相对分子质量最低的乙基三甲基碘化铵和四乙基氯化铵的鼻腔吸收速率最高，而相对分子质量较高的四丁基氯化铵和四正丙基溴化铵的鼻腔吸收速率较低。因此，季铵化合物在大鼠体内的鼻腔吸收速率有随其分子量增加而降低的趋势。物理化学研究表明，十种季铵化合物的分子量与其分配系数之间存在线性关系，从而表明亲油性随分子量的增加而增加。此外，所研究的季铵化合物的鼻腔吸收程度与其相对分子质量或分配系数之间有很好的相关性。这些数据表明，季铵化合物在鼻黏膜中的膜转运与其亲脂性之间存在着相互作用的关系。总之，季铵化合物似乎主要通过充满水的通道或毛孔从大鼠的鼻黏膜吸收，而不是通过脂膜吸收。
The present study was undertaken to investigate the in situ nasal absorption of a series of tetraethylammonium chloride-related aliphatic quaternary ammonium compounds in rats and its relationship with their physicochemical properties (molecular weight and partition coefficient). All of the ten quaternary ammonium compounds examined were found to be absorbed through the nasal mucosa of rats. The nasal absorption rates of ethyltrimethyl-ammonium iodide and tetraethylammonium chloride, with the lowest molecular weight, were the highest, and those of tetra-n-butylammonium chloride and tetra-n-propylammonium bromide, with high molecular weight, were much lower. Thus, there was a tendency that the nasal absorption rates of quaternary ammonium compounds in rats decreased with an increase in their molecular weight. A physicochemical study has shown that there was a linear relationship between the molecular weight of the ten quaternary ammonium compounds and their partition coefficient, thereby suggesting an increase in lipophilicity with the molecular weight. In addition, there was a good correlation between the extent of the nasal absorption of the quaternary ammonium compounds studied and their molecular weight or partition coefficient. These data suggest that there is a reciprocal relationship between the membrane transport of quaternary ammonium compounds in the nasal mucosa and their lipophilic character. In conclusion, it seems likely that quaternary ammonium compounds are predominantly absorbed from the nasal mucosa of the rat through waterfilled channels or pores rather than through the lipid membrane.