Attwood D, Udeala O K
J Pharm Sci. 1976 Jul;65(7):1053-7. doi: 10.1002/jps.2600650724.
The effects of electrolytes on the self-association of the antihistaminic drugs, tripelennamine hydrochloride, thenyldiamine hydrochloride, pyrilamine maleate, pheniramine maleate, chlorpheniramine maleate, and brompheniramine maleate, in aqueous solution were examined by light-scattering from tripelennamine bydrochloride and thenyldiamine hydrochloride in 0.154 mole of sodium chloride/kg and 0.150 mole of sodium maleate/kg indicated a micellar pattern of aggregation. Higher aggregation numbers and lower CMC's were determined in the presence of the maleate ion. No significant discontinuity in the concentration dependence of the light scattering of the remaining compounds in either of the two electrolytes was evident, and the aggregation of these compounds was treated using a stepwise association model. Values of the association constants and the limiting number of associating species were, in general, increased by the addition of electrolyte in the order water less than sodium chloride less than sodium maleate. An apparently nonmicellar pattern of aggregation could be induced by chemically changing the counterion from chloride to maleate.
通过对盐酸曲吡那敏和盐酸噻吩二胺在0.154摩尔氯化钠/千克和0.150摩尔马来酸钠/千克溶液中的光散射研究，考察了电解质对水溶液中抗组胺药物盐酸曲吡那敏、盐酸噻吩二胺、马来酸氯苯那敏、马来酸苯那敏、马来酸氯苯那敏和马来酸溴苯那敏自缔合的影响，结果表明存在胶束聚集模式。在马来酸根离子存在下，测定了更高的聚集数和更低的临界胶束浓度。在两种电解质中，其余化合物的光散射浓度依赖性均无明显不连续性，这些化合物的聚集采用逐步缔合模型处理。一般来说，通过添加电解质，缔合常数和缔合物种的极限数的值按水＜氯化钠＜马来酸钠的顺序增加。通过将抗衡离子从氯离子化学改变为马来酸根离子，可以诱导出明显的非胶束聚集模式。
