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表面活性阳离子药物的光子相关光谱法

Photon correlation spectroscopy of surface active cationic drugs.

作者信息

Atherton A D, Barry B W

出版信息

J Pharm Pharmacol. 1985 Dec;37(12):854-62. doi: 10.1111/j.2042-7158.1985.tb04989.x.

Abstract

Photon correlation spectroscopy (PCS) has been used to examine the aggregation in aqueous NaCl solution of a series of antidepressant and antihistamine drugs (hydrochlorides of imipramine, clomipramine, amitriptyline, butriptyline, protriptyline, doxepin, dothiepin, iprindole, diphenhydramine, bromodiphenhydramine, orphenadrine) propranolol hydrochloride and propantheline bromide. Critical micelle concentrations were measured by surface tension and PCS. Micellar sizes were investigated as functions of drug structure and drug and NaCl concentration. Generally, antidepressants formed the largest micelles. We propose that the antidepressants aggregate in a similar fashion to the phenothiazines by stacking with size increasing by addition of single monomers to stacks and by addition of more stacks to the aggregate.

摘要

光子相关光谱法(PCS)已被用于研究一系列抗抑郁药和抗组胺药(丙咪嗪、氯米帕明、阿米替林、布替林、普罗替林、多塞平、度硫平、茚满二酮、苯海拉明、溴苯海拉明、奥芬那君的盐酸盐)、盐酸普萘洛尔和溴丙胺太林在NaCl水溶液中的聚集情况。通过表面张力和PCS测量临界胶束浓度。研究了胶束大小与药物结构、药物和NaCl浓度的关系。一般来说,抗抑郁药形成的胶束最大。我们认为,抗抑郁药通过堆叠以类似于吩噻嗪的方式聚集,其大小通过向堆叠中添加单个单体以及向聚集体中添加更多堆叠而增加。

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