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电解质和非电解质对盐酸丙咪嗪抗抑郁药溶液的浊点及染料增溶作用的研究。

Investigation of the role of electrolytes and non-electrolytes on the cloud point and dye solubilization in antidepressant drug imipramine hydrochloride solutions.

作者信息

Alam Md Sayem

机构信息

Department of Chemistry, Aligarh Muslim University, Aligarh 202002, UP, India.

出版信息

Colloids Surf B Biointerfaces. 2008 Aug 1;65(1):74-9. doi: 10.1016/j.colsurfb.2008.02.021. Epub 2008 Mar 18.

Abstract

Antidepressant drug imipramine hydrochloride (IMP) is amphiphilic which shows surfactant-like behavior in aqueous solutions. We have studied the effect of adding electrolytes and non-electrolytes on the micellar behavior of IMP by making cloud point (CP) and dye solubilization measurements. The CP of a 100mM IMP solution (prepared in 10mM sodium phosphate (SP) buffer) was found to decrease with increasing pH, both in the absence as well as presence of added salts. Increase in pH increased the visible absorbance of Sudan III dye solubilized in the drug micelles, implying micellar growth. Addition of increasing amounts of salts to 100mM IMP solutions (at pH 6.7) caused continuous increase in CP due to micellar growth. On the basis of these studies, the binding-effect orders of counter- and co-ions have been deduced, respectively, as: Br(-)>Cl(-)>F(-) and Li(+)<Na(+)<K(+)<NH(4)(+). The trend of increasing CP with addition of increasing amounts of quaternary salts (tetramethylammonium bromide, TMeAB; tetraethylammonium bromide, TEtAB; tetra-n-propylammonium bromide, TPrAB; tetra-n-butylammonium bromide, TBuAB; tetra-n-pentylammonium bromide, TPeAB) to 100mM IMP solutions (at pH 6.7) was found to be dependent upon the alkyl chain length of the particular salt. Ureas caused CP depression, which was found to be dependent upon the number of methyl groups present in the molecule. Contrary to this, thioureas increased the CP slightly, but the presence of methyl group(s) had effect similar to that of alkylureas. The visible absorbance due to solubilized dye increased/decreased with addition of electrolytes/ureas. The overall behavior has been discussed in terms of electrostatic interactions, micellar growth, and mixed micelle formation.

摘要

抗抑郁药物盐酸丙咪嗪(IMP)具有两亲性,在水溶液中表现出类似表面活性剂的行为。我们通过测定浊点(CP)和染料增溶量,研究了添加电解质和非电解质对IMP胶束行为的影响。发现在不存在和存在添加盐的情况下,100mM IMP溶液(在10mM磷酸钠(SP)缓冲液中制备)的CP均随pH值升高而降低。pH值升高会增加溶解在药物胶束中的苏丹III染料的可见吸光度,这意味着胶束在生长。向100mM IMP溶液(pH 6.7)中添加越来越多的盐,由于胶束生长,CP持续增加。基于这些研究,分别推导出抗衡离子和共离子的结合效应顺序为:Br(-)>Cl(-)>F(-)和Li(+)<Na(+)<K(+)<NH(4)(+)。向100mM IMP溶液(pH 6.7)中添加越来越多的季铵盐(四甲基溴化铵,TMeAB;四乙基溴化铵,TEtAB;四正丙基溴化铵,TPrAB;四正丁基溴化铵,TBuAB;四正戊基溴化铵,TPeAB)时,CP升高的趋势被发现取决于特定盐的烷基链长度。尿素会导致CP降低,这被发现取决于分子中甲基的数量。与此相反,硫脲会使CP略有增加,但甲基的存在与烷基脲的影响相似。添加电解质/尿素时,溶解染料引起的可见吸光度增加/降低。已根据静电相互作用、胶束生长和混合胶束形成对整体行为进行了讨论。

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