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药用辅料对两亲性药物浊点的影响。

Effects of pharmaceutical excipients on cloud points of amphiphilic drugs.

机构信息

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

出版信息

J Colloid Interface Sci. 2011 Sep 1;361(1):42-8. doi: 10.1016/j.jcis.2011.05.037. Epub 2011 May 26.

DOI:10.1016/j.jcis.2011.05.037
PMID:21679963
Abstract

The clouding behavior, i.e., formation of phase separation at elevated temperature (the temperature being known as cloud point (CP)), of three amphiphilic drugs, amitriptyline (AMT), clomipramine (CLP) and imipramine (IMP) hydrochlorides in the presence of various additives, like cationic surfactants (conventional and gemini), nonionic surfactants, bile salts, anionic hydrotropes, sodium salts of fatty acids and cyclodextrin has been investigated. These additives are generally used as drug delivery systems. The drugs used are tricyclic antidepressants. All the surfactants increase the CP of mixed micelles formed by cationic (conventional and gemini) and nonionic surfactants. Hydrotropes, bile salts and fatty acid salts, when added in low concentrations, increase the CP, whereas at high concentrations, they decrease it. β-Cyclodextrin behaves as simple sugar and decreases the CP of the drug solutions.

摘要

三种两亲性药物(阿米替林、氯米帕明和盐酸丙咪嗪)在不同添加剂(如阳离子表面活性剂(常规和双子)、非离子表面活性剂、胆汁盐、阴离子增溶剂、脂肪酸钠盐和环糊精)存在下的浊点行为(即在高温下形成相分离的行为,该温度称为浊点(CP))已被研究。这些添加剂通常用作药物传递系统。所用的药物是三环类抗抑郁药。所有表面活性剂都增加了由阳离子(常规和双子)和非离子表面活性剂形成的混合胶束的 CP。增溶剂、胆汁盐和脂肪酸盐在低浓度下增加 CP,而在高浓度下则降低 CP。β-环糊精的行为类似于单糖,降低了药物溶液的 CP。

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