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硝苯地平的水增溶作用。

Hydrotropic solubilization of nifedipine.

作者信息

Jain N K, Patel V V, Taneja L N

机构信息

Pharmacy Department, Faculty of Technology and Engineering, M.S. University of Baroda, India.

出版信息

Pharmazie. 1988 Mar;43(3):194-6.

PMID:3380863
Abstract

Nifedipine (1), a drug practically insoluble in water, has been solubilized employing sodium benzoate (2) and sodium salicylate (3) as hydrotropes. In 30% w/v 2 solution the solubility of 1 increased 85 and 76 fold at 25 +/- 1 degree C and at 37 +/- 1 degree C respectively. The corresponding increase in solubility of 1 in 30% w/v 3 solution was 135 and 107 fold respectively. To study the mechanism of hydrotropic solubilization of 1, the solution properties of 2 and 3 over a concentration range of 1 to 30% w/v were undertaken. The probable mechanism involves a complexation type of interaction at a low concentration of hydrotrope, aggregation of the hydrotropic molecules and inclusion of 1 in these aggregates at high concentration; and structural changes in water caused by hydrotropes.

摘要

硝苯地平(1)是一种几乎不溶于水的药物,已使用苯甲酸钠(2)和水杨酸钠(3)作为助溶剂进行增溶。在30%(w/v)的2溶液中,1的溶解度在25±1℃和37±1℃时分别增加了85倍和76倍。1在30%(w/v)的3溶液中的溶解度相应增加分别为135倍和107倍。为了研究1的助溶增溶机制,对2和3在1%至30%(w/v)浓度范围内的溶液性质进行了研究。可能的机制包括在低浓度助溶剂下的络合型相互作用、助溶分子的聚集以及在高浓度下1被包含在这些聚集体中;以及助溶剂引起的水的结构变化。

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