Determination and correlation of solubilities of famotidine in water plus co-solvent mixed solvents

被引:18
|
作者
Matsuda, Hiroyuki [1 ]
Matsumoto, Sho [1 ]
Kaguragi, Kenta [1 ]
Kurihara, Kiyofumi [1 ]
Tochigi, Katsumi [1 ]
Tomono, Kazuo [2 ]
机构
[1] Nihon Univ, Dept Mat & Appl Chem, Chiyoda Ku, Tokyo 1018308, Japan
[2] Nihon Univ, Coll Pharm, Chiba 2748555, Japan
关键词
Solubility; Pharmaceutical compounds; Famotidine; Co-solvent; Local composition model; MATHEMATICAL REPRESENTATION; POLYMORPHIC MODIFICATIONS; THERMODYNAMIC PROPERTIES; MIXTURES; CONSTANTS; MODEL; SOLUBILIZATION; LAMOTRIGINE; DISSOLUTION; IMIDAZOLES;
D O I
10.1016/j.fluid.2010.09.029
中图分类号
O414.1 [热力学];
学科分类号
摘要
This study aims to measure the solubilities of poorly water-soluble drugs and to enhance their solubilities by adding co-solvents. The solubilities were measured using high-performance liquid chromatography (HPLC). We selected famotidine, a histamine H-2-receptor antagonist, as the pharmaceutical compound. We measured the solubilities of famotidine at 298.15K in five water/co-solvent mixed solvents, that is, two water + liquid co-solvent mixtures: water + ethanol, and water + polyethylene glycol (PEG) 400; and three water + solid co-solvent mixtures: water + beta-cyclodextrin (beta-CD), water + PEG 1000, and water + lauryl sulfate (SLS). In the two water + liquid co-solvent mixed solvents, the solubilities were measured over the entire co-solvent mole fraction range. In the three water + solid co-solvent mixtures, the solubility was determined up to the co-solvent saturation point. In addition, for the three solid co-solvents, i.e. beta-CD, PEG 1000, and SLS, the solubilization power of each co-solvent-solute system was evaluated using a log-linear model. The experimental solubility data for the two water + liquid co-solvent mixtures were correlated using three local composition models: modified Wilson, NRTL 1, and UNIQUAC. For the three water + solid co-solvent mixtures, a modified Chrastil model was used to correlate the experimental solubility data. (C) 2010 Elsevier B.V. All rights reserved.
引用
收藏
页码:115 / 122
页数:8
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