文章基本信息

标题：Enthalpy–Entropy Compensation in the Structure-Dependent Effect of Nonsteroidal Anti-inflammatory Drugs on the Aqueous Solubility of Diltiazem
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作者：Takatoshi Kinoshita ; Chihiro Tsunoda ; Satoru Goto 等
期刊名称：Chemical and Pharmaceutical Bulletin
印刷版ISSN：0009-2363
电子版ISSN：1347-5223
出版年度：2022
卷号：70
期号：2
页码：120-129
DOI：10.1248/cpb.c21-00834
语种：English
出版社：The Pharmaceutical Society of Japan
摘要：Certain combinations of acidic and basic drugs can cause significant changes in physicochemical properties through the formation of ionic liquids, eutectic mixtures, or deep eutectic solvents. In particular, combining indomethacin and lidocaine is known to result in apparent increases in both the partition coefficients (hydrophobicity) and aqueous solubilities (hydrophilicity). The physicochemical interactions between drugs change the water solubility of the drugs and affect the bio-availability of active pharmaceutical ingredients. Therefore, we need to clarify the mechanism of changes of water solubility of drugs through the physicochemical interactions. In the present study, we identified a thermodynamic factor that regulates the dissolution of a basic drug, in the presence of various acidic nonsteroidal anti-inflammatory drugs. The results demonstrated that enthalpy–entropy compensation plays a key role in the dissolution of drug mixtures and that relevant thermodynamic conditions should be considered.
关键词：solubility;intermolecular interaction;diltiazem;non-steroid anti-inflammatory;entropy;van’t Hoff plot