Cocrystal or Salt Crystallization for Active Pharmaceutical Ingredients By Using Deep Eutectic Solvents

IF 3.2 2区化学 Q2 CHEMISTRY, MULTIDISCIPLINARY

Crystal Growth & Design Pub Date : 2023-08-18 DOI:10.1021/acs.cgd.3c00155

Masataka Ito*, Yuriko Iwata, Hiroyasu Iwasaki, Kyu Hayashi, Taku Nakayama, Hidemasa Hikawa, Isao Azumaya, Hironori Suzuki and Shuji Noguchi,

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引用次数: 0

Abstract

Active pharmaceutical ingredients (APIs) often exhibit physicochemical problems that one can remedy by various methods (e.g., salt formation, grinding, ordered mixtures, and cocrystal or amorphous formation). Crystallizing salts or cocrystals from solutions of an API and a coformer is widely used today. In recent years, green chemistry and sustainable development goals have been an active area of research, and a production method is required for reducing the use of organic solvents and implementing a low environmental load. In this study, deep eutectic solvents (DESs) were used as the mother liquids for crystallization and environmentally friendly solvents. The DESs were made by combining three types of choline salts and a coformer compound of malonic acid. Nine model APIs were then dissolved in each DES and crystals precipitated from the DESs. As a result, five kinds of cocrystals or salts precipitated in 10 conditions, two of which were identified for the first time in this study. Crystallization by using DESs is a potent alternative for discovering novel cocrystals or salts with low environmental impact.

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用深共晶溶剂进行有效药物成分的共晶或盐结晶

活性药物成分(api)通常表现出物理化学问题，人们可以通过各种方法(例如，盐形成，研磨，有序混合物，共晶或无定形形成)来补救。从原料药和共变器的溶液中结晶盐或共晶目前被广泛应用。近年来，绿色化学和可持续发展目标一直是一个活跃的研究领域，需要一种减少有机溶剂使用和实现低环境负荷的生产方法。本研究采用深共晶溶剂(DESs)作为结晶母液和环保溶剂。以三种胆碱盐和丙二酸共构合体为原料，制备了DESs。然后在每个DES中溶解9个模型api，并从DES中析出晶体。结果，在10种条件下共析出5种共晶或盐，其中两种是本研究首次发现的。使用DESs结晶是发现低环境影响的新型共晶或盐的有效替代方法。

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来源期刊

Crystal Growth & Design 化学-材料科学：综合

CiteScore

6.30

自引率

10.50%

发文量

650

审稿时长

1.9 months

期刊介绍： The aim of Crystal Growth & Design is to stimulate crossfertilization of knowledge among scientists and engineers working in the fields of crystal growth, crystal engineering, and the industrial application of crystalline materials. Crystal Growth & Design publishes theoretical and experimental studies of the physical, chemical, and biological phenomena and processes related to the design, growth, and application of crystalline materials. Synergistic approaches originating from different disciplines and technologies and integrating the fields of crystal growth, crystal engineering, intermolecular interactions, and industrial application are encouraged.