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Preparation of pharmaceutical co-crystals through sustainable processes using supercritical carbon dioxide: a review

机译：通过使用超临界二氧化碳的可持续工艺制备药物共晶：综述

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摘要

The preparation of pharmaceutical co-crystals using supercritical CO2(scCO(2)) is reviewed. Co-crystallization is an emerging and powerful technique to improve the physicochemical properties of an active pharmaceutical ingredient (API). The solid-state and solution co-crystallization methods usually employed present several disadvantages that may be overcome using the supercritical methods. All the methods employing scCO(2) have low environmental impact and operate at relatively low temperature avoiding API degradation and producing solvent-free pharmaceuticals. The role of the fluid varies from one method to another. In the rapid expansion of supercritical solutions (RESS) the API and the coformer are dissolved in scCO(2). In the co-crystallization with supercritical solvents (CSS), the fluid also acts as a solvent that facilitates molecular interactions in a suspension of the API and coformer powders. However, in the supercritical antisolvent (SAS) and the gas antisolvent (GAS) crystallizations scCO(2) acts as an antisolvent that induces precipitation of the API and the coformer previously dissolved in an organic solvent. In the atomization and antisolvent (AAS) technique and supercritical fluid enhanced atomization (SEA) the fluid may act either as a spray enhancer or an antisolvent depending on the process conditions. Each method is described and its application, advantages and disadvantages are discussed. Future perspectives and areas to be investigated are outlined.
机译：综述使用超临界CO 2（SCCO（2））的药物共晶的制备。共结晶是一种改善活性药物成分（API）的物理化学性质的新兴和强大的技术。固态和溶液共结晶方法通常采用若干可能使用超临界方法克服的若干缺点。采用SCCO（2）的所有方法都具有低的环境影响，并且在相对低的温度下运行避免API降解和产生无溶剂药物。流体的作用从一种方法变化到另一个方法。在超临界溶液（RESS）的快速膨胀中，API和COFORMER溶解在SCCO（2）中。在具有超临界溶剂（CSS）的共结晶中，流体也用作促进API和CoFormer粉末悬浮液中的分子相互作用的溶剂。然而，在超临界抗溶剂（SAS）和气体抗溶剂（气体）结晶SCCO（2）中的用作诱导API沉淀和预先溶解在有机溶剂中的共甲酸的抗溶剂。在雾化和抗溶剂（AAS）技术和超临界流体增强雾化（海）的情况下，流体可以根据过程条件作为喷雾增强剂或防溶剂。描述了每个方法，并讨论其应用，优点和缺点。概述了未来的观点和要调查的区域。

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  • 来源
    《RSC Advances》 |2016年第75期|共17页
  • 作者

    Pando Concepcion; Cabanas Albertina; Cuadra Isaac A.;

  • 作者单位

    Univ Complutense Fac Quim C Dpto Quim Fis 1 E-28040 Madrid Spain;

    Univ Complutense Fac Quim C Dpto Quim Fis 1 E-28040 Madrid Spain;

    Univ Complutense Fac Quim C Dpto Quim Fis 1 E-28040 Madrid Spain;

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  • 正文语种 eng
  • 中图分类 化学;
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