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用于通过柱色谱法纯化活性药物成分的更安全溶剂。

Safer Solvents for Active Pharmaceutical Ingredient Purification Using Column Chromatography.

作者信息

Ayafor Christian, Burton Toren, George Nathaniel, Morose Gregory, Wong Hsi-Wu

机构信息

Energy Engineering Program, University of Massachusetts Lowell, Lowell, Massachusetts 01854, United States.

Department of Chemical Engineering, University of Massachusetts Lowell, Lowell, Massachusetts 01854, United States.

出版信息

ACS Environ Au. 2024 Jun 24;4(5):236-247. doi: 10.1021/acsenvironau.4c00015. eCollection 2024 Sep 18.

DOI:10.1021/acsenvironau.4c00015
PMID:39309977
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11413887/
Abstract

Column chromatography is a technique widely used for the purification of active pharmaceutical ingredients (APIs). One of the common solvent systems used by this technique is blends of dichloromethane (DCM) and methanol (MeOH), thereby exposing workers to health and safety risks and making the pharmaceutical sector one of the major contributors to chlorinated solvent waste. In this work, API separation and purification using several alternative safer solvent blends in column chromatography were evaluated and compared to DCM/MeOH. Ibuprofen and acetaminophen were used as model APIs, and caffeine was used as a model additive. Overall, some of the safer solvent blends tested provided better performance, with higher API recovery and purity compared to DCM/MeOH, in addition to potential health, safety, and environmental benefits. Specifically, blends of heptane/ethyl acetate and heptane/methyl acetate showed the most promise. Our work demonstrates the potential of these safer solvent blends as possible replacements for DCM/MeOH in API purification, thereby addressing a critical safety concern in the pharmaceutical industry.

摘要

柱色谱法是一种广泛用于纯化活性药物成分（API）的技术。该技术常用的溶剂系统之一是二氯甲烷（DCM）和甲醇（MeOH）的混合物，这使工人面临健康和安全风险，并使制药行业成为氯化溶剂废物的主要贡献者之一。在这项工作中，评估了在柱色谱中使用几种更安全的替代溶剂混合物进行API分离和纯化，并与DCM/MeOH进行了比较。布洛芬和对乙酰氨基酚用作模型API，咖啡因用作模型添加剂。总体而言，一些测试的更安全的溶剂混合物表现出更好的性能，与DCM/MeOH相比，API回收率和纯度更高，此外还具有潜在的健康、安全和环境效益。具体而言，庚烷/乙酸乙酯和庚烷/乙酸甲酯的混合物显示出最大的潜力。我们的工作证明了这些更安全的溶剂混合物在API纯化中作为DCM/MeOH的可能替代品的潜力，从而解决了制药行业的一个关键安全问题。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bc03/11413887/2c0e8ab42a28/vg4c00015_0008.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bc03/11413887/05ec103852ec/vg4c00015_0002.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bc03/11413887/169f41668855/vg4c00015_0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bc03/11413887/61fae7bd07e4/vg4c00015_0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bc03/11413887/ccc38386a2e8/vg4c00015_0007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bc03/11413887/2c0e8ab42a28/vg4c00015_0008.jpg

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