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Organic salts as a tool for pharmaceutical ingredient purification: Bibliographic review
Sales orgánicas como herramienta para la purificación de ingredientes farmacéuticos: revisión bibliográfica
Sais orgânicos como ferramenta para purificação de ingredientes farmacêuticos: revisão bibliográfica
DOI:
https://doi.org/10.15446/rcciquifa.v53n1.112981Palabras clave:
Pharmaceutical salts, impurity content, salt formation, salt hydrolysis, purification, solubility change, synthesis (en)Sales farmacéuticas, contenido de impurezas, hidrólisis de sales, purificación, cambio de solubilidad, síntesis (es)
Sais farmacêuticos, teor de impurezas, formação de sal (pt)
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Introduction: Medicines aims to improve the health of the population; for this reason, pharmaceutical ingredients with a high purity level are necessary. In this context, the impurity content is one of the premises in the manufacture of the pharmaceutical ingredients; to comply with this parameter several unit operations can be implemented. In this regard, the pharmaceutical salts can be used as an alternative in the purification process to generate pharmaceutical ingredients with a high purity. Purpose: This review will discuss in first instance, the importance of the impurities in the regulated environment (known, unknown impurities, genotoxic, residual solvents, and elemental impurities). Continuing with the basis of the pharmaceutical salts including functional groups that can form salts, basis of generation and hydrolysis and the main characteristic: the change in the solubility properties due to the formation of the ionic bond. This part also includes general references of previous works and compilations. The next part involves two methodological approaches to purify pharmaceutical ingredients. The first approach is based in salt formation extractions followed by salt hydrolysis. The second tactic is based on salt formation and the solubility properties. Results: Some examples will demonstrate the advantages of these tools. One interesting input is the compilation of several synthetic method to form salts, including examples and alternatives for sensitives cases (water, solid form, ion interchange, etc.). Finally, the salt structure determination will be commented on including the main characterization methodologies.
Introducción: Los medicamentos tienen como objetivo mejorar la salud de la población; por este motivo, son necesarios ingredientes farmacéuticos con un alto nivel de pureza. En este contexto, el contenido de impurezas es una de las premisas en la fabricación de los ingredientes farmacéuticos; para cumplir con este parámetro se pueden implementar varias operaciones unitarias. Objetivo: En este sentido, las sales farmacéuticas se pueden utilizar como una alternativa en el proceso de purificación para generar ingredientes farmacéuticos con una alta pureza. Esta revisión discutirá en primera instancia la importancia de las impurezas en el ambiente regulado (impurezas conocidas, desconocidas, genotóxicas, solventes residuales e impurezas elementales). Continuando con la base de las sales farmacéuticas incluyendo los grupos funcionales que pueden formar sales, base de generación e hidrólisis y la característica principal: el cambio en las propiedades de solubilidad debido a la formación del enlace iónico. Esta parte también incluye referencias generales de trabajos y compilaciones anteriores. La siguiente parte involucra dos enfoques metodológicos para purificar ingredientes farmacéuticos. El primer enfoque se basa en extracciones de formación de sales seguidas de hidrólisis de sales. La segunda táctica se basa en la formación de sales y las propiedades de solubilidad. Resultados: Algunos ejemplos demostrarán las ventajas de estas herramientas. Un aporte interesante es la recopilación de varios métodos sintéticos para formar sales, incluyendo ejemplos y alternativas para casos sensibles (agua, forma sólida, intercambio iónico, etc.). Finalmente, se comentará la determinación de la estructura de la sal incluyendo las principales metodologías de caracterización.
Introdução: Os medicamentos visam melhorar a saúde da população; por esta razão, são necessários ingredientes farmacêuticos com alto nível de pureza. Neste contexto, o teor de impurezas é uma das premissas na fabricação dos insumos farmacêuticos; para cumprir este parâmetro diversas operações unitárias podem ser implementadas. Nesse sentido, os sais farmacêuticos podem ser utilizados como alternativa no processo de purificação para gerar ingredientes farmacêuticos com alta pureza. Objetivo: Esta revisão discutirá, em primeira instância, a importância das impurezas no ambiente regulamentado (impurezas conhecidas, desconhecidas, genotóxicas, solventes residuais e impurezas elementares). Continuando com a base dos sais farmacêuticos incluindo grupos funcionais que podem formar sais, base de geração e hidrólise e a principal característica: a alteração nas propriedades de solubilidade devido à formação da ligação iônica. Esta parte também inclui referências gerais de trabalhos e compilações anteriores. A próxima parte envolve duas abordagens metodológicas para purificar ingredientes farmacêuticos. A primeira abordagem é baseada em extrações de formação de sal seguidas de hidrólise de sal. A segunda tática é baseada na formação de sal e nas propriedades de solubilidade. Alguns exemplos demonstrarão as vantagens destas ferramentas. Resultados: Uma contribuição interessante é a compilação de diversos métodos sintéticos para formação de sais, incluindo exemplos e alternativas para casos sensíveis (água, forma sólida, intercâmbio iônico, etc.). Por fim, será comentada a determinação da estrutura do sal incluindo as principais metodologias de caracterização.
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