Segurança dos excipientes utilizados pela indústria farmacêutica
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Data
2015
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A parte mais importante de um Medicamento, em termos de volume total da formulação, é constituída pelos seus excipientes que têm as funções importantes de garantir a dose, a estabilidade e biodisponibilidade do princípio activo. As substâncias utilizadas como excipientes devem apresentar as características exigidas pela sua função, mas como acontece com qualquer substância administrada ao homem, devem também corresponder aos requisitos de Segurança exigidos. De facto, no passado, a importância de se avaliar os possíveis efeitos adversos dos excipientes foi subestimada, pois a sua inércia e inocuidade foram tomadas como garantidas.
A toxicidade dos excipientes farmacêuticos não é simples por várias razões, entre as quais, o grande número de substâncias existentes no mercado e a diversidade dos seus perfis químicos, das suas fontes, das suas funções técnicas, e da presença de produtos secundários ou de impurezas, que podem ser as verdadeiras causas de efeitos adversos.
Os excipientes são incluídos no Medicamento para auxiliar a produção deste, a administração ao doente ou a absorção do princípio activo no organismo. Apesar de serem considerados farmacologicamente inertes, os excipientes podem iniciar, propagar ou participar em interacções físicas ou químicas com as moléculas de fármaco, o que pode comprometer a Eficácia do Medicamento. Os excipientes não são perfeitamente puros, pelo que é necessário entender o contexto da sua origem e produção, de modo a identificar as possíveis interacções entre o princípio activo e as suas impurezas. As interacções químicas podem levar à degradação da substância activa, reduzindo assim a quantidade disponível para o efeito terapêutico. Por outro lado, as interacções físicas podem afectar a taxa de dissolução, a uniformidade da dose ou a facilidade de administração.
The most important part of a drug in terms of the total volume of the formulation comprises the excipients, which have the important function of ensuring the dose, stability and bioavailability of the active ingredient. Substances used as excipients must have the characteristics required for its function, but as with any substance administered to humans, must also meet the requirements of safety required. In fact, in the past, the importance of evaluating the possible adverse effects of excipients was underestimated because its inertia and safety have been taken for granted. The toxicity of pharmaceutical excipients is not simple, for several reasons, including the large number of substances on the market and the diversity of their chemical profiles, their sources, their technical functions, and the presence of side products or impurities which may be the real cause of adverse effects. The excipients are included in the medicine to help their production, to allow the drug absorption after its administration in the organism. Although considered as pharmacologically inert, excipients can start or participate in physical or chemical interactions with drug molecules, which can compromise the efficacy of the drug. Excipients are not perfectly pure, it is necessary to understand the context of its origin and production, in order to identify possible interactions between the active substance and impurities. Chemical interactions may lead to degradation of the active substance, thereby reducing the amount available of drug for the therapeutic effect. Furthermore, the physical interaction may affect the dissolution rate, dose uniformity or ease of administration.
The most important part of a drug in terms of the total volume of the formulation comprises the excipients, which have the important function of ensuring the dose, stability and bioavailability of the active ingredient. Substances used as excipients must have the characteristics required for its function, but as with any substance administered to humans, must also meet the requirements of safety required. In fact, in the past, the importance of evaluating the possible adverse effects of excipients was underestimated because its inertia and safety have been taken for granted. The toxicity of pharmaceutical excipients is not simple, for several reasons, including the large number of substances on the market and the diversity of their chemical profiles, their sources, their technical functions, and the presence of side products or impurities which may be the real cause of adverse effects. The excipients are included in the medicine to help their production, to allow the drug absorption after its administration in the organism. Although considered as pharmacologically inert, excipients can start or participate in physical or chemical interactions with drug molecules, which can compromise the efficacy of the drug. Excipients are not perfectly pure, it is necessary to understand the context of its origin and production, in order to identify possible interactions between the active substance and impurities. Chemical interactions may lead to degradation of the active substance, thereby reducing the amount available of drug for the therapeutic effect. Furthermore, the physical interaction may affect the dissolution rate, dose uniformity or ease of administration.
Descrição
Orientação: Ana Catarina Reis
Palavras-chave
MESTRADO INTEGRADO EM CIÊNCIAS FARMACÊUTICAS, FARMACOLOGIA, TOXICIDADE, SEGURANÇA, PHARMACOLOGY, TOXICITY, SECURITY, EXCIPIENTES FARMACÊUTICOS, PHARMACEUTICAL EXCIPIENTS, CIÊNCIAS FARMACÊUTICAS, PHARMACEUTICAL SCIENCES