The safety of pharmaceutical excipients

Abstract

The most important part of a medicine as far as its weight is concerned, is constituted by its excipients, which have the important functions of guaranteeing the dosage, stability and bioavailability of the active principle. The components employed as excipients must present the characteristics required by their technological function but, as with any substance administered to man, they must also correspond to suitable safety requirements. In fact, in the past the importance of evaluating the possible adverse effects of excipients was underestimated, because their inertia and innocuity were taken for granted. The safety profile of these substances is more deeply researched as regards the toxicological aspect only if they are also employed in the food industry (anti-oxidants, sweeteners, colouring agents, etc.). Indeed, in this case, the International Toxicological Committees (among which the Joint Expert Committee on Food Additives, a mixed committee of the WHO/FAO) demand thorough studies in laboratory animals, with the intent of protecting the consumer's safety. Tackling the question of the toxicity of excipients thoroughly is not a simple matter for several reasons: the large number of substances on the market and the diversity of their chemical profiles, their sources, their technological functions, and the presence of secondary products and/or contaminants that may be the true causes of adverse effects. In this article we shall review the principal classes of excipients and their respective side effects. Then we shall proceed to their toxicological evaluation, giving examples of: (a) intrinsic toxicity, or adverse effects that may be encountered in the whole population; and (b) specific toxicity, which manifests only in people who are carriers of a transmissible disease or who are genetically predisposed, such as people with allergies and intolerances.

Physicochemical properties and lubricant potentials of Blighia sapida Sapindaceaeae seed oil in solid dosage formulations

“…Excipients are essential for manufacturing and administration of the dosage form and also help in stability and bioavailability of the active drug [3]. Exploring local sources of low-cost substitutes could lead to the discovery of excipients with outstanding properties [4].…”

Síntese e caracterização de beads acrílicos preparados por polimerização em suspensão visando aplicação como excipiente farmacêutico para compressão direta

“…1 Em decorrência dos avanços no delineamento de novos sistemas de liberação de fármacos (SLFs), inclusive de comprimidos, faz-se necessário que sejam desenvolvidos novos excipientes, idealizados para exercerem funções específicas nas formulações, tais como, melhorar a biodisponibilidade do fármaco e otimizar as características de manufaturabilidade dos comprimidos bem como de outras formas farmacêuticas. [2][3][4][5][6][7] Portanto, é cada vez maior na literatura o número de artigos que relatam pesquisas voltadas para o desenvolvimento de novos excipientes farmacêuticos. [8][9][10][11][12][13][14][15][16][17] A maioria dos comprimidos de liberação prolongada disponíveis comercialmente contém hidroxipropilmetilcelulose (HPMC) como agente formador de matriz.…”

“…Algumas das análises preconizadas para a avaliação destas propriedades são denominadas micromeríticas, e referem-se à ciência que investiga características como forma das partículas, diâmetro, distribuição de tamanho, densidade, área superficial, carga superficial, entre outras. 2,3 Neste sentido, o objetivo principal do presente trabalho foi desenvolver um excipiente acrílico, na forma sólida, a ser utilizado na preparação de comprimidos matriciais inertes por compressão direta. Os monômeros selecionados para o preparo dos copolímeros foram o acrilato de etila (EA), o metacrilato de metila (MMA) e o metacrilato de butila (BMA).…”

Untitled

“…Rationality in Concept of Excipient: Excipient, the term comprises with verb "excipere" which means to receive, to gather or to take out 8 . This refers to one of the properties of an excipient, which ensure the medicinal product has the weight, consistency and volume necessary for the correct administration of the active principle.…”