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Excipients are often described as inert or inactive, in the context of formulating drugs. But this is only partially true, as while they don’t interact with proteins, enzymes, receptors, nucleic acid or bio- membranes in the same way as an active pharmaceutical ingredient, they can have physical and chemical interactions with an API itself. This can be a positive or a negative, depending on the desired use for a drug. Monica Karpinski speaks to Robert Luxenhofer, professor of soft matter chemistry at the University of Helsinki; Fernando Muzzio, distinguished professor of chemical and biochemical engineering at Rutgers University; and Amal Eli Elkordy, professor of pharmaceutics at the University of Sunderland, to find out why physicochemical interactions are important in drug development.
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n the Australian city of Brisbane, 55 years ago, there was a widespread overdose of anticonvulsant medication among people with
epilepsy. It turned out that those affected were all taking the same brand of the drug phenytoin. Just a few months before the outbreak, the main excipient within its formulation, calcium sulphate dihydrate, had been replaced with lactose. In 87% of patients, the blood phenytoin levels were above the therapeutic range, and conclusions were drawn
that the lactose changed the solubility of the drug so that more – too much in fact – of the active ingredient was absorbed by the blood. Luckily, a reduction of phenytoin dosage relieved the intoxication in all patients, but the event serves as a good example of the importance of formulating using the right excipients.
Excipients are substances added to a drug alongside the active pharmaceutical ingredient (API) that establish the functional properties it
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