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Drug Derivatives and Formulations

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Ibuprofen: Pharmacology, Therapeutics and Side Effects

Abstract

A large number of formulations and derivatives of ibuprofen have been developed for application in the treatment of a wide variety of inflammatory and painful conditions. Among the derivatives, the single enantiomer, S(+)-ibuprofen, or dexibuprofen has been developed and shown to have comparable anti-inflammatory efficacy in rheumatic and musculo-skeletal and various painful conditions usually at about one-third the dose of conventional (or racemic) ibuprofen. The pattern and incidence of adverse reactions with dexibuprofen are comparable to that with conventional ibuprofen.

A variety of alkali salts or amino acid formulations of ibuprofen have been developed whose properties are to enhance absorption of the drug and so increase the speed of onset of pain relief. Other sustained- or delayed-release formulations have been designed to prolong the anti-inflammatory/analgesic activity which is especially useful for treating chronic pain. Likewise, topical formulations have been successfully used for local application to painful joints.

Combinations of ibuprofen with caffeine, codeine and paracetamol have been developed with the objective of increasing pain relief (or the analgesic ceiling) over that of ibuprofen alone. In the case of ibuprofen–paracetamol combinations, the objective is to increase analgesic effects over that of the two drugs.

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Rainsford, K.D. (2012). Drug Derivatives and Formulations. In: Ibuprofen: Pharmacology, Therapeutics and Side Effects. Springer, Basel. https://doi.org/10.1007/978-3-0348-0496-7_5

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