Ketoprofen Comparative Pharmacokinetics Analysis in Humans and Animals: A Review

INTRODUCTION. Ketoprofen is a non-steroidal anti-inflammatory drug (NSAID) with pronounced analgesic, anti-inflammatory and antipyretic effect. Ketoprofen pharmacokinetics is comparatively well described in various in vivo models. Since it is potentially possible to create new dosage forms of ketoprofen, with pharmacokinetics studies contributing to high-quality pharmaceutical development, a comparative assessment is relevant for the data on animals and humans.

AIM. This study aimed to identify animal species relevant for preclinical studies of different ketoprofen dosage forms by summarising bioanalytical methods used to assess pharmacokinetics and by comparing different test systems.

DISCUSSION. Reversed-phase high-performance liquid chromatography with ultraviolet/mass spectrometric detection and acetonitrile or methanol-based eluents in various buffer solutions is the most ubiquitous method for ketoprofen analysis in biomaterials. Ketoprofen pharmacokinetics was studied in humans and animals of several phylogenetic species using various dosage forms (injectable solutions, tablets, paste forms, etc.) and the relevant administration (intravenous, intramuscular, oral, transdermal). High drug bioavailability was noted for different routes. Maximum concentration (C_max) range at similar doses and similar time parameters (time to maximum concentration, T_max, half-life, T_1/2 and mean residence time, MRT) for the three main administration routes (oral, intravenous and intramuscular) was comparable in humans and rats, cats, and dogs; thus these test systems were suggested for pharmacokinetics studies of ketoprofen preparations.

CONCLUSIONS. The analysis suggested that rats and larger animals (cats, dogs) can serve as test systems in ketoprofen pharmacokinetics studies, at least for oral, intravenous, and intramuscular administration. Using ketoprofen as an example, the study showed feasibility of integrating heterogeneous pharmacokinetic data, as well as comparison challenges due to variable test systems, study objects, dosages, and administration routes.

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