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Refined diatomite from the Kolubara coal basin (Serbia) was inorganically functionalized through a simple, one-pot, non-time-consuming procedure. Model drug ibuprofen was adsorbed on the functionalized diatomite under optimized conditions providing high drug Loading (similar to 201 mg g(-1)). Physicochemical characterization was performed on the starting and modified diatomite before and after ibuprofen adsorption. Dissolution testing was conducted on comprimates containing the drug adsorbed on the modified diatomite (composite) and those containing a physical mixture of the drug with the modified diatomite. The antihyperalgesic and the antiedematous activity of ibuprofen from both composites and physical mixtures were evaluated in vivo employing an inflammatory pain model in rats. Functionalization and subsequent drug adsorption had no significant effect on the diatomite ordered porous structure. Two forms of ibuprofen most likely coexisted in the adsorbed state - the acidic form and a salt/complex with aluminium. Both comprimate types showed extended ibuprofen release in vitro, but no significant influence on the duration of the ibuprofen effect was observed upon in vivo application of the composite or physical mixture. However, both the composite and the physical mixture were more effective than equivalent doses of ibuprofen in pain suppression in rats. This potentiation of the ibuprofen antihyperalgesic effect may result from the formation of the drug complex with the carrier and can be of clinical relevance.