Abstract
A procedure was developed for radioiodination of ibuprofen with 125I via an electrophilic substitution reaction. With the aim to optimize the labeling conditions and obtain a high radiochemical yield of 125I-ibuprofen (125I-Ibup), the effect exerted on the process by the reaction conditions (ibuprofen concentration, pH, reaction time, temperature, oxidizing agent) was studied. With 3.7 MBq of Na125I, 100 μg of ibuprofen as substrate and 100 μg of iodogen as oxidizing agent, with the reaction performed in ethanol at 60°C for 10 min, the maximum radiochemical yield of 125I-Ibup (78%) was obtained. The labeled compound was separated and purified to remove inactive ibuprofen by HPLC. The biological distribution in normal and inflamed mice shows that radioiodinated ibuprofen is suitable for imaging of inflammation only induced with turpentine oil.
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