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Comparative study between chloramine-T and iodogen to prepare radioiodinated etodolac for inflammation imaging
Faculty
Science
Year:
2011
Type of Publication:
Article
Pages:
9-15
Authors:
Seddik, U, Hussien, H, Goud, A. A, Amin, A. M, EL-Sheikh, R
DOI:
10.1007/s10967-010-0967-9
Journal:
JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY SPRINGER
Volume:
288
Research Area:
Chemistry; Nuclear Science \& Technology
ISSN
ISI:000288220400002
Keywords :
Non steroid anti-inflammatory drugs, Electrophilic substitution, Inflammation imaging
Abstract:
This study describes a fast and efficient method for radiolabeling of etodolac with iodine-125 {[}(125)I], where both chloramine-T and iodogen were used as oxidizing agents. The labeling reaction was carried out via electrophilic substitution of hydrogen atom with the iodonium cation I(+). The labeling yield was found to be influenced by different factors such as drug concentration, pH of the reaction mixtures, different oxidizing agents, reaction time, temperature and different organic media. The radiochemical yield (RCY) was determined by TLC system using methylene chloride:ethyl acetate (3:7 v/v) as a developing solvent and by electrophoresis using cellulose acetate moistened with 0.02 M phosphate buffer pH 7. The maximum radiochemical yield of {[}(125)I]Etodolac (87.7\%) was obtained. Labeled etodolac shows a good localization in inflamed muscle. It excretes mainly via kidney and to some via liver.
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