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Radioiodination, purification and bioevaluation of Piroxicam in comparison with Meloxicam for imaging of inflammation
Faculty
Science
Year:
2009
Type of Publication:
Article
Pages:
589-598
Authors:
Seddik, U, Hussien, H, Amin, A. M, EL-Sheikh, R, Gouda, A. A
DOI:
10.1007/s10967-009-7483-9
Journal:
JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY SPRINGER
Volume:
280
Research Area:
Chemistry; Nuclear Science \& Technology
ISSN
ISI:000267032000022
Keywords :
Radioiodination, purification , bioevaluation , Piroxicam , comparison with
Abstract:
The present study is performed to compare the electrophilic substitution radioiodination reaction of two non-steroidal anti-inflammatory drugs namely, Piroxicam (Pirox) and Meloxicam (Melox) with (125)I where both chloramine-T (CAT) and iodogen were used as oxidizing agents. The factors affecting the percent of radiochemical yields such as drug concentration, pH of the reaction mixtures, different oxidizing agents, reaction time, temperature and different organic media were studied to optimize the conditions for labeling of Pirox and Melox and to obtain high radiochemical yields. The maximum radiochemical yield of (125)I-Piroxicam ((125)I-Pirox) was 94\% using 3.7 MBq of Na(125)I, 0.4 mM of Pirox as substrate, 3.6 mM of chloramine-T (CAT) as oxidizing agent in acetone at neutral pH = 7 and at 60 A degrees C within 20 min where the maximum radiochemical yield of (125)I-Melox was 92\% using 0.7 mM of Melox as substrate, 0.62 mM of iodogen as oxidizing agent in acetone at neutral pH = 7 and at 25 A degrees C within 30 min. The radiochemical yields were determined by TLC and high-pressure liquid chromatography (HPLC). Tracers showed good localization in inflamed muscle either septic or sterile. The collected data indicates that Pirox and Melox can be used as antiinflammatory imaging agents at 24 and 2 h post injection, respectively.
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