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Technetium‐99m labeling and freeze‐dried kit formulation of levofloxacin (L‐Flox): a novel agent for detecting sites of infection
Author(s) -
Elghany E. A.,
Amin A. M.,
Elkawy O. A.,
Amin Magdy
Publication year - 2007
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.1153
Subject(s) - chemistry , pertechnetate , levofloxacin , technetium , chloride , technetium 99m , nuclear chemistry , radiochemistry , scintigraphy , nuclear medicine , biochemistry , organic chemistry , medicine , antibiotics
Abstract In this study, the labeling method of levofloxacin with technetium‐99m and its biological evaluation were described. 99m Tc‐L‐Flox was synthesized via direct complexation with technetium‐99m in the presence of stannous chloride dihydrate as reducing agent. The optimum amounts of the reactants are: 1–2 mg levofloxacin, 150 µg stannous chloride dihydrate and 48–1490 MBq pertechnetate. The reaction mixture was bring to pH 6 and kept at room temperature for 30 min. The labeled levofloxacin was stable for more than 8 h. The in vivo evaluation of 99m Tc‐L‐Flox in man‐induced inflammation models showed that this tracer was localized with different values. The live E. Coli model had the highest value which was 2.9%, the heat killed E. coli model had a value of 2.0%, and the turpentine oil model had a value of 1.2% at 24 post injection, while the non‐inflamed muscle had activity of 0.5%. All the gathered biological data support the usefulness of 99m Tc‐L‐Flox as infection imaging agent. The freeze‐dried form of Sn‐L‐Flox was prepared and found meet all the radiochemical and biological tests. Copyright © 2007 John Wiley & Sons, Ltd.