Synthesis and evaluation of (99m)Tc-moxifloxacin, a potential infection specific imaging agent.
To synthesize and evaluate a (99m)Tc labeled fluroquinolone, moxifloxacin as a potential bacteria specific infection imaging agent. A radiolabeling formulation including moxifloxacin, [Moxicip(TM) injection, Cipla] (4mg), sodium pertechnetate and stannous chloride (5microg) gave the best radiolabeling efficiency and moderately stable labeled (99m)Tc moxifloxacin. Quality control analysis was performed by ITLC. Rats and rabbit with infectious intramuscular lesions induced in either thigh with E. Colli were used for studying biodistribution and scintigraphic imaging of the labeled product. Imaging of an infected thigh of a rabbit was performed with a gamma-camera at various intervals. A good radiolabeling efficiency (90-95%) was obtained within 5min. No purification of the labeled product was done. Labeled product retained its radiochemical purity upto 85% even at 3h. Scintigraphy showed uptake in infectious lesions at 30min after injection, which remains constant upto 3h study. Abscess-to-muscle ratios were 1.60, 1.62, 1.74 and 1.75 at 30min, 1, 2 and 3h, respectively. Thus, (99m)Tc moxifloxacin, a new potential radiopharmaceutical has been developed for infection imaging agent.
Chattopadhyay
Sankha
S
Radiopharmaceuticals Laboratory, Board of Radiation and Isotope Technology, Variable Energy Cyclotron Centre, 1/AF, Bidhan Nagar, Kolkata 700 064, India. sankha@veccal.ernet.in
Saha Das
Sujata
S
Chandra
Susmita
S
De
Kakali
K
Mishra
Mridula
M
Ranjan Sarkar
Bharat
B
Sinha
Samarendu
S
Ganguly
Shantanu
S
D000818:Animals; D000890:Anti-Infective Agents / Q000737:chemistry / Q000493:pharmacokinetics; D001372:Aza Compounds / Q000737:chemistry / Q000493:pharmacokinetics*; D004927:Escherichia coli Infections / Q000000981:diagnostic imaging* / Q000378:metabolism*; D005240:Feasibility Studies; D024841:Fluoroquinolones; D007089:Image Enhancement / Q000379:methods; D007553:Isotope Labeling / Q000379:methods; D008657:Metabolic Clearance Rate; D000077266:Moxifloxacin; D009928:Organ Specificity; D049268:Positron-Emission Tomography / Q000379:methods*; D011804:Quinolines / Q000737:chemistry / Q000493:pharmacokinetics*; D011817:Rabbits; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics; D051381:Rats; D017208:Rats, Wistar; D013667:Technetium / Q000737:chemistry / Q000493:pharmacokinetics*; D014018:Tissue Distribution
D000890:Anti-Infective Agents; D001372:Aza Compounds; D024841:Fluoroquinolones; D011804:Quinolines; D019275:Radiopharmaceuticals; D013667:Technetium; D000077266:Moxifloxacin