AIM OF THE STUDY: A new method to label antibiotics with 99mTc, using a third generation, wide spectrum cephalosporine (ceftizoxime), is presented. MATERIAL AND METHODS: 2.5 mg of ceftizoxime, 6.25 mg sodium dithionite in sodium bicarbonate buffer (pH=11.4) as a reductor agent, and 300 MBq of 99mTc were used. The final pH was adjusted to 8.4 with NaOH 0.1N. Radiochemical purity was assessed using ITLC-SG/MEK, ITLC-SG/0.9% NaCl and reverse phase HPLC. Biologic activity was assessed with the agar diffusion technique soaked with E. Coli in disks containing 10.5 microg labelled and non-labelled antibiotic. The maintenance of antibiotic activity was assessed by the diameter of the inhibition halos measured after 24 hours of incubation at 37 degrees C. RESULTS: The labelling efficiency was 94.9 +/- 2.4% (n = 20) and the complex was stable up to 6 h post-labelling. The HPLC chromatography showed five peaks: two of them at 1.7-2.0 min, which corresponds to the ceftizoxime derived product (82%-83% of the absorbance and about 90% of the radioactivity) and a third one at 4.7 min which corresponds to the intact ceftizoxime (6% of absorbance). The remaining two peaks appeared at 3.8 and 6.7 min and represented about 7%-8% of the absorbance. The antibiotic activity of the ceftizoxime-derived compound (CDC) was 83% of the unlabelled one. CONCLUSIONS: 1) The labelling method of ceftizoxime described causes a modification in its structure. 2) The 99mTc binds to the newly formed compound with high labelling efficiency and an acceptable shelf life stability. 3) The 99mTc-CDC maintains 83% of the original antibiotic activity and could be used for the detection of in vivo infection.
AIM OF THE STUDY: A new method to label antibiotics with 99mTc, using a third generation, wide spectrum cephalosporine (ceftizoxime), is presented. MATERIAL AND METHODS: 2.5 mg of ceftizoxime, 6.25 mg sodium dithionite in sodium bicarbonate buffer (pH=11.4) as a reductor agent, and 300 MBq of 99mTc were used. The final pH was adjusted to 8.4 with NaOH 0.1N. Radiochemical purity was assessed using ITLC-SG/MEK, ITLC-SG/0.9% NaCl and reverse phase HPLC. Biologic activity was assessed with the agar diffusion technique soaked with E. Coli in disks containing 10.5 microg labelled and non-labelled antibiotic. The maintenance of antibiotic activity was assessed by the diameter of the inhibition halos measured after 24 hours of incubation at 37 degrees C. RESULTS: The labelling efficiency was 94.9 +/- 2.4% (n = 20) and the complex was stable up to 6 h post-labelling. The HPLC chromatography showed five peaks: two of them at 1.7-2.0 min, which corresponds to the ceftizoxime derived product (82%-83% of the absorbance and about 90% of the radioactivity) and a third one at 4.7 min which corresponds to the intact ceftizoxime (6% of absorbance). The remaining two peaks appeared at 3.8 and 6.7 min and represented about 7%-8% of the absorbance. The antibiotic activity of the ceftizoxime-derived compound (CDC) was 83% of the unlabelled one. CONCLUSIONS: 1) The labelling method of ceftizoxime described causes a modification in its structure. 2) The 99mTc binds to the newly formed compound with high labelling efficiency and an acceptable shelf life stability. 3) The 99mTc-CDC maintains 83% of the original antibiotic activity and could be used for the detection of in vivo infection.