Nuclear Applications, Ege University Institute of Nuclear Sciences, Bornova, Izmir, Turkey.
Biopharm Drug Dispos. 2021 Jun;42(6):285-293. doi: 10.1002/bdd.2281. Epub 2021 May 6.
Early detection of the site of infection non-invasively with radiolabeled molecules is important for the success of treatment. Technetium-99m labeled antibiotics have the potential to discriminate between bacterial infection and sterile inflammation. Sultamicillin is the tosylate salt of the double ester of sulbactam plus ampicillin. In this study, sultamicillin was labeled with Tc according to the stannous chloride method. Quality control studies of radiolabeled sultamicillin were performed by radiochromatographic methods. In vitro binding assays were performed in live and heat-killed gram-positive Staphylococcus aureus and gram-negative Escherichia coli strains. The radiolabeling yield of Tc-sultamicillin was determined as 97.8% ± 3.1% (n = 5). The maximum bacterial uptake of Tc-sultamicillin was 80.7% ± 11.00% at 4 h for living S. aureus and 93.2% ± 4.40% at 2 h for E. coli. Bacterial uptake study results show that sultamicillin has the potential to be a nuclear imaging agent, especially in infections caused by gram-negative E. coli and gram-positive S. aureus.
早期无创地用放射性标记分子检测感染部位对于治疗的成功非常重要。锝-99m 标记的抗生素有可能区分细菌感染和无菌性炎症。舒他西林是舒巴坦与氨苄西林的双酯硫酸盐。在这项研究中,根据氯化亚锡法对舒他西林进行了放射性标记。通过放射色谱法对放射性标记的舒他西林进行了质量控制研究。在活的和热灭活的革兰氏阳性金黄色葡萄球菌和革兰氏阴性大肠杆菌菌株中进行了放射性结合测定。 Tc-舒他西林的标记产率为 97.8%±3.1%(n=5)。对于活的金黄色葡萄球菌,Tc-舒他西林的最大细菌摄取率在 4 小时时为 80.7%±11.00%,对于大肠杆菌,在 2 小时时为 93.2%±4.40%。细菌摄取研究结果表明,舒他西林有可能成为核成像剂,特别是在由革兰氏阴性大肠杆菌和革兰氏阳性金黄色葡萄球菌引起的感染中。