Technetium-99m ceftizoxime kit preparation

Abstract

The aim of this work was to prepare a kit of 99mTc-ceftizoxime (99mTc-CFT), with stability and biological activity preserved, able to identify a septic focus (E. coli) in the experimental infection model in rats. The preparation of the CFT kit involved the use of lyophilized solutions containing the antibiotic ceftizoxime and the sodium dithionite reducing agent (6.0 mg/mL). After lyophilization, the kit was reconstituted with 1.0 mL of sodium 99mTc-pertechnetate solution (Na99mTcO4-) with an activity of 370 MBq. The solution was boiled for 10 min and filtered through a cellulose ester filter. The labeling efficiency was on the order of 92%, remaining stable for six hours and the kit remained stable for two months. The biological activity of the 99mTc-CFT was evaluated by diffusion in agar impregnated with E.coli and S. aureus. Seven Wistar rats, weighing from 200 to 250 g, were used for the development of the septic focus. After 24 hours from the induction of the infectious site (E.coli), the animals were anesthetized and 0.1 mL of 99mTc-CFT (37 MBq) was injected into the tail veins of the animals. The images were obtained with a gamma camera one, two and six hours after injection and the regions of interest (ROIs) were calculated. The diameters of the inhibition halos for 99mTc-CFT were 27.16 ± 0.23 and 27.17 ± 0.20 for S.aureus and E.coli, respectively, while those for the unlabeled CFT were 30.4 ± 0.33 and 29.43 ± 0.26, respectively. The results for the biodistribution of 99mTc-CFT in infected animals furnished a ratio of 1.97 ± 0.31, 2.10 ± 0.42 and 2.01 ± 0.42 for cpm-target/cpm-no target for the one, two and six-hour periods, respectively. The images showed a clear uptake of labeled antibiotic (99mTc-CFT) by the infectious site during the experiment. The results attest to the viability of producing a kit with 99m technetium-labeled ceftizoxime for the investigation of infectious processes.<br>O objetivo deste trabalho foi preparar um kit de Tc-99m Ceftizoxima (99mTc-CFT), com estabilidade e atividade biológica preservadas, capaz de identificar um foco séptico (E.coli) em um modelo experimental de infecção em ratos. A preparação do kit de CFT baseou-se em uma mistura de soluções contendo o antibiótico ceftizoxima (2,5mg/mL) e o agente redutor ditionito de sódio (6,0mg/mL) que foram submetidos a um processo de liofilização. Após a liofilização, o kit foi reconstituído with 1,0 mL de solução de pertecnetato de sódio (Na99mTcO4 -), contendo uma atividade de 370 MBq. Em seguida, a solução foi incubada, por 10 min, em banho fervente (1000C) e, posteriormente, foi resfriada em água corrente por 5 min. A eficiência de marcação foi da ordem de 92% permanecendo estável por 6 horas e o kit permaneceu estável por 2 meses. A atividade biológica do 99mTc-CFT foi avaliada por difusão em ágar impregnado com E.coli e S. aureus. Foram utilizados 07 ratos Wistar, pesando entre 200 a 250 g, para o desenvolvimento do foco séptico. Após 24 horas da indução do foco infeccioso (E.coli), os animais foram anestesiados e 0,1 mL da 9...

Efficacy of99mTc-Labeled Ceftizoxime in the Diagnosis of Subclinical Infections Associated with Titanium Implants in Rats

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Alendronate-coated long-circulating liposomes containing 99mtechnetium-ceftizoxime used to identify osteomyelitis

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Influence of biomaterials on scintigraphic diagnosis of periprosthetic infections. Ceftizoxime-99m technetium model

“…In our study, we used a third-generation cephalosporin as the radiopharmaceutical that is active against gram-positive, gram-negative, and anaerobic bacteria. Moreover, its application as a radiopharmaceutical has shown to be effective for soft tissue infections, osteomyelitis, and prosthetic infections 10,11,12,14,15 .…”