Optimized preparation and evaluation of 99mTc-Streptomycin

Document Type: Original Article


Radiation Application Research School, Nuclear Science and Technology Research Institute, Tehran, Iran


Introduction: The endemic occurrence of new strains of tuberculosis around the globe has initiated new research on developing diagnostic radiopharmaceutical based on antibiotics. Methods:Tc-99m labeled streptomycin was prepared using freshly milked 99mTcO4- and various concentrations of streptomycin, stannous chloride at various temperatures in high yield radiochemical purity shown by HPLC/RTLC. Results:At various pHs tested (3-10) the best labeling yield at optimized conditions were at 6-8 range, however pH.7 was considered the best. The radiochemical purity at the best optimized conditions was >95% as shown by RTLC and >97% using HPLC (specific activity; 1-3 GBq/mmole). The tracer proved to be stable in the final product and in presence of human serum at 37°C up to 2h. However, biodistribution and high resolution SPECT studies in wild type mice showed instability of the complex due to high stomach and thyroid activity uptake. Conclusion: Regardless the reported methods in the literature the direct 99mTc-labeling of aminoglycosides did not proved a suitable tracer.


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Britton KE, Vinjamuri S, Hall AV, Solanki K, Siraj QH, Bomanji J, Das S. Clinical evaluation of technetium-99m infecton for the localisation of bacterial infection. Eur J Nucl Med. 1997 May;24(5):553-6.

Calame W, Welling M, Feitsma HI, Ensing GJ, Pauwels EK. Improved detection of a staphylococcal infection by monomeric and protein A-purified polyclonal human immunoglobulin. Eur J Nucl Med. 1993 Jun;20(6):490-4.

Knight LC. Non-oncologic applications of radiolabeled peptides in nuclear medicine. Q J Nucl Med. 2003 Dec;47(4):279-91.

Xgen. Pharmaceuticals Inc. Streptomycin for Injection, USP. http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/064210s009lbl.pdf [Accessed 28 Dec 2014].

Zenilman JM, Miller MH, Mandel LJ. In vitro studies simultaneously examining effect of oxacillin on uptake of radiolabeled streptomycin and on associated bacterial lethality in Staphylococcus aureus. Antimicrob Agents Chemother. 1986 Dec;30(6):877-82.

Ercan MT, Aras T, Unsal IS.  Evaluation of 99mTc-erythromycin and 99mTc-streptomycin sulphate for the visualization of inflammatory lesions. Int J Rad Appl Instrum B. 1992 Oct;19(7):803-6.

European Association of Nuclear Medicine Radiopharmacy Committee, Guidelines on current good radiopharmacy practice (cGRPP) in the preparation of radiopharmaceuticals, version 2, 2007. http://www.eanm.org/publications/guidelines/gl_radioph_cgrpp.pdf [Accessed 28 Dec 2014].

Abdel Razzak M, Naguib M, el-Garhy M. Fate of sodium pertechnetate-technetium-99m. J Nucl Med. 1967 Jan;8(1):50-9.