Characterization of 99mTc-ciprofloxacin radiopharmaceuticals as the infection imaging

Nurlaila Z; T. Hasan Basry; Rukmini Iljas; Mimin R. Suminar

doi:10.14499/indonesianjpharm0iss0pp214-221

Characterization of 99mTc-ciprofloxacin radiopharmaceuticals as the infection imaging

Nurlaila Z, T. Hasan Basry, Rukmini Iljas, Mimin R. Suminar

Abstract

Technetium-99m-ciprofloxacin (99mTc-ciprofloxacin) is used in nuclear medicine for infection diagnoses by imaging method. Since a succesful diagnose is depend on its radiopharmaceutical characters, the several physicochemical and biological characters should be investigated in order to have the expectation diagnose. The radiochemical purity was determined with ascending paper chromatography (Whatman 3MM) using 50 % of acetonitril solution as the solvents. The lipophilicity =(P) of 99mTcciprofloxacin was obtained by determination of octanol-water partition and the plasma binding protein was in-vitro investigated with precipitation method using 5% of trichloro acetic acid solution. The biological activity of antibiotic and microbiological uptake was observed in-vitro using Staphylococcus aureus (S. aureus) and Escherichia coli (E.coli). From the experiment, it was obtained that 99mTc-ciprofloxacin has 98.04 ± 0.51 % of radiochemical purity, the lipophilicity (P) = 0.088 ± 0.003, the human plasma binding protein of 64.20 ± 1.74%. The biological activity of 99mTcciprofloxacin was indentic with ciprofloxacin as the starting material and the maximum uptake by S. aureus and E.coli was 97.30 ± 1.01% and 96.03 ± 2.10%, at one hour incubation, respectively. The stability determination showed that 99mTc-ciprofloxacin was still able to be used until two hours after labelling with radiochemical purity of 97.55 ± 0.24%.
Key words :radiopharmaceutical, technetium-99m, ciprofloxacin, in, characterization.

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References

Anonim, 1995, Farmakope Indonesia, Edisi IV, Departemen Kesehatan Republik Indonesia, 891 – 899.

Britton K.E., Wareham D.W., Das S.S., Solanki K.K., Amaral H., Bhatnagar A., Kartamihardja A.H.S., Malamitsi J., Moustafa H.M., Soroa V.E., Sundram F.X., Padhy A.K., 2002, Imaging bacterial infecton with 99mTc-ciprofloxacin(Infecton), J.Clin.Pathol., 55, 817 – 823.

Das S.S., Hall A.V., Wareham D.W., Britton K.E., 2002, Infection imaging with radiopharmaceuticals in the 21st century, Brazilian Archives of Biology and Technology, 45, 223 – 228.

Gano L., Patricio L., Cantiho G., Pena H., Martins T., Marques E., 1998 Ciprofloxacin in imaging of infective versus sterile inflamation, IAEA-TecDoc 1029, Vienna, 213- 220.

Hasan Basry T., Nurlaila Z., Rukmini I., 2005, Formulasi radiofarmaka 99mTc-siprofloksasin untuk diagnosis infeksi. Seminar Nasional Sains dan Teknik Nuklir 2005, Puslitbang Teknik Nuklir-BATAN, Bandung.

Nurlaila Z., 2002, Radiofarmaka untuk deteksi inflamasi dan infeksi, Jurnal Sains dan Teknologi Nuklir Indonesia, 3(1),15 – 30.

Owunwanne A., Patel M., Sadek S., 1995, The Handbook of Radiopharmaceuticals, 1st ed., Chapman & Hall Medical, London, 9 – 12.

Saha G. B., 1986, Fundamental of Nuclear Pharmacy, 2nd ed., Springer-Verlag, New York, 74 - 75.

Theobald A., 1989, Radiopharmaceuticals Using Radioactive Compounds in Pharmaceutics and Medicine, Ellis Horwood Limited, New York, 28 – 57.

Winter F.D., Van De Wille C., Dumont F., 2001, Biodistribution and dosimetry of 99mTcciprofloxacin a promising agent for the bacterial infection, Eur.J. Nucl. Med., 28, 570 – 574.

DOI: http://dx.doi.org/10.14499/indonesianjpharm0iss0pp214-221