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Synthesis of 99mTc-Rifabutin: A Potential Tuberculosis Radiodiagnostic Agent.
Infect Disord Drug Targets. 2017 Jun 05;:
Authors: Shah SQ, Alam M
Abstract
BACKGROUND: Rifabutin (RFN) is bactericidal antibiotic with a very broad spectrum of activity against gram positive & gram negative organisms including Pseudomonas aeruginosa and specifically Mycobacterium tuberculosis.
OBJECTIVE: RFN inhibits DNA dependent RNA polymerase activity in susceptible cells. In the instant work, the therapeutic characteristics of RFN were intended for diagnostic rationale by labeling it with 99mTc (Technetium-99m). The 99mTc labeled RFN (99mTc-RFN) was investigated for labeling capacity, steadiness in saline & serum, in vitro Mycobacterium tuberculosis (MBT) uptake & distribution in MBT stained animal model rats.
METHOD: It was found that 99mTc-RFN prepared by mixing 2 mg of RFN, 2.5 mCi sodium pertechnetate, 150 µg stannous chloride at pH 5.4 gave highest yield after 30 minutes and was intact above 90 % after 240 min at room temperature in saline.
RESULTS: The 99mTc-RFN showed a stable profile in serum at 37 °C and impurities appeared up 16 h was 15.20 %. The maximum in vitro MBT uptake observed in live strain was 71.75 ± 0.75 %. The premier uptake observed in the MBT infected site (target site) was 14.15 ± 0.00 %, in animal model rat.
CONCLUSION: Higher labeling capacity, steadiness in saline & serum, higher MBT uptake, maximum uptake in the MBT infected sites and precise imaging posed 99mTc-RFN as an alternate radio-drug for tuberculosis scintigraphy.
PMID: 28595542 [PubMed - as supplied by publisher]
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