Thesis (Ph.D.) - Cairo University - Faculty of Pharmacy - Department of Pharmaceutics

The aim of this study in its first chapter includes studying the factors affecting the labeling of tiludronate with Tc-99m, using direct labeling technique, and determination of the radiochemical purity of the labeled compound. The second chapter includes formulation of a novel bone imaging probe via Synthesis of a new organic ligand (EMIHPBP) with expected higher selective bone targeting, characterize the synthesized compound using IR, elemental analysis, mass spectroscopy and 1H-NMR, radiolabeling of the newly synthesized EMIHPBP with the radioactive technetium-99m, study factors affecting the labeling yield in details , evaluate its utility as a novel bone scintigraphy radiopharmaceutical agent via studying its biological distribution, finally tracing pharmacokinetics of 99mTc-EMIHPBP complex into bone was also been studied. Tiludronate and EMIHPBP were labeled with Tc-99m and gave maximum labeling yield of 93 and 91.51% ,respectively, at 200 and 1000?g of tiludronate and EMIHPBP, 2 and 50mg of NaBH4, reaction time of 30, and 60 min, respectively, at pH 10and 9 at room temperature. 125I-sibutramine, 125I-99mTc-EMIHPBP and 99mTc-tiludronate were stable up to 6h in-vitro and their uptake in bone was 31.6 and 29.74% injected activity/gm tissue organ at 60 and 300 min post-injection, respectively, and so they can be used as new radiopharmaceuticals for bone imaging

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