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Brain imaging is a technique that scientists and physicians use to view and monitor brain areas to diagnose abnormalities in the brain. This study aimed to develop a potential labeled compound for non-invasive brain imaging. Pramipexole (a drug thµat has the ability to penetrate the blood-brain barrier) has been successfully labeled iodine-131 (131I) through a diazonium salt reaction, followed by a sandmeyer reaction at room temperature, and physicochemical characterization has been carried out. The reaction parameters studied were computation simulation, pramipexole and sodium nitrite amounts, diazotization reaction time, pH of the mixture, the optimum amount of chloramine T and sodium metabisulfite, and optimum reaction time. As for the physicochemical characterization, the parameters tested were: radiochemical purity, lipophilicity, plasma protein binding, electric charges, and stability. The [131I]I-Pramipexole labeled compound showed no significant energy difference between pramipexole and pramipexole labeled 131I; the optimum condition of reaction was: pramipexole amount 100 µg, sodium nitrite 50 µg, diazotization reaction time 2-3 hours, pH of the mixture 6, chloramine T amount 50 µg, sodium metabisulfite amount 50 µg, and labeling reaction time 15 minutes at room temperature. The physicochemical characterization showed that radiochemical purity was 97.54 ± 1.4%, lipophilicity score (log P) 0.03 ± 0.01, protein plasma binding score 44.95 ± 0.80%, neutral electric charges, and [131I]I-pramipexole remained stable until 4 hours at four °C, so the [131I]I-Pramipexole labeled compound is feasible to proceed to biological studies. [ABSTRACT FROM AUTHOR]

Cancer is a genetic disease that causes by mutations in DNA from a normal cell to a cancer cell. As a result, the cancer cell grows quickly and spread to other parts of the body; this condition became the leading cause of death. One of the detection methods currently used to detect tumors and metastatic tissues is conducted with radiopharmaceutical of [18F] fluoro-2-deoxy-2-D-glucose (18F-FDG). This method is quite accurate but is relatively expensive because it needs PET / CT camera that is still limited in Indonesia. With these limitations, in previous studies was developed 99mTc-DTPA-deoxy-D-glucose (99mTc-DTPA-DG) radiopharmaceutical that application using a gamma camera. As new radiopharmaceuticals, the physical and chemical characteristics of these compounds must be known. In this study, physicochemical characterization tests determined radiochemical purity, electric charge, lipophilicity (log P), and plasma protein binding. The study determines that 99mTc-DTPA-DG radiopharmaceuticals have high radiochemical purity (95.28 ± 0.87 %), neutral electric charge, the lipophilic value (log P) -1.24 and the plasma protein binding was 72.09 ± 1.65 %. The 99mTc-DTPA-DG radiopharmaceuticals liquid kit that storage up to 60 days in -20oC or additional volumes of technetium-99m up to 3 mL still gives radiochemical purity above 95%. This study obtained physicochemical characteristics that can be used as reference in a subsequent in-vivo study of 99mTc-DTPA-DG radiopharmaceutical. A comprehensive information on the bioactivity of this compound for diagnostic cancer can be obtained from an in-vivo study. [ABSTRACT FROM AUTHOR]

Quality control of Radiopharmaceutical or labeled compound is performed to ensure the optimal quality of radiopharmaceutical or labeled compound. The existence of chemical/radiochemical impurities cause false diagnosis or inefficient therapy due to unnecessary radiation or undesirable high background. The quality control of labeled compound involves two different aspects including pharmaceutical and radioactive parameters. The objective of this study is to test the radiochemical stability of [131I]I-Rutin produced under acidic conditions under different storage conditions as evidenced by the quality of its radiochemical purity. The radiochemical purity of 131I-Rutin carried out by thin-layer chromatography method (TLC-SG F254 as stationary phase and methanol as mobile phase). This study investigated the quality of routine in time under the influence of environmental factors. The results showed that [131I]I-Rutin was stable for up to 4 hours at 37° C with radiochemical purity of [131I]I-Rutin 93.90% ± 2.57%. [ABSTRACT FROM AUTHOR]

Cancer is the uncontrolled growth of new cells beyond the normal limits. The process by which cancers invade and spread to the other organs is called metastasis, this condition became the leading cause of death. One of detection methods that are currently used to detect tumors and metastatic tissues is conducted with radiopharmaceutical of [18F] fluoro-2-deoxy-2-D-glucose ([18F] FDG). This method is quite accurate, but is relatively expensive because it needs PET / CT camera that is still limited in Indonesia. Therefore, this study was conducted to develop other imaging methods using SPECT-CT camera that is cheaper and easy to reach especially for developing countries. Labelling 2-deoxy-D-glucose with technetium-99m (99mTc) indirectly using diethylenetriaminepentaacetic acid (DTPA) as a co-ligand / bifunctional agent has been carried out. The determination of the optimum conditions for the labelling of 99mTc-DTPA-DG were done by varying the amount of reducing agent (SnCl2.2H2O), ligand (2-deoxy-D-glucose), pH, and incubation time. Radiochemical purity of 99mTc-DTPA-DG was determined by ascending paper chromatography and electrophoresis paper. The results showed that the labelling optimum conditions of 99mTc-DTPA-DG was achieved by the number of ligand 2-deoxy-D-glucose as much as 2 mg, co-ligand DTPA 750 µg, 50 µg SnCl2.2H2O, the reaction takes place at pH 6 with an incubation time of 30 min at room temperature. 99mTc-DTPA-DG has a radiochemical purity of 93.16±1.31% and the electrophoresis results showed that there is a difference between the peaks of 99mTc-DTPA-DG with other impurities including 99mTc-DTPA. [ABSTRACT FROM AUTHOR]