• IE interfaces
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• v.24 no.3
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• pp.187-195
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• 2011

The automatic radiopharmaceutical module consists of several 2-way valves, couple of syringes, gas supply unit, heating(cooling) unit and sensors to control the chemical reagents as well as to help the chemical reaction. In order to control the actuators of radiopharmaceutical module, the process is tabulated using spread sheet as like excel. Unlike the common program, a trivial error is too critical to allowed in the process because the error can lead to leak the radioactive reagent and to cause the synthesis equipment failure during synthesizing. Hence, the synthesis process has been validated using graphic simulation while the operator checks the whole process visually and undergoes trial and error. The verification of the synthesis process takes a long time and has a difficulty in finding the error. This study presents a methodology to verify the process algebraically while the radiopharmaceutical module is converted to the network model. The proposed method is validated using actual synthesis process.

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.8 no.2
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• pp.87-93
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• 2022

[¹⁸F]FDG is known as the most widely used radiopharmaceutical in the imaging field of nuclear medicine worldwide. With the introduction of PET equipment, the demand for [¹⁸F]FDG has increased and the production volume has also increased. However, in order to increase production, the use of ¹⁸F radioisotope must be increased or [¹⁸F]FDG must be synthesized in high yield. Therefore, in order to meet the high yield and purity of radiopharmaceuticals, a radiopharmaceutical automatic synthesizer was required. As the use of [¹⁸F]FDG increased, automated synthesizer manufacturers supplied various types of radiopharmaceutical automated synthesizers to the market. In this study, we developed a commercialized [¹⁸F]FDG radiopharmaceutical automatic synthesizer (sCUBE FDG) using a disposable cassette type that complies with GMP developed by FutureChem, a leading radiopharmaceutical company. We used sCUBE FDG to verify the production process, radiopharmaceutical's quality (radiochemical purity, etc.), and radiochemical yield of [¹⁸F]FDG. As a result of optimizing the automatic synthesis process and synthesizing a total of 30 times, the production time was 35 ± 3 minutes and the average production yield was 65.6%.

• IE interfaces
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• v.24 no.2
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• pp.156-163
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• 2011

The radiopharmaceutical synthesis for PET (positron emission tomography) is composed of chemical reactions using automated synthetical equipment. Due to the radioactive material, the automated equipment is being frequently developed to replace human operators who conduct dangerous, repetitive and dexterous operations. As to operation, the manipulating program is commonly coded using the spread sheet while the whole actuators are mapped in every step. The process map (program) is changed according to such parameters as temperature of reactor, keeping time, mixture sequence and amount of reagent. In cases of customizing the automated synthetical equipment or developing the new radiopharmaceuticals, lots of experiments should be conducted and the programming mistake is not allowed as it can lead abnormal control of the equipment to leak the radioactive materials. The exact process map has depended on trial and error manner. Thus, this study developed the methodology to tabulate the synthetical process to convert the process map automatically while the synthetical module formation is represented by a network model. The proposed method is validated using the actual radiopharmaceutical synthetical procedure.

• Journal of the Institute of Electronics and Information Engineers
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• v.51 no.4
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• pp.193-200
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• 2014

In this paper, the prototype of one-channel gamma-ray spectroscope for automatic radiopharmaceutical systhesis system was designed and characterized. The prototype employed CZT (CdZnTe) spear detector for gamma-ray detection and employed analog-type signal processing method. A radioactive sample Co-60 was used for measuring performance of the gamma-ray spectroscope and energy spectrum is gained with bandwidth of 1173keV. The analog board is made up of SF (shaping filter) and PHA (peak and hold amplifier) for shaping CZT output signal appropriately and ADC (analog to digital converter) and FPGA (field programmable gate array) for drawing gamma-ray spectrum by counting the digitalized gamma-ray signal data.

• Nuclear Medicine and Molecular Imaging
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• v.43 no.5
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• pp.478-486
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• 2009

Purpose: 5-iododeoxyuridine analogues have been exclusively developed for the potential antiviral and antitumor therapeutic agents. In this study, we synthesized carbocyclic radioiododeoxyuridineanalogue (ddIVDU) and carbocyclic intermediate as efficient carbocyclic radiopharmaceuticals. Materials and Methods: The synthesis is LAH reduction, hetero Diels-Alder reaction as key reactions including Pd(0)-catalyzed coupling reaction together with organotin. MCA-RH7777 (MCA) and MCA-tk (HSV1-tk positive) cells were treated with various concentration of carbocyclic ddIVDU, and GCV. Cytotoxicity was measured by the MTS methods. For in vitro uptake study, MCA and MCA-tk cells were incubated with 1uCi of [$^{125}I$]carbocyclic ddIVDU. Accumulated radioactivity was measured after various incubation times. Results: The synthesis of ddIVDU and precursor for radioiodination were achieved from cyclopentadiene in good overall yield, respectively. The radioiododemetallation for radiolabeling gave more than 80% yield with > 95% radiochemical purity. GCV was more toxic than carbocyclic ddIVDU in MCA-tk cells. Accumulation of [$^{125}I$]carbocyclic ddIVDU was higher in MCA-tk cells than MCA cells. Conclusion: Biological data reveal that ddIVDU is stable in vitro, less toxic than ganciclovir (GCV), and selective in HSV1-tk expressed cells. Thus, this new carbocyclic nucleoside, referred to in this paper as carbocyclic 2',3'-didehydro-2',3'-dideoxy-5- iodovinyluridine (carbocyclic ddIVDU), is a potential imaging probe for HSV1-tk.

• Journal of Radiation Industry
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• v.5 no.4
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• pp.313-316
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• 2011

[$^{18}F$]FDG (2-[$^{18}F$] Fluoro-2-deoxy-D-Glucose), which is required Automated Synthetic Module for production, is most often used Radiopharmaceuticals in nuclear medicine. In this study, an Automated Synthesis Module was developed to produce FDG in two consecutive time when F-18 feds continuously by modifying a domestic FDG Automated Synthetic Module on structural geometry and control system. The results were showed that the Average Synthesis Yields on the developed Automated Synthetic Module were $45{\pm}3%$ (n=20), $50{\pm}3%$ (n=20) respectively. The Quality Control results, such as Radio TLC, Radiochemical purity, Gamma-counter, pH, LAL Test, Micro bacteria test, showed in same level with domestic [$^{18}F$]FDG Auto-Synthetic modules. Therefore, if some features were improved by considering the components life time and appearance, commercial sales can be expected because of low price and easy maintenance compared with foreign products.

• Bulletin of the Korean Chemical Society
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• v.32 no.6
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• pp.1931-1935
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• 2011

The synthesis of carbocyclic analogues of normal nucleosides has grown exclusively since they have shown potential antiviral and antitumor activities. Radiolabeled cis-1-[4-(hydroxy-methyl)-cyclopent-2-enyl]-5-$[^{124}I]$-iodocytosine (carbocyclic d4IC) and cis-1-[4-(hydroxy-methyl)-cyclopent-2-enyl]-5-(2-$[^{124}I]$iodovinyl)cytosine(carbocyclic d4IVC) were synthesized. The synthetic route employed Pd(0)-catalyzed coupling reaction together with organotin and exchange reaction for radioiodination as key reactions. Carbocyclic $[^{124}I]$d4IC gave more than 75% radiochemical yield with greater than 95% radiochemical purity. Carbocyclic $[^{124}I]$d4IVC gave more than 80% radiochemical yield with greater than 95% radiochemical purity.

• Bulletin of the Korean Chemical Society
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• v.25 no.8
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• pp.1147-1150
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• 2004

Hypericin (1,3,4,6,8,13-hexahydroxy-10,11-dimethylphenanthro[1,10,9,8-opqra]perylene-7,14-dione), an antidepressant which is also known to be a potent protein kinase C (PKC) inhibitor was synthesized as a precursor for radioiodine labeling via two step reactions. Malignant glioma cells express higher PKC activity compared to untransformed glial cell. Here we report the synthesis and radioiodine labeling of hypericin as a potential brain tumor imaging radiopharmaceutical. The reference compound, 2-iodohypericin, and its radiolabelled analogues, 2-[$^{123}I$]iodohypericin and 2-[$^{124}I$]iodohypericin have been prepared by the reaction of hypericin with NaI or [$^{123}I$]NaI or [$^{124}I$]NaI. The labeling yield was 60-65% for each analogue and the optimal reaction time was 10 min. The purification and isolation of the labelled products were achieved by a reversed-phase HPLC.

• Journal of Radiation Industry
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• v.11 no.1
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• pp.13-18
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• 2017

Recently, the number of PET cyclotrons has increased in Korea. A cyclotron mainly produces $^{18}F$, which is used for the production of [$^{18}F$]FDG, a cancer diagnostic radiopharmaceutical. For radiation protection, the discharge control standard under the Nuclear Safety Act limits the radioactive concentration of $^{18}F$ in the exhaust discharged from a nuclear power utilization facility to below $2,000Bq\;m^{-3}$. However, the radioactive concentration of $^{18}F$ discharged during [$^{18}F$]FDG production at the cyclotron facility at Chosun University is maintained at about $1,500Bq\;m^{-3}$ on average, which is 75% of the concentration limit of the discharge control standard, and temporarily exceeds the standard as per the real-time monitoring results. This study evaluated the performance of the exhaust filter unit of the cyclotron facility at Chosun University by assessing the concentration of $^{18}F$ in the exhaust, and an experiment was conducted on the discharge reduction, where $^{18}F$ is discharged without reacting with the FDG precursors during [$^{18}F$]FDG synthesis and is immediately captured by the [$^{18}F$]FDG automatic synthesis unit. Based on the performance evaluation results of the exhaust filter at the cyclotron facility of Chosun University, the measured capture efficiency before and after the filter was found to be 92%. Furthermore, the results of the discharge reduction experiment, where the exhaust $^{18}F$ was immediately captured by the [$^{18}F$]FDG synthesizer, showed a very satisfactory 94.3% reduction in the concentration of discharge compared to the existing discharge concentration.

• Journal of Radiation Industry
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• v.4 no.1
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• pp.1-6
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• 2010

The purpose of this study is to synthesize the radio fluorine labelled isoquinoline salt derivative as new radiopharmaceutical for imaging tumors using positron emission tomography (PET). The planarity of isoquinoline allows to inhibit topoisomerase or intercalate between adjacent DNA base pairs, which result in producing double strand breaks in the DNA and a cell death. Therefore, the isoquinoline has seemed to have a potential anticancer activity. In order to obtain 2-(5-[$^{18}F$]fluoropentylisoquinolinium salt with good radiochemical yield, tosylated precursors have been synthesized. The labelling reaction was carried out for 30 minute in HMPA at $120^{\circ}C$. The radiochemical yield was about 50~60%.