• 대한핵의학회:학술대회논문집
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• 1973.11a
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• pp.62.3-62.3
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• 1973

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.5 no.2
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• pp.158-162
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• 2019

[¹¹C]GR205171, a Neurokinin 1 (NK1) radioligand, has been known as such a promising PET probe for quantitation of NK1 receptors in the brain by positron emission tomography (PET) imaging. First trial to synthesis of [¹¹C]GR205171 was to use methylene chloride and tetrabutylammonium hydroxide for preactivation of precursor, but the result was not successful in radiochemical yield (0~25%) and unreliable. 7 years later, inorganic base (Cs₂CO₃) was tried to achieve higher radiochemical yield, and they showed higher yield (~53%). We have tried to repeat the same synthesis method, but it did not work properly, because there were the lack of the detail procedure and still reproducibility in radiochemical yield. Here we report the improved synthesis protocol to produce [¹¹C]GR205171 in high yield via commercial automated synthesizer. The sonicator which combines water heating bath was used to activate desmethyl-GR205171, and this method showed high efficiency and reasonable yields (4.7 ± 0.6%, non-decay corrected from molecular sieve trap) with >95% radiochemical purity.

• The Korean Journal of Nuclear Medicine
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• v.24 no.1
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• pp.49-55
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• 1990

For the development of $^{99m}Tc-labelled$ 3-iodo-2,4,6-trimethyl-iminodiacetic acid $(^{99m}Tc-IOTIDA)$, various experiments such as synthesis of IOTIDA, establishment of labelling conditions, determination of radiochemical purity, examination of stability, and organ distribution of rat were carried out. 1) IOTIDA was synthesized with a total yield of 42% from the starting material of 2,4-6-trimethylaniline via chloroacetylation, iodination, and condensation with iminodiacetic acid (IDA). 2) Freeze-dried instant labelling kits were prepared from aqueous solution $(pH\;5.8\sim6.0)$ so as to contain 40 mg IDA compound and 0.4 mg $SnCl_2$, per vial. Labelling of the contents of kit vials with $Na^{99m}TcO_4$, exhibited formation of two kinds of complex which was identified by ITLC-SA. After labelling, complex ( I ) was gradually converted to complex (II) with time. Labelling yield and radiochemical purity were above 99.5% based on the two complexes over-all. 3) $^{99m}Tc-IOTIDA$ maintained high radiochemical purity of above 99% until 6 hours after preparation at room temperature. Instant labelling kits stored at $4^{\circ}C$ for 6 month period also exhibited high labelling yield of above 99%. 4) Results obtained from animal experiments showed that most of the $^{99m}Tc-IOTIDA$ was rapidly excreted through hepatobiliary track into the intestines but with negligible renal excretion.

• The Korean Journal of Nuclear Medicine
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• v.23 no.1
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• pp.63-69
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• 1989

In order to develop technetium-99m-labelled human albumin microsphere (HAM) for lung scintigraphy, various experimemts such as preparation and fractionation of HAM, establishment of optimal labelling conditions, determination of radiochemical purity, stability test and biodistribution of $^{99m}Tc-HAM$ were carried out. HAM was prepared from the suspension of 1ml aqueous human serum albumin (25%) in 130 ml of olive oil at $130\sim135^{\circ}$ with vigorous stirring. The resulting HAM was fractionated with microsieve to get the desired particle size $(15\sim50\mu)$ and autoclaved for sterilizaiton. The HAM particles were treated with stannous chloride and the pH of the suspension was adjusted to $3.0\sim3.5$ with phosphate buffer. After freeze-drying the contents of single reaction vial containing 5 mg of HAM and 0.2 mg of $SnCl_2$ it was reacted with $Na^{99m}TcO_4$. The labelling yield was higher than 99.5% and the stability of $^{99m}Tc-HAM$ was high enough to maintain 99.1% of radiochemical purity up to 24 hours. Lung and liver uptake in mice was found to be 94% and 0.9%, respectively. Excellent rabbit and human lung scans were also obtained.

• 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%.

• Nuclear Engineering and Technology
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• v.55 no.2
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• pp.669-673
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• 2023

Introduction: The crucial step in preclinical process of radiopharmaceutical production is internal dosimetry evaluation by different ways to realize radiobiological dose-response relationships and to extract the results for clinical use. Till now several bone-seeking radiopharmaceuticals have been developed for bone metastasis. Interesting features of bisphosphonates attracted attentions to them in the field of radiopharmaceutical therapy and studies on new generation of them have been doing too. Materials and methods: In this study, we used ZNA as representative of the third generation. The radiopharmaceutical ¹⁸⁸Re-ZNA was produced and its radiochemical purity was investigated. Then, the biological distribution of the produced radiopharmaceutical at 1, 2, 4 and 24 h after injection on different organs of mice were investigated. Finally, the absorbed dose of organs in the human body was assessed using the RADAR method. Results: The results show 96% radiochemical purity of the ¹⁸⁸Re-ZNA radiopharmaceutical. The amount of %ID/g in bone is 1.131% after 1 h and in 24 h it has a significant amount compared to other organs, that is 0.516%. Also dosimetric results show that the highest absorption dose is related to bone and the amount of this dose is 0.050 mGy/MBq. Conclusion: Considering the possibility of producing the ¹⁸⁸Re-ZNA radiopharmaceutical, as well as the proper distribution of this radiopharmaceutical in target and non-target organs and increasing the absorbed dose in bone, it can be concluded that this radiopharmaceutical can be useful in the "radiopharmaceutical therapy" in metastases.

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.3 no.2
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• pp.98-102
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• 2017

We demonstrate a detail protocol for the radiosynthesis of a $^{125}I-labeled$ tetrazine prosthetic group and its application to the efficient radiolabeling of trans-cyclooctene-group conjugated human serum albumin (3) using inverse-electron-demand Diels-Alder reaction. Radioiodination of the stannylated precursor (2) was carried out by using [$^{125}I$]NaI and chloramine T as an oxidant at room temperature for 15 min. After HPLC purification of the crude product, the purified $^{125}I-labeled$ azide ([$^{125}I$]1) was obtained with high radiochemical yield ($65{\pm}8%$, n = 5) and excellent radiochemical purity (>99%). Inverse-electron-demand Diels-Alder reaction between ([$^{125}I$]1) and 3 gave the $^{125}I-labeled$ human serum albumin ([$^{125}I$]4) with more than 99% of radiochemical yield as determined by radio-thin-layer chromatography (radio-TLC). These results clearly indicate that the present radiolabeling method will be useful for the efficient and convenient radiolabeling of trans-cyclooctene-group containing biomolecules.

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.4 no.2
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• pp.85-89
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• 2018

We demonstrate a detail protocol for the radiosynthesis of an $^{125}I$-labeled MSTP prosthetic group and its application to the efficient radiolabeling of human serum albumin (HSA). Radioiodination of the precursor (2) was carried out by using $[^{125}I]$NaI and chloramine T as an oxidant at room temperature for 15 min. After HPLC purification of the crude product, the purified $^{125}I$-labeled MSTP ($[^{125}I]1$) was obtained with high radiochemical yield ($73{\pm}5%$, n = 3) and excellent radiochemical purity (>99%). Site-specific reaction between ($[^{125}I]1$) and HSA gave the $^{125}I$-labeled human serum albumin ($[^{125}I]3$) with more than 99% of radiochemical yield as determined by radio-thin-layer chromatography (radio-TLC). These results clearly demonstrate that the present radiolabeling method will be useful for the efficient and convenient radiolabeling of thiol-bearing biomolecules.

• Journal of Radiation Protection and Research
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• v.35 no.4
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• pp.151-156
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• 2010

The types of test items which were recorded in this test report of quality control domestic $^{18}F$-FDG radiopharmaceutical which consisted of 13 different types: appearance, half-life, radioactive heterokaryosis, radiochemical Confirmation (measure of Rf value), radiochemical Purity, Ethanol, Acetonitrile, Kryptofix, Aluminium, pH, Endotoxin, aseptic test, and radioactivity${\cdot}$ml-1. The record was fully recorded in 'appearance', 'radioactive heterokaryosis', 'pH', 'Endotoxin', and 'aseptic test'. In 'half-life', 'radiochemical Confirmation (measure of Rf value), 'radiochemical Purity', 'Ethanol', 'Acetonitrile', 'Kryptofix', 'Aluminium', 'radioactivity${\cdot}$ml-1', there were differences in records of each manufacturing business on radioactive medicine and medical supplies. The result of the test showed all 13 items of quality control test were 100% suitable on the basis of recorded data. There were more radiopharmaceutical made in the laboratory than in hospitals and businesses and in for result of suitability test, the laboratory showed higher suitability than did the hospitals or businesses. Domestically, there are differences of the test report items in the safety of radiopharmaceutical of each facility, and since it is not standardized, supplements are needed. To submit standardized test reports of quality guarantee in radiopharmaceutical, GMP of U.S. and CE Mark of Europe should be referred as well as receiving advice from professionals to standardize as suitable domestic standard.

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.3 no.2
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• pp.91-97
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• 2017

$^{18}F-THK-5351$ is a PET radiotracer to image the hyperphosphorylated tau fibrillar aggregates in human brain. This protocol describes the optimized radiosynthesis of $^{18}F-THK-5351$ using a commercial GE $TRACERlab^{TM}$ $FX_{FN}$ radiosynthesis module. $^{18}F-THK-5351$ was prepared by nucleophilic [$^{18}F$]fluorination from its protected tosylate precursors, (S)-(2-(2-methylaminopyrid-5-yl)-6-[[2-(tetrahydro-2H-pyran-2-yloxy)-3-tosyloxy]propoxy] quinolone(THK-5352), at $110^{\circ}C$ for 10 min in dimethyl sulfoxide, followed by deprotection with 1 N HCl. The average radiochemical yield of $^{18}F-THK-5351$ was $31.9{\pm}6.7%$(decay-corrected, n = 10), with molar activity of $198.1{\pm}33.9GBq/{\mu}mol$($5.4{\pm}0.9Ci/{\mu}mol$, n = 10). The radiochemical purity was determined to be above 98%. The overall production time including HPLC purification is approximately 70 min. This fully-automated protocol is validated for clinical use.