• 대한방사성의약품학회지
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• 제3권1호
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• pp.38-43
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• 2017

Tc-99m labeled sestamibi ($^{99m}Tc$-MIBI) is one of most widely used radiopharmaceuticals for myocardial SPECT imaging. Radiolabeling of $^{99m}Tc$-MIBI is recommended by heating in $100^{\circ}C$ water bath for 15 min. However, the water bath might be a source of contamination. Thus, if radiolabeling of $^{99m}Tc$-sestamibi can be performed at room temperature, then it would be more convenient to use in clinical application. In this study, we performed the radiolabeling of $^{99m}Tc$-MIBI in different temperature conditions or using different instruments to find out the efficient labeling condition. We studied the $^{99m}Tc$-MIBI labeling at room temperature or $100^{\circ}C$ heating block, and checked the labelling yields every 1 min for 10 min using radio-TLC with 2 different eluents-saline and acetone. From the experiment, we confirmed that the $^{99m}Tc$-MIBI can be labeled over 90% yield but not completed at room temperature. However, the $^{99m}Tc$-MIBI labeling was completed when it was performed in the $100^{\circ}C$ heating block. Finally, we proved that heating is essential for complete $^{99m}Tc$-MIBI labelling, furthermore using heating block is also possible instead of water bath.

• 대한방사성의약품학회지
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• 제2권2호
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• pp.132-136
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• 2016

Radiolysis is the process of decreasing in Radio-Chemical Purity (RCP) of [$^{18}F$]FDG by direct effect and indirect effect of self Radio-activity. The objective of our study was to figure out the ideal conditions which minimize damages of quality of [$^{18}F$]FDG using radical scavenger and controlling temperature of storage.

• 핵의학기술
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• 제16권2호
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• pp.131-134
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• 2012

핵의학검사에서 방사성의약품의 표지효율은 검사의 정확성과 신뢰성 측면에서 중요하다. 보통 Brain SPECT검사에 사용되는 $^{99m}Tc$-HMPAO는 화학적으로 불안정하고 불순물의 발생이 많아 표지효율의 저하가 나타나기 쉽다. 이에 본 연구는 $^{99m}Tc$-HMPAO의 표지효율에 영향을 미치는 인자에 대한 실험을 통해 $^{99m}Tc$-HMPAO 표지 및 사용에 도움이 되고자 한다. Brain SPECT에 사용되는 국산 동아제약의 HMPAO vial을 대상으로 실험하였다. 삼영사의 generator 55.5 GBq (1,500 mCi)를 이용하였고, TLC 측정세트(ITLC-SG, butanone, saline, TLC chamber)와 Radio-TLC 스캐너(Bioscan, AR-2000)를 이용하였다. 첫 번째 실험은 generator에서 1, 8, 16, 24, 28시간 간격을 두고 용출한 $^{99m}Tc$-pertechnetate를 각각 HMPAO와 표지하여 표지효율을 측정하였다. 두 번째 실험은 generator에서 용출한 $^{99m}Tc$-pertechnetate를 0, 1, 3, 6시간경과에 따라 1.85GBq (50mCi)/1 ml를 취하여 HMPAO와 표지하여 표지효율을 측정하였다. 세 번째는 $^{99m}Tc$-HMPAO를 표지 후 0, 30분, 3시간, 5시간, 7시간이 경과했을 때 표지효율을 측정하였다. 첫 번째 실험에서 표지효율은 시간 순으로 95.05%, 94.64%, 94.94%, 95.64%, 96.76%로 나타났다. 두 번째 실험에서는 94.38%, 94.23%, 93.26%, 91.03%로 나타났다. 세 번째 실험에서는 95.76%, 94.17%, 88.19%, 83.6%, 76.86%로 나타났다. 첫 번째 실험에서 generator에서 24시간 후에용출한 $^{99m}Tc$-pertechnetate를 사용 한 표지효율은 비교적 높게 측정되었다. 추가실험을 통하여 임상에서의 사용 가능성에 대한 논의가 필요할 것으로 사료된다. 두 번째 실험에서 시간이 지날수록 표지효율은 다소 감소하였으나 6시간 이후에도 91% 이상으로 높게 측정되었다. 보충실험을 통하여 보완이 필요할 것으로 판단된다. 세 번째 실험에서 시간이 흐를수록 표지효율은 급격하게 감소하였다. 특히, 정확한 검사를 위해 표지후 3시간 이내에 사용하는 것이 좋다고 판단된다.

• 대한방사성의약품학회지
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• 제3권2호
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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.

• 대한방사성의약품학회지
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• 제4권2호
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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.

• 대한방사성의약품학회지
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• 제1권1호
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• pp.46-52
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• 2015

Herein we present the synthesis of $^{68}Ga$-labeled gold nanoparticles for in vivo PET imaging. A novel chelator DTPA-Cys was easily prepared from diethylenetriaminepentaacetic dianhydride in high yield. The ${\alpha}_v{\beta}_3$ integrin receptor targeted gold nanoparticle probe was synthesized by using DTPA-Cys, polyethylene glycol and cRGD peptide. $^{68}Ga$ labeling of cRGD conjugated gold nanoparticle was carried out at $40^{\circ}C$ for 30 min. Observed radiochemical yield was more than 75% as determined by radio-TLC and the probe was purified by centrifugation. In vitro stability test showed that 90% of $^{68}Ga$-labeled gold nanoparticle probe was stable in FBS for 1 h. Those results demonstrated that $^{68}Ga$-labeled gold nanoparticle could be used as a potentially useful probe for specific tumor imaging.

• Bulletin of the Korean Chemical Society
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• 제32권1호
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• pp.71-76
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• 2011

An efficient nucleophilic [$^{18}F$]fluorination has been studied to reduce byproducts and preparation time. Instead of conventional aqueous solution of $K_2CO_3-K_{222}$, several organic solution containing inert organic salts were used to release [$^{18}F$]fluoride ion and anion bases captured in the polymer cartridge, concluding that methanol solution is the best choice. Comparing to azeotropic drying process, one min was sufficient to remove methanol completely, resulting in about 10% radioactivity saving by reducing drying time. The polymer cartridge, Chromafix$^{(R)}$ (PS-$HCO_3$) was pretreated with several anion bases to displace pre-loaded bicarbonate base. Phosphate bases showed better results than carbonate bases in terms of lower basicity. tert-Butanol solvent used as a reaction media played another critical role in nucleophilic [18F]fluorination by suppressing eliminated side product. Consequent [$^{18}F$]fluorination under the present condition afforded fast preparation of reaction solution and high radiochemical yields (98% radio-TLC, 84% RCY) with 94% of precursor remained.

• 방사선산업학회지
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• 제5권4호
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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.

• 핵의학기술
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• 제16권1호
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• pp.8-11
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• 2012

상용화된 자동합성장치는 사용되는 유기용매의 종류가 다르고 합성수율에 차이를 보인다. 따라서 본 연구에서는 자동합성장치에 따른 $^{18}F$-FDG의 방사선분해에 관한 방사화학적순도 변화를 비교하였다. Cyclotron (PETtrace, GE Healthcare)을 사용하여 $^{18}F$를 생산하고, 자동합성장치(FASTlab, Tracerlab MX, GE Healthcare)를 이용하여 FDG로 합성하였다. 방사화화적순도는 Radio-TLC Scanner (AR 2000, Bioscan), GC(Gas Chromatography, Agilent 7890A)를 사용하여 $^{18}F$-FDG에 함유되어 있는 에탄올의 양을 측정하였다. 고정상은 실리카겔로 도포된 유리판($1{\times}10cm$), 이동상은 아세토니트릴과 물 19:1 혼합액을 사용하고, 각각의 합성장치에서 고농도와 저농도의 $^{18}F$-FDG를 생산 후 2시간 간격으로 방사화학적순도를 측정하였다. 저농도 (약 2.59 GBq/mL 이하)에서 순도변화는 Tracerlab MX에서는 99.26%, 98.69%, 98.25%, 98.09%, FASTlab에서는 99.09%, 97.83, 96.89%, 96.62%를 얻었다. 고농도(약 3.7 GBq/mL 이상)에서 순도변화는 Tracerlab MX에서는 평균 99.54%, 96.08%, 93.77%, 92.54%, FASTlab의 경우 99.53%, 95.65%, 92.39%, 89.82%를 얻었다. 그리고 FASTlab에서 생산한 $^{18}F$-FDG의 GC에서는 에탄올이 검출되지 않았으며, Tracerlab MX에서는 100~300 ppm의 에탄올이 검출되었다. 이러한 결과를 비추어 봤을 때 방사선 보호제인 에탄올의 유무보다 방사능농도가 방사선분해에 더 큰 영향을 미치기 때문에 고농도의 $^{18}F$-FDG 생산 후 무균 생리식염수로 희석하여 농도를 낮춘 후 사용해야 한다.

• 대한방사성의약품학회지
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• 제6권1호
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• pp.3-9
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• 2020

Tetraiodothyroacetic acid (tetrac) is a derivative of thyroid hormone T₄ and causes anti-angiogenesis by blocking T₄ binding to integrin α_vβ₃. In this study, we synthesized [^99mTc]Tc-Cys-Asp-Gly(CDG)-tetrac and evaluated it in vitro as a tumor angiogenesis imaging ligand. The CDG was conjugated to tetrac as a chelator for technetium-99m labeling. The cold vial containing CDG-tetrac, sodium glucoheptonate, and reducing agent was completed under nitrogen-filled atmospheric glove bag. [^99mTc]Tc-CDG-tetrac was synthesized in quantitative yield by heating the cold vial with [^99mTc]TcO₄^- at 100℃ for 30 min. In vitro serum stability of [^99mTc]Tc-CDG-tetrac was measured by incubating the radioligand in 50% fetal bovine serum at 37℃ and analyzing the incubation mixture by radio-TLC, which showed high stability over 6 h (≥ 98%). Cell binding study was carried out by incubating [^99mTc]Tc-CDG-tetrac with human umbilical vein endothelial (HUVE) cells at 37℃ for 6 h. The cell binding of the radioligand increased from 100% at 0.5 h to 293.7% at 6 h in a time-dependent manner. For blocking study, the cells were incubated with the radioligand in the presence of either tetrac (20 μM) or cRGDyK (20 μM) at 37℃ for 4 h. The results demonstrated that the cell binding of the radioligand was inhibited by tetrac (19.1%) or cRGDyK (35.6%), indicating specific binding of the radioligand to integrin α_vβ₃. Thus, this study suggests that [^99mTc]Tc-CDG-tetrac may be a potential radioligand for tumor angiogenesis imaging.