• Title/Summary/Keyword: Radio isotope

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Synthesis of 14C-Radio Isotope Labeled Quinolone Intermediates

  • Shin, Hyun-Il;Kim, Young-Seok;Lee, Ki-Seung;Song, Sung-Geun;Ye, In-He;Ham, Won-Hun;Oh, Chang-Young
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.232.1-232.1
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    • 2002
  • Methods of 14C-radio isotope labeling of quinolone intermediates at four different sites are described. 14C-radio isotope labeled quinolone intermediates can be synthesized from 14C-1-malonic acid, 14C-2-malonic acid, 14C-benzene ring. and 14C-trimethyl orthoformate. The major site of 14C-radio isotope labeled quinolone intermediates is from 14C-2-malonic acid. We want to help customers to choose the best way for synthesis of 14C-radio isotope labeled quinolone derivatives. and give a general comprehension for 14C-radio isotope labeled pharmaceutical compounds. (omitted)

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Non-clinical Trials using 14C-Acetaminophen to Validate Biomedical Accelerator Mass Spectrometry System (14C-아세트아미노펜 비임상시험을 통한 생체시료 분석용 가속질량분석기의 검증)

  • Jinho Song;Jae Hoon Shim;Jung Bae Park;Chang Su Yeo;Soo Hyeon Bae;Min Sun Choi;Mi Hye Kwon;Kyeong Min Kim
    • Journal of Radiation Industry
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    • v.17 no.2
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    • pp.127-134
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    • 2023
  • Pharmacokinetic (PK) data provide pivotal information in drug development, and they are usually first studied in the preclinical stage using various animals. However, quite often, animal PK data may not match with human PK, especially in metabolites. Thus, most regulatory agencies in the world make it mandatory to obtain metabolite information using 14C radiolabeled drug in human for small molecule drug candidates. However, such studies are expensive and time consuming and they are usually done at the end of Phase II trials using ~3.7 MBq of 14C labeled drug in a limited number of human subjects. Introduction of accelerator mass spectrometry (AMS) in this kind of study has revolutionized it. Since AMS can measure 14C level as close as natural abundance, it can quantify the amounts of 14C labeled drugs and their metabolites produced in human body that consumes less than the amount of 0.0037 MBq of 14C labeled drug, a very safe level of radioactive dose in human. Therefore, it is now possible to conduct human 14C studies safely in early clinical trials without spending hefty amount of money and time. Korea Radioisotope Center for Pharmaceuticals(KRICP) at Korea Institute of Biological and Medical Sciences(KIRAMS) has established an AMS facility in 2018, housing a 0.5MV AMS manufactured at the US National Electrostatics Corps (NEC). The AMS instrument has been validated using various standard samples that have been prepared at Lawrence Livermore National Laboratory in the US, a worldly reputable provider of AMS standards. In this paper, we present a mass balance study for acetaminophen in rats using AMS and prove that the study results are equivalent with those of literature, which shows the AMS facilities at KRICP has successfully installed and be ready to be used in the various PK studies using 14C labelled compounds for new drug development.

[18F]FET PET is a useful tool for treatment evaluation and prognosis prediction of anti-angiogenic drug in an orthotopic glioblastoma mouse model

  • Kim, Ok-Sun;Park, Jang Woo;Lee, Eun Sang;Yoo, Ran Ji;Kim, Won-Il;Lee, Kyo Chul;Shim, Jae Hoon;Chung, Hye Kyung
    • Laboraroty Animal Research
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    • v.34 no.4
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    • pp.248-256
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    • 2018
  • O-2-$^{18}F$-fluoroethyl-l-tyrosine ($[^{18}F]FET$) has been widely used for glioblastomas (GBM) in clinical practice, although evaluation of its applicability in non-clinical research is still lacking. The objective of this study was to examine the value of $[^{18}F]FET$ for treatment evaluation and prognosis prediction of anti-angiogenic drug in an orthotopic mouse model of GBM. Human U87MG cells were implanted into nude mice and then bevacizumab, a representative anti-angiogenic drug, was administered. We monitored the effect of anti-angiogenic agents using multiple imaging modalities, including bioluminescence imaging (BLI), magnetic resonance imaging (MRI), and positron emission tomography-computed tomography (PET/CT). Among these imaging methods analyzed, only $[^{18}F]FET$ uptake showed a statistically significant decrease in the treatment group compared to the control group (P=0.02 and P=0.03 at 5 and 20 mg/kg, respectively). This indicates that $[^{18}F]FET$ PET is a sensitive method to monitor the response of GBM bearing mice to anti-angiogenic drug. Moreover, $[^{18}F]FET$ uptake was confirmed to be a significant parameter for predicting the prognosis of anti-angiogenic drug (P=0.041 and P=0.007, on Days 7 and 12, respectively, on Pearson's correlation; P=0.048 and P=0.030, on Days 7 and 12, respectively, on Cox regression analysis). However, results of BLI or MRI were not significantly associated with survival time. In conclusion, this study suggests that $[^{18}F]FET$ PET imaging is a pertinent imaging modality for sensitive monitoring and accurate prediction of treatment response to anti-angiogenic agents in an orthotopic model of GBM.

Simple measurement the chelator number of antibody conjugates by MALDI-TOF MS

  • Shin, Eunbi;Lee, Ji Woong;Lee, Kyo Chul;Shim, Jae Hoon;Cha, Sangwon;Kim, Jung Young
    • Journal of Radiopharmaceuticals and Molecular Probes
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    • v.3 no.2
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    • pp.54-58
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    • 2017
  • Matrix-assisted laser desorption/ionization time-of-flight mass spectrometry(MALDI-TOF MS) is one of the powerful methods that enable analysis of small molecules as well as large molecules up to about 500,000 Da without severe fragmentation. MALDI-TOF MS, thus, has been a very useful an analytical tool for the confirmation of synthetic molecules, probing PTMs, and identifying structures of a given protein. In recent nuclear medicine, MALDI-TOF MS liner ion mode helps researcher calculate the average number of chelator(or linkage) per an antibody conjugate, such as DOTA-(or DFO-) trastuzumab for labeling a medical radioisotope. This simple technique can be utilized to improve the labeling method and control the quality at the development of antibody-based radiopharmaceuticals, which is very effected to diagnosis and therapy for in vivo tumor cells, with radioisotopes like $^{89}Zr$, $^{64}Cu$, and 177Lu. To minimize the error, MALDI-TOF MS measurement is repeatedly performed for each sample in this study, and external calibration is carried out after data collection.

Flow Analysis for Fission Moly Target Cooling in HANARO (하나로 Fission Moly 표적 냉각에 대한 유동해석)

  • Park, Yong-Chul
    • 유체기계공업학회:학술대회논문집
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    • 2003.12a
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    • pp.502-507
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    • 2003
  • The HANARO, multi-purpose research reactor, 30 MWth open-tank-in-pool type, is under normal operation since it reached the initial critical in February 1995. The HANARO is used for fuel performance tests, radio isotope productions, reactor material performance tests, silicone semiconductor productions and etc. Specially, the HANARO is planning to produce a fission moly-99 of radio isotopes, a mother nuclide of Tc-99m, a medical isotope and is under developing a target handling tool for loading and unloading those at a flow tube (OR-5). The target should be sufficiently cooled in the flow tube without an interference with the cooling of the others and an induction of extremely vibration. This topic is described an analectic analysis for the cooling characteristics of the fission moly-99 target to find the minimum cooling water. It was confirmed through the analysis results that the minimum cooling water, about 2.717 kg/s flew through the flow tube under the worst case that the guide tube got no perforating holes for cooling water to pass through the holes and that the target was safely cooled under about seventy percent (70%) of the maximum allowable temperature of the target.

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RF heating experiment to verify the design process of graphite target at the RAON µSR facility

  • Jae Young Jeong;Jae Chang Kim;Kihong Pak;Yong Hyun Kim;Yong Kyun Kim;Wonjun Lee;Ju Hahn Lee;Taek Jin Jang
    • Nuclear Engineering and Technology
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    • v.55 no.10
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    • pp.3768-3774
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    • 2023
  • The purpose of the target system for the muon spin rotation, relaxation, and resonance (µSR) facility at the Rare isotope Accelerator complex for ON-line experiments (RAON) is to induce the production of a significant number of surface muons in thermally stable experiments. The manufactured target system was installed at RAON in the Sindong area near Daejeon in 2021. The design was made conservatively with a sufficient margin of safety through ANSYS calculations; however, verification experiments had to be performed on the ANSYS calculations. Because the 600-MeV proton beam has not yet been provided, an alternative way to reproduce the calculation conditions was required. The radio frequency (RF) heating method, which has not yet been applied to the target verification experiment but has several advantages, was used. It was observed that the RF heating method has promise for testing the thermal stability of the target, and whether the target system design process was performed conservatively enough was verified by comparing the RF heating experiments with the ANSYS calculations.

Various Shape of Carbon Layer on Ga2O3 Thin Film by Controlling Methane Fraction in Radio Frequency Plasma Chemical Vapor Deposition (Ga2O3박막 상에서의 RF 플라즈마 화학기상증착법의 메테인 분율 조절에 의한 탄소층의 다양한 형상 제어 연구)

  • Seo, Ji-Yeon;Shin, Yun-Ji;Jeong, Seong-Min;Kim, Tae-Gyu;Bae, Si-Young
    • Journal of the Korean Society for Heat Treatment
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    • v.35 no.2
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    • pp.51-56
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    • 2022
  • In this study, we controlled the shape of a carbon layer on gallium oxide templates. Gallium oxide layers were deposited on sapphire substrates using mist chemical vapor deposition. Subsequently, carbon layers were formed using radio frequency plasma chemical vapor deposition. Various shapes of carbon structures appeared according to the fraction of methane gas, used as a precursor. As methane gas concentration was adjusted from 1 to 100%, The shapes of carbon structures varied to diamonds, nanowalls, and spheres. The growth of carbon isotope structures on Ga2O3 templates will give rise to improving the electrical and thermal properties in the next-generation electronic applications.

A Study on Design of Transport Container for Radio-activated Targets (방사화 표적물질 운반용기 설계 연구)

  • Hey Min Park;Tae Young Kim;Hae Young Kim;Yang Soo Song;Un Jang Lee;Won-Je Cho;Myeong Hwan Jeong
    • Journal of Radiation Industry
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    • v.17 no.2
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    • pp.191-197
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    • 2023
  • Abstract KOMAC(Korea Multi-Purpose Accelerator Complex, KAERI) has been operating a 100 MeV proton accelerator and is going to produce 68Ga isotope which is useful for diagnosis of cancer. So, it is necessary to develop a transport container for radio-activated targets. In this study, we carry out shielding analysis and structural analysis for the radio-activated target transport container using simulation programs. According to the Type A standard, the transport container includes an inner container and an overpack container. The main material of inner container is lead, and the shape is cylindrical with diameter of 152mm, height of 142mm and weight about 29 kg. It is planned to verify the possibility of field application through production of the transport container prototype in the future.