The Korean Journal of Nuclear Medicine (대한핵의학회지)

The Korean Society of Nuclear Medicine (대한핵의학회)
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Preparation and Animal Imaging of $^{153}Sm$-EDTMP as a Bone Seeking Radiopharmaceutical

골친화성 방사성의약품 $^{153}Sm$-EDTMP의 합성과 동물영상

  • Choi, Tae-Hyun (Laboratory of Nuclear Medicine, Korean Institute of Radiological & Medical Science) ;
  • Kim, Se-Jung (Hanaro Application Research, Korea Atomic Energy Research Institute) ;
  • Shin, Byung-Chul (Hanaro Application Research, Korea Atomic Energy Research Institute) ;
  • Woo, Kwang-Sun (Laboratory of Nuclear Medicine, Korean Institute of Radiological & Medical Science) ;
  • Chung, Wee-Sup (Laboratory of Nuclear Medicine, Korean Institute of Radiological & Medical Science) ;
  • Choi, Chang-Woon (Laboratory of Nuclear Medicine, Korean Institute of Radiological & Medical Science) ;
  • Lim, Sang-Moo (Laboratory of Nuclear Medicine, Korean Institute of Radiological & Medical Science)
  • 최태현 (원자력의학원 핵의학연구실) ;
  • 김세중 (한국원자력연구소 하나로이용연구단 동위원소이용연구부) ;
  • 신병철 (한국원자력연구소 하나로이용연구단 동위원소이용연구부) ;
  • 우광선 (원자력의학원 핵의학연구실) ;
  • 정위섭 (원자력의학원 핵의학연구실) ;
  • 최창운 (원자력의학원 핵의학연구실) ;
  • 임상무 (원자력의학원 핵의학연구실)
  • Published : 2005.02.28
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Abstract

Purpose: Ethylenediamine-tetramethylenephosphonic acid (EDTMP) has widely used chelator for the labeling of bone seeking radiopharmaceuticals complexed with radiometals. $^{153}Sm$ can be produced by the HANARO reactor at the Korea Atomic Energy Research Institute, Taejon, Korea. $^{153}Sm$ has favourable radiation characteristics $T1/2=46.7\;h,\;{\beta}_{max}=0.81\;MeV\;(20%),\;0.71\;MeV\;(49%),\;0.64\;MeV\;(30%)\;and\;{\gamma}=103\;keV\;(30%)$ emission which is suitable for imaging purposes during therapy. We investigated the labeling condition of $^{153}Sm$-EDTMP and imaging of $^{153}Sm$-EDTMP in normal rats. Materials and methods: EDTMP 20 mg was solved in 0.1 mL 2 M NaOH. $^{153}SmCl^3$ was added to EDTMP solution and pH of the reaction mixtures was adjusted to 3 and 12, respectively. Radiochemical purity was determined with paper chromatography. After 30 min. reaction, reaction mixtures were neutralized to pH 7.4, and the stability was estimated upto 120 hrs. Imaging studies of each reaction were perfomed in normal rats (37 MBq/0.1 mL). Results: The labeling yield of $^{153}Sm$-EDTMP was 99%. The stability of pH 8 reaction at 60, 96 and 120 hr was 99%, 95%, 89% and that of pH 12 at 36, 60, 96 and 120 hr was 99%, 95%, 88%, 66%, respectively. The $^{153}Sm$-EDTMP showed constantly higher bone uptake from 2 to 48 hr after injection. Conclusion: $^{153}Sm$-EDTMP, labeled at pH 8 reaction condition, has been stably maintained. Image of $^{153}Sm$-EDTMP at 2, 24, 48 hr after injection, demonstrate that $^{153}Sm$-EDTMP is a good bone seeking radiopharmaceuticals.

목적: Ethylenediamine-tetramethylenephosphonic acid (EDTMP)는 방사성 금속과 안정된 착화물을 형성하여 골친화성 방사성의약품으로 사용되고 있다. $^{153}Sm$은 원자력연구소의 하나로에서 생산가능하며, 물리적 반감기가 46.7시간이고 베타 최대에너지=0.81 MeV (20%), 0.71 MeV(49%), 0.64 MeV (30%)와 감마방출=103 KeV (30%)하여 치료와 영상이 동시에 가능한 방사성동위원소이다. $^{153}Sm$-EDTMP의 표지 조건과 정상 래트에서의 영상을 확인하고자 하였다. 방법: EDTMP 20 mg을 2 M NaOH 0.1 mL로 녹이고 $^{153}SmCl_3$를 넣어 pH 8 과 pH 12에서의 표지 수율과 안정성을 관찰하였다. 방사화학적 순도는 ITLC와 paper chromatography법으로 확인하였다. 반응 후, pH 7.4로 중화하고 실온 방치하며 안정성을 관찰하였다. 정상 래트에 $^{153}Sm$-EDTMP 37 MBq을 주사하여 평면영상을 얻었다. 결과: 표지 수율은 실온 반응 1시간에 99%를 나타내었다. pH 중화 후 안정성은 pH 8 반응물이 60시간 99%, 96시간 95%, 120시간 89%이였고 pH 12 반응물은 36시간 99%, 60시간 95%, 96시간 88%, 120시간 66%를 나타내었다. 정상래트에서의 평면영상은 주사 후 2시간, 24시간, 48시간에서 동일하게 뼈에 흡수 된 것을 관찰하였다. 결론: $^{153}Sm$-EDTMP는 pH 8에서 표지된 것이 pH 12 조건보다 안정하게 유지되었으며, 2시간, 24시간, 48시간 평면영상에서 골섭취되는 것을 관찰하여 생체 내에서 안정하게 유지됨을 확인할 수 있었다.

Keywords

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