Studies on Preparation of $^{99m}Tc$ Labelled 3-Iodo-2,4,6-trimethyl-iminodiacetic acid $(^{99m}Tc-IOTIDA)$ for Diagnosis of Hepatobiliary Disease

간.담도계 질환 진단용 $^{99m}Tc$ 표지 3-요오도-2,4,6-트리메틸 이미노 2초산$(^{99m}Tc-IOTIDA)$의 제조에 관한 연구

  • Park, Kyung-Bae (Department, Korea Atomic Energy Research Institute) ;
  • Awh, Ok-Doo (Department, Korea Atomic Energy Research Institute) ;
  • Kim, Jae-Rok (Department, Korea Atomic Energy Research Institute)
  • 박경배 (한국원자력연구소 원자로동위원소실) ;
  • 오옥두 (한국원자력연구소 원자로동위원소실) ;
  • 김재록 (한국원자력연구소 원자로동위원소실)
  • Published : 1990.04.25

Abstract

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.

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