COMPARISON OF ~(131)I-TYR~3-OCTREOTATE AND ~(131)I- DOTA-TYR~3-OCTREOTATE: THE EFFECT OF DOTA ON PHARMACOKINETICS AND STABILITY

摘要

The authors compared the biodistribution, and in vivo and in vitro stabilities of ~(131)I-Tyr~3-octreotate and ~(131)I-DOTA-Tyr~3-octreotate. The peptides were radioiodinated by the chloramine T method and high radiochemical yields were obtained (greater than 97%). Both labelled compounds showed high stability when incubated in human plasma at 37°C. The ~(131)I-Tyr~3-octreotate showed significant hepatic uptake and biliary excretion. The biodistribution of ~(131)I-DOTA-Tyr~3-octreotate, however, can be compared with the distribution of radiometal labelled octreotide analogues.