Theodorakis M C, Groutas W C, Bermudez A J, Magnin D, Stefanakou S V
J Pharm Sci. 1980 May;69(5):581-4. doi: 10.1002/jps.2600690528.
Two radiopharmaceuticals, technetium 99m-N-(2-mercapto-1-oxopropyl)glycine (99mTc-I) and technetium 99m-ethylenediamine-N,N'-bis(alpha-2-hydroxy-5-bromophenyl)acetic acid (99MTc-II), were prepared and evaluated in dogs, rabbits, and rats. Both agents gave good scintigraphic images of the liver and gallbladder in dogs. The cumulative amount of 99mTc-I and 99mTc-II excreted in the bile of dogs and the physiological disposition data in rats revealed slight, inconclusive differences in their distributions. However, the scintigraphic images and physiological disposition data in rabbits revealed gross differences in the distribution pattern of the two agents. The observed similarities in the biliary excretion of both agents in dogs and rats were attributed to the fact that these species are relatively good biliary excretors, and both agents therefore were excreted extensively. However, rabbits, which are poor biliary excretors relative to dogs and rats, excreted 99mTc-II more extensively than 99mTc-I because of the favorable molecular characteristics of 99mTc-II.
制备了两种放射性药物，锝99m-N-(2-巯基-1-氧代丙基)甘氨酸(99mTc-I)和锝99m-乙二胺-N,N'-双(α-2-羟基-5-溴苯基)乙酸(99mTc-II)，并在犬、兔和大鼠身上进行了评估。两种药物在犬体内均能获得肝脏和胆囊的良好闪烁显像图。99mTc-I和99mTc-II在犬胆汁中的排泄累积量以及在大鼠体内的生理处置数据显示，它们在分布上存在轻微的、无定论的差异。然而，兔体内的闪烁显像图和生理处置数据显示这两种药物的分布模式存在显著差异。在犬和大鼠体内观察到两种药物胆汁排泄的相似性，原因是这些物种是相对较好的胆汁排泄者，因此两种药物都有广泛的排泄。然而，相对于犬和大鼠，兔是较差的胆汁排泄者，由于99mTc-II具有有利的分子特性，其排泄99mTc-II比99mTc-I更广泛。
