快速制备99mTc(V) -DMSA用于肿瘤和转移显像的DMSA试剂盒的评价

U.P.S. Chauhan, A. Babbar, R. Kashyap, R. Prakash
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引用次数: 12

摘要

开发了一种快速制备99mTc(V) -DMSA的试剂盒。由DMSA、氯化亚锡和抗坏血酸按适当比例组成的冻干试剂盒,与0.2 mL 3.5% NaHCO3溶液和2-4 mL [99mTc]高技术酸盐混合,可制得优质的99mTc(V) -DMSA。用ITLC-SG在0.9%生理盐水中进行层析,在50 mM vernol缓冲液(pH 8.6)中进行水平纸电泳,电位梯度为15 V/cm,对放射性药物进行了表征,显示出与99mTc(III)-DMSA(一种已知的肾脏成像剂)不同的迁移率。与99mTc(III)-DMSA相比,新药物的血浆蛋白结合较少。五价DMSA在小鼠体内的生物分布表明,与三价DMSA相比,骨骼和肌肉的摄取更多,肝脏和肾脏的摄取更少。从C3H Jax小鼠的乳腺癌和患者的髓质癌的闪烁图可以明显看出软组织肿瘤的特异性和肿瘤闪烁图的适用性。一名乳腺癌患者在服用该药后也可见脑转移灶。
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Evaluation of a DMSA kit for instant preparation of 99mTc(V)—DMSA for tumour and metastasis scintigraphy

A kit has been developed to instantly prepare 99mTc(V)—DMSA. The freeze-dried kit consisting of DMSA, stannous chloride and ascorbic acid in appropriate proportions, produces quality 99mTc(V)—DMSA when mixed with 0.2 mL of 3.5% NaHCO3 solution and 2–4 mL of [99mTc] pertechnetate. The radiopharmaceutical characterized by chromatography with ITLC-SG in 0.9% saline and horizontal paper electrophoresis in 50 mM vernol buffer, pH 8.6, at a potential gradient of 15 V/cm showed a different mobility with respect to 99mTc(III)-DMSA, a known agent for kidney imaging. The new agent exhibited less plasma protein binding as compared to that of 99mTc(III)-DMSA. Biodistribution of the pentavalent DMSA in mouse demonstrated greater uptake in bone and muscle and lower uptake in liver and kidney with respect to trivalent DMSA. The soft tissue tumour specificity and its suitability for tumour scintigraphy was apparent from the scintigrams of mammary carcinoma in a C3H Jax mouse and medullary carcinoma in a patient. Brain metastatic lesions were also visible in a breast carcinoma patient after administering him with the agent.

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