Lee Yun-Sang, Jeong Jae Min, Kim Young Joo, Chang Young Soo, Lee Hak Jeong, Son Miwon, Lee Jung Woo, Yoon Heung Sik, Kang Won Jun, Lee Dong Soo, Chung June-Key, Lee Myung Chul, Suh Young-Ger
Department of Nuclear Medicine and Institute of Radiation Medicine, Seoul National University College of Medicine, 28 Yongon-dong, Jongno-gu, Seoul 110-744, Korea.
Appl Radiat Isot. 2007 Jan;65(1):64-9. doi: 10.1016/j.apradiso.2006.07.008. Epub 2006 Sep 28.
A lipiodol solution of (188)Re-4-hexadecyl-2,2,9,9-tetramethyl-4,7-diaza-1,10-decanedithiol ((188)Re-HDD/lipiodol) is in clinical study for liver cancer therapy. However, formulation of it is difficult due to highly active and unstable sulfhydryl groups. We produced new kits using diacetylated HDD (AHDD), in which sulfhydryl groups are protected. We found that AHDD kit can replace HDD kit due to an increased stability for formulation, the better radiolabeling efficiency (78%) and the equivalent biodistribution pattern in mice.
一种（188）Re-4-十六烷基-2,2,9,9-四甲基-4,7-二氮杂-1,10-癸二硫醇（（188）Re-HDD/碘油）的碘油溶液正在进行肝癌治疗的临床研究。然而，由于其巯基具有高活性和不稳定性，其制剂制备困难。我们使用二乙酰化的HDD（AHDD）制备了新的试剂盒，其中巯基得到了保护。我们发现，由于制剂稳定性提高、放射性标记效率更好（78%）以及在小鼠体内具有等效的生物分布模式，AHDD试剂盒可以替代HDD试剂盒。
