在镓-68放射性药物生产中使用4-(2-羟乙基)-1-哌嗪乙磺酸缓冲液——是时候重新考虑严格的药典限度了吗？
The use of HEPES-buffer in the production of gallium-68 radiopharmaceuticals - time to reconsider strict pharmacopoeial limits?
作者信息
le Roux Jannie, Kleynhans Janke, Rubow Sietske
机构信息
NuMeRI Node for Infection Imaging, Central Analytical Facilities, Stellenbosch University, Stellenbosch, South Africa.
Nuclear Medicine Division, Stellenbosch University, Stellenbosch, South Africa.
出版信息
EJNMMI Radiopharm Chem. 2021 Apr 1;6(1):15. doi: 10.1186/s41181-021-00129-w.
Abstract
HEPES (4-(2-hydroxyethyl) piperazine-1-ethanesulfonic acid) is a buffer that is used in the radiolabelling of gallium-68 compounds. The beneficial effects of HEPES on molar activity in bioconjugates have been well described. Current strict regulations on the HEPES content in radiopharmaceuticals limit its use when intended for parenteral administration.This short communication summarizes data from the literature on the toxicity of HEPES in dogs after intravenous infusion and the subsequent use in humans. We also highlight the use of HEPES in an FDA labelled intravenous drug formulation. Regulatory institutions may consider this data to review current strict limits.
摘要
HEPES（4-（2-羟乙基）哌嗪-1-乙磺酸）是一种用于镓-68化合物放射性标记的缓冲剂。HEPES对生物共轭物摩尔活性的有益作用已得到充分描述。目前对放射性药物中HEPES含量的严格规定限制了其用于肠胃外给药时的使用。本简短通讯总结了文献中关于静脉输注后HEPES在犬类中的毒性以及随后在人类中的使用的数据。我们还强调了HEPES在一种获得美国食品药品监督管理局（FDA）批准的静脉药物制剂中的应用。监管机构可考虑这些数据以审查当前的严格限制。
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