3,4,3-LI(1,2-HOPO)的表征、高效液相色谱法方法开发及杂质鉴定,3,4,3-LI(1,2-HOPO)是一种用于放射性核素促排的高效锕系元素螯合剂。
Characterization, HPLC method development and impurity identification for 3,4,3-LI(1,2-HOPO), a potent actinide chelator for radionuclide decorporation.
作者信息
Liu Mingtao, Wang Jennie, Wu Xiaogang, Wang Euphemia, Abergel Rebecca J, Shuh David K, Raymond Kenneth N, Liu Paul
机构信息
Pharmaceutical Development Department, Biosciences Division, SRI International, 333 Ravenswood Avenue, Menlo Park, CA 94025, United States.
Pharmaceutical Development Department, Biosciences Division, SRI International, 333 Ravenswood Avenue, Menlo Park, CA 94025, United States.
出版信息
J Pharm Biomed Anal. 2015 Jan;102:443-9. doi: 10.1016/j.jpba.2014.10.015. Epub 2014 Oct 22.
3,4,3-LI(1,2-HOPO), 1,5,10,14-tetra(1-hydroxy-2-pyridon-6-oyl)-1,5,10,14-tetraazatetradecane), is a potent octadentate chelator of actinides. It is being developed as a decorporation treatment for internal contamination with radionuclides. Conventional HPLC methods exhibited speciation peaks and bridging, likely attributable to the agent's complexation with residual metallic ions in the HPLC system. Derivatization of the target ligand in situ with Fe(III) chloride, however, provided a single homogeneous iron-complex that can readily be detected and analyzed by HPLC. The HPLC method used an Agilent Eclipse XDB-C18 column (150 mm × 4.6mm, 5 μm) at 25°C with UV detection at 280 nm. A gradient elution, with acetonitrile (11% to 100%)/buffer mobile phase, was developed for impurity profiling. The buffer consisted of 0.02% formic acid and 10mM ammonium formate at pH 4.6. An Agilent 1200 LC-6530 Q-TOF/MS system was employed to characterize the [Fe(III)-3,4,3-LI(1,2-HOPO)] derivative and impurities. The proposed HPLC method was validated for specificity, linearity (concentration range 0.13-0.35 mg/mL, r = 0.9999), accuracy (recovery 98.3-103.3%), precision (RSD ≤ 1.6%) and sensitivity (LOD 0.08 μg/mL). The LC/HRMS revealed that the derivative was a complex consisting of one 3,4,3-LI(1,2-HOPO) molecule, one hydroxide ligand, and two iron atoms. Impurities were also identified with LC/HRMS. The validated HPLC method was used in shelf-life evaluation studies which showed that the API remained unchanged for one year at 25°C/60% RH.
3,4,3-LI(1,2-HOPO),即1,5,10,14-四(1-羟基-2-吡啶酮-6-酰基)-1,5,10,14-四氮杂十四烷,是一种有效的锕系元素八齿螯合剂。它正被开发用于治疗放射性核素体内污染的促排治疗。传统的HPLC方法出现了物种峰和桥连现象,这可能归因于该试剂与HPLC系统中残留金属离子的络合。然而,用氯化铁对目标配体进行原位衍生化,得到了一种单一的均相铁络合物,可通过HPLC轻松检测和分析。HPLC方法使用安捷伦Eclipse XDB-C18柱(150 mm×4.6mm, 5μm),在25°C下,于280 nm处进行紫外检测。采用乙腈(11%至100%)/缓冲液流动相进行梯度洗脱,用于杂质分析。缓冲液由0.02%甲酸和10mM甲酸铵组成,pH值为4.6。使用安捷伦1200 LC-6530 Q-TOF/MS系统对[Fe(III)-3,4,3-LI(1,2-HOPO)]衍生物和杂质进行表征。所提出的HPLC方法在特异性、线性(浓度范围0.13 - 0.35 mg/mL,r = 0.9999)、准确度(回收率98.3 - 103.3%)、精密度(RSD≤1.6%)和灵敏度(LOD 0.08μg/mL)方面得到了验证。LC/HRMS显示该衍生物是一种由一个3,4,3-LI(1,2-HOPO)分子、一个氢氧根配体和两个铁原子组成的络合物。杂质也通过LC/HRMS进行了鉴定。经过验证的HPLC方法用于保质期评估研究,结果表明该原料药在25°C/60%RH条件下一年内保持不变。
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