干旱区生态环境知识资源中心(Arid): An improved preparation of [F-18]AV-45 by simplified solid-phase extraction purification

Arid

DOI	10.1002/jlcr.3813
	An improved preparation of [F-18]AV-45 by simplified solid-phase extraction purification
	Zhang, Lifang 1; Zhang, Aili 1; Yao, Xinyue 1,3; Zhang, Yan 1; Liu, Futao 1; Hong, Haiyan 1; Zha, Zhihao 2,3; Liu, Yajing 2; Wu, Zehui 2; Qiao, Jinping 1; Zhu, Lin 1,2; Kung, Hank F.2,3
通讯作者	Zhu, Lin ; Kung, Hank F.
来源期刊	JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
ISSN	0362-4803
EISSN	1099-1344
出版年	2020
卷号	63 期号:3 页码:108-118
英文摘要	Amyvid (florbetapir f18, [F-18]AV-45, [F-18]5) was the first FDA-approved positron emission tomography imaging agent targeting beta-amyloid (A beta) plaques for assisting the diagnosis of Alzheimer disease. This work aimed to improve the [F-18]AV-45 ([F-18]5) preparation by using solid-phase extraction (SPE) purification. [F-18]AV-45 ([F-18]5) was synthesized by direct nucleophilic radiofluorination of O-tosylated precursor (1 mg) at 120 degrees C in anhydrous dimethyl sulfoxide (DMSO), followed by acid hydrolysis of the N-Boc protecting group. Purification was accomplished by loading the crude reaction mixture to a cartridge (Oasis HLB 3 cc) and eluting with different combinations of solvents. This method removed the chemical impurity while leaving [F-18]AV-45 ([F-18]5) on the cartridge. The final dose was eluted by ethanol. [F-18]AV-45 ([F-18]5) was produced within 51 minutes (radiochemical yield 42.7 +/- 5.9%, decay corrected, n = 3), and the radiochemical purity was greater than 95%. Total chemical impurity per batch (24.1 +/- 2.7 mu g per batch) was below the limit described in the package insert of Amyvid, florbetapir f18 (chemical mass: less than 50 mu g/dose). In summary, [F-18]AV-45 ([F-18]5) was produced efficiently and reproducibly using a cartridge-based SPE purification. This method brings the process closer for routine preparation, similar to the commercially used [F-18]FDG.
英文关键词	automated radiosynthesis florbetapir f18 fluorine-18 solid-phase extraction purification
类型	Article
语种	英语
国家	Peoples R China ; USA
收录类别	SCI-E
WOS记录号	WOS:000510029200001
WOS关键词	POSITRON-EMISSION-TOMOGRAPHY ; MILD COGNITIVE IMPAIRMENT ; PET IMAGING AGENT ; RADIOSYNTHESIS ; DEPOSITION ; CARTRIDGE ; F-18
WOS类目	Biochemical Research Methods ; Chemistry, Medicinal ; Chemistry, Analytical
WOS研究方向	Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
EI主题词	2020-01-30
来源机构	北京师范大学
资源类型	期刊论文
条目标识符	http://119.78.100.177/qdio/handle/2XILL650/312628
作者单位	1.Beijing Normal Univ, Coll Chem, Key Lab Radiopharmaceut, Minist Educ, Beijing, Peoples R China; 2.Capital Med Univ, Beijing Inst Brain Disorders, Beijing, Peoples R China; 3.Univ Penn, Dept Radiol, 3700 Market St,Room 305, Philadelphia, PA 19104 USA
推荐引用方式 GB/T 7714	Zhang, Lifang,Zhang, Aili,Yao, Xinyue,et al. An improved preparation of [F-18]AV-45 by simplified solid-phase extraction purification[J]. 北京师范大学,2020,63(3):108-118.
APA	Zhang, Lifang.,Zhang, Aili.,Yao, Xinyue.,Zhang, Yan.,Liu, Futao.,...&Kung, Hank F..(2020).An improved preparation of [F-18]AV-45 by simplified solid-phase extraction purification.JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS,63(3),108-118.
MLA	Zhang, Lifang,et al."An improved preparation of [F-18]AV-45 by simplified solid-phase extraction purification".JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS 63.3(2020):108-118.