摘要
目的制备标记率>90%的 ^(99)Tc^m-2β-[N,N'-双(2-巯乙基)乙撑二胺基]-甲基-3β-(4-氯苯基)托烷(TRODAT-1)药盒,并研究药盒中各组分含量与 pH 值对其标记率的影响。方法按每支药盒含 TRODAT-1 50μg、SnCl_2·2H_2O 70 μg、EDTA-2Na 1.0 mg、Na_2HPO_4·12H_2O 17.6 mg,KH_2PO_42.37 mg 和葡庚糖酸钠(GH)10 mg 制备药盒,用上行薄层色谱法测定标记率;保持其他组分含量不变,分别改变 TRODAT-1、SnCl_2,EDTA-2Na 和 GH 的用量,并测定标记率;保持其他组分含量不变,调节 pH 缓冲剂的用量,使药盒在不同的 pH 值下标记,测定标记率。结果制备的药盒标记率>90%,稳定性好。药盒中各组分含量在下列范围内标记率>90%:TRODAT-1 20～200μg、SnCl_2 4～100μg、EDTA-2Na 0.5～2.0 mg、GH 1～20 mg、pH 值4.5～8.3。结论可成功制备标记率>90%的TRODAT-1药盒,其稳定性较好。
Objective To develop a kit formulation for preparing ^99Tc^m-2β-[N,N′-bis（2-mercaptoethyl） ethylenediamino ] methyl-3β- （4-chlorophenyl） tropane （ TRODAT-1 ） as a dopamine transporter imaging agent. Methods ^99Tc^m-TRODAT-1 kit was prepared by the following formulation： 50μg TRODAT-1, 70 μg SnCl2·2H2O, 1.0 mg EDTA-2Na, 17.64 mg Na2HPO4·12 H2O, 2.37mg KH2PO4 and 10 mg sodium glucoheptonate （GH）. Radiolabelling yield （or radiochemical purity） was determined by thin layer chromatograph （TLC）. A series of studies were performed to optimize labeling efficiency of ^99Tc^m-TRODAT-1 kit. ① Varying the amount of TRODAT-1, SnCl2·2H2O, EDTA-2Na and GH, labeling yield was measured by TLC. ② Varying the pH value, radiochemical purity was also determined by TLC. Results Labeling yield of ^99Tc^m-TRODAT-1 kit was over 90% （ n 〉 10）. The optimal amounts of each ingredient were ： TRODAT-1 20 ～ 200μg, SnCl2 4～100μg, EDTA-2Na 0.5～2.0 mg, GH 1～20 mg and pH 4.5～8.3. The kit was stable within 3 month when stored at 25℃ or 1 year at - 18℃ as evaluated by labeling yield. Conclusions ^99Tc^m-TRODAT-1 kit of new formulation was successfully prepared, labeling yield and radiochemical purity were all over 90% , with good stability.
出处
《中华核医学杂志》
CAS
CSCD
北大核心
2006年第4期235-237,共3页
Chinese Journal of Nuclear Medicine
基金
国家自然科学基金(30570518
39770230)
江苏省科技指导性计划项目(BS2003612)
江苏省卫生厅科研项目(H200401)
