中华核医学与分子影像杂志
中華覈醫學與分子影像雜誌
중화핵의학여분자영상잡지
Chinese Journal of Nuclear Medicine and Molecular Imaging
2012年
4期
291-293
,共3页
虞燕华%陈志明%汪洋%吴二明%黄荷云
虞燕華%陳誌明%汪洋%吳二明%黃荷雲
우연화%진지명%왕양%오이명%황하운
亚锡依替菲宁%锝%肝%放射性核素显像
亞錫依替菲寧%锝%肝%放射性覈素顯像
아석의체비저%득%간%방사성핵소현상
Stannous chloride etifinine%Technetium%Liver%Radionuclide imaging
目的 对注射用亚锡依替菲宁的制备工艺进行改进,并将该药盒应用于临床.方法 将2,6-二乙基苯胺与氯乙酰氯经酰化反应得中间体氯乙酰(2,6-二乙基)苯胺,中间体与亚胺基二乙酸缩合反应生成(2,6-二乙基乙酰苯胺基)亚氨二乙酸(即依替菲宁).改变反应温度,并采用重结晶纯化方法以提高收率.40 mg依替菲宁与0.4 mg氯化亚锡制备得到药盒.依照《中华人民共和国药典》进行质量检测,检查药盒的性状、鉴别、澄明度、酸度、亚锡含量、依替菲宁含量、无菌情况、细菌内毒素.以99Tcm标记亚锡依替菲宁,检测标记物99Tcm的放化纯.观察99Tcm-依替菲宁临床显像效果.结果 合成的依替菲宁经红外光谱、氢谱、质谱等方法确证.红外光谱( KBr,cm-1):3308、3010、1706、1665、1535和1471;氢谱(CD3OD;相对位移,×10-6):1.16、2.57、3.62、3.67、7.11和7.20;质谱m/z:323(M+).成功制备注射用亚锡依替菲宁药盒.产品为白色粉末,易溶于水,加氯化钠溶液后澄清无色,pH值为4.6,细菌内毒素含量＜75内毒素单位(EU)/瓶.标记物99Tcm-依替菲宁经纸层析方法测定,其放化纯为96％,达到临床使用要求.患者显像肝胆图像清晰,表明该药可应用于肝胆疾病的诊断.结论 改进后的药盒制备方法合理可行,制备得到的药盒满足临床显像要求.
目的 對註射用亞錫依替菲寧的製備工藝進行改進,併將該藥盒應用于臨床.方法 將2,6-二乙基苯胺與氯乙酰氯經酰化反應得中間體氯乙酰(2,6-二乙基)苯胺,中間體與亞胺基二乙痠縮閤反應生成(2,6-二乙基乙酰苯胺基)亞氨二乙痠(即依替菲寧).改變反應溫度,併採用重結晶純化方法以提高收率.40 mg依替菲寧與0.4 mg氯化亞錫製備得到藥盒.依照《中華人民共和國藥典》進行質量檢測,檢查藥盒的性狀、鑒彆、澄明度、痠度、亞錫含量、依替菲寧含量、無菌情況、細菌內毒素.以99Tcm標記亞錫依替菲寧,檢測標記物99Tcm的放化純.觀察99Tcm-依替菲寧臨床顯像效果.結果 閤成的依替菲寧經紅外光譜、氫譜、質譜等方法確證.紅外光譜( KBr,cm-1):3308、3010、1706、1665、1535和1471;氫譜(CD3OD;相對位移,×10-6):1.16、2.57、3.62、3.67、7.11和7.20;質譜m/z:323(M+).成功製備註射用亞錫依替菲寧藥盒.產品為白色粉末,易溶于水,加氯化鈉溶液後澄清無色,pH值為4.6,細菌內毒素含量＜75內毒素單位(EU)/瓶.標記物99Tcm-依替菲寧經紙層析方法測定,其放化純為96％,達到臨床使用要求.患者顯像肝膽圖像清晰,錶明該藥可應用于肝膽疾病的診斷.結論 改進後的藥盒製備方法閤理可行,製備得到的藥盒滿足臨床顯像要求.
목적 대주사용아석의체비저적제비공예진행개진,병장해약합응용우림상.방법 장2,6-이을기분알여록을선록경선화반응득중간체록을선(2,6-이을기)분알,중간체여아알기이을산축합반응생성(2,6-이을기을선분알기)아안이을산(즉의체비저).개변반응온도,병채용중결정순화방법이제고수솔.40 mg의체비저여0.4 mg록화아석제비득도약합.의조《중화인민공화국약전》진행질량검측,검사약합적성상、감별、징명도、산도、아석함량、의체비저함량、무균정황、세균내독소.이99Tcm표기아석의체비저,검측표기물99Tcm적방화순.관찰99Tcm-의체비저림상현상효과.결과 합성적의체비저경홍외광보、경보、질보등방법학증.홍외광보( KBr,cm-1):3308、3010、1706、1665、1535화1471;경보(CD3OD;상대위이,×10-6):1.16、2.57、3.62、3.67、7.11화7.20;질보m/z:323(M+).성공제비주사용아석의체비저약합.산품위백색분말,역용우수,가록화납용액후징청무색,pH치위4.6,세균내독소함량＜75내독소단위(EU)/병.표기물99Tcm-의체비저경지층석방법측정,기방화순위96％,체도림상사용요구.환자현상간담도상청석,표명해약가응용우간담질병적진단.결론 개진후적약합제비방법합리가행,제비득도적약합만족림상현상요구.
Objective To improve the synthesis of etifenin and stannous chloride for injection in clinical practice.Methods N-chloracetyl-2,6-diethylaniline was obtained by reaction of chloroacetyl chloride with (2,6-diethyl) aniline.It was condensed by iminodiacetic acid to generate (2,6-diethylacetanilide) iminodiacetate (etifenin).The reaction temperature was changed and the product was recrystallized for purification.The ligand,40 mg etifenin,and the reducing agent,0.4 mg SnCl2,were reacted in the kit.Quality control analysis was performed according to the Chinese Pharmacopoeia.The radiochemical purity of the labeled compound,99Tcm-etifenin,and its use in hepatobiliary imaging was studied.Results The synthetic ligand was confirmed by infrared spectroscopy( IR),1 H-nuclear magnetic resonance ( NMR),mass spectroscopy (MS) and elemental analysis.IR peaks ( KBr,cm-1 ) were located at:3308,3010,1706,1665,1535,1471; 1H-NMR(CD3OD,ppm) peaks were:1.16,2.57,3.62,3.67,7.11,7.20;MS m/z was 323 ( M + ).The ligand and reducing agent were lyophilized to form a sterile nonpyrogenic kit.The quality satisfied the Chinese Pharmacopoeia standard,including the identity test,pH (4.6),tin content,etifenin content,sterile test and endotoxin test (the content was ＜75 endotoxin unit (EU)/bottle).The radiochemical purity of 99Tcm-etifenin was 96％.The hepatobiliary imaging by 99Tcm-etifenin was of high quality.Conclusion The modified synthesis of etifenin and stannous chloride for injection is simple and feasible.The improved etifenin and stannous chloride kit could be applied to clinical imaging.
