不同比活度11C-氟马西尼体内代谢的差异分析  

The metabolic analysis of 11C-flumazenil in different specific radioactivity

作　　者：张宗鹏 王治国 石庆学 张国旭 霍花 ZHANG Zongpeng;WANG Zhiguo;SHI Qingxue;ZHANG Guoxu;HUO Hua(Department of Nuclear Medicine,General Hospital of Northern Theater Command,Shenyang 110840,China;Institute of Drug Clinical Trial,General Hospital of Northern Theater Command,Shenyang 110840,China)

机构地区：[1]北部战区总医院核医学科,辽宁沈阳110840 [2]北部战区总医院药物临床试验机构办公室,辽宁沈阳110840

出　　处：《药学实践杂志》2020年第4期318-321,共4页Journal of Pharmaceutical Practice

基　　金：辽宁省自然科学基金项目(2019-ZD-1036)。

摘　　要：目的通过测定11C-氟马西尼(11C-flumazenil,11C-FMZ)在体内主要代谢物的百分占比,分析不同比活度11CFMZ的代谢差异。方法选取2019年5月至10月10名受试者,其中,男性5名,女性5名,平均年龄(41.7±4.7)岁,平均体重(69.3±6.8)kg。先后注射高低两种比活度(268.3±57.2)×10^3和(57.8±11.4)×10^3Ci/mol的11C-FMZ,并分别测定注射后1、2、3、4、5、10、15、20、30、40、60 min时血浆中11C-FMZ及其代谢物的百分注射剂量率,使用配对样本均数t检验计算并对比两组代谢物的百分占比。结果代谢物的百分占比随时间逐步增加,于15 min后基本趋于稳定,且低比活度组的百分占比明显高于高比活度组,在15~60 min的区间存在显著统计学差异(P<0.05)。结论不同比活度的11C-FMZ注射后的代谢率存在明显差异,临床应用时应尽量避免比活度差异过大。Objective To analyze the metabolic differences of 11C-flumazenil(11C-FMZ) with different specific radioactivity by detecting the percentage proportion of the main metabolites in vivo. Methods 5 male and 5 female volunteers with average age of(41.7±4.7) years and weight of(69.3±6.8) kg were selected from May to October 2019. 11C-FMZ with high and low specific radioactivity(268.3±57.2)×10^3 and(57.8±11.4)×10^3 Ci/mol was injected successively. The percentage of injected dose/liter of 11C-FMZ and its metabolites in the plasma at 1, 2, 3, 4, 5, 10, 15, 20, 30, 40 and 60 min after the injection was measured. Paired sample mean t test was used to calculate and compare the percentage of metabolites in the two groups. Results The percentage proportion of metabolites increased gradually with time, and reached the stable level after 15 min. The percentage proportion of low specific radioactivity group was higher than that of high specific radioactivity group with a significant statistical difference between 15 min and 60 min(P<0.05). Conclusion The metabolic rate of 11C-FMZ with different specific radioactivity was significantly different after injection and the specific radioactivity difference should be avoided if possible in clinical application.

关 键 词：11C-氟马西尼 羧酸代谢物 放射性比活度 

分 类 号：TQ421.7[化学工程]