国产^(99)Tc^(m)-DTPA注射液的生物分布研究  

A Study on the Biological Distribution of Domestic ^(99)Tc^(m)-DTPA Injection

作　　者：张春丽[1] 贾娟娟[2] 施亚琴[2] 王玉琦 孙宏伟[1] 闫平[1] 王荣福[1] ZHANG Chunli;JIA Juanjuan;SHI Yaqin;WANG Yuqi;SUN Hongwei;YAN Ping;WANG Rongfu(Department of Nuclear Medicine,Peking University First Hospital.Beijing 100034,China;National Institutes for Food and Drug Control,Beijing 102629,China)

机构地区：[1]北京大学第一医院核医学科,北京100034 [2]中国食品药品检定研究院,北京102629

出　　处：《标记免疫分析与临床》2022年第10期1714-1718,1776,共6页Labeled Immunoassays and Clinical Medicine

基　　金：国家药典委员会药品标准制修订研究课题(编号:2019H01)。

摘　　要：目的建立锝[^(99m)Tc]喷替酸盐(^(99)Tc^(m)-DTPA)注射液的生物分布测定方法,测定国产^(99)Tc^(m)-DTPA注射液的生物分布,为《中国药典》“放射性药物质量标准”中^(99)Tc^(m)-DTPA注射液的生物分布测定项的制定提供方法学依据及参考值。方法测定测量仪器(CRC-55tR活度计与HRS-2000锝分析仪)的可检测范围。选择国内常用的3个厂家的DTPA药盒,采用^(99)Tc^(m)进行标记,得到^(99)Tc^(m)-DTPA注射液。将^(99)Tc^(m)-DTPA注射液经尾静脉注射于小鼠体内,测定注射后不同时间^(99)Tc^(m)-DTPA在小鼠血液、肾脏、肝脏、膀胱中的摄取值(%ID)。将不同剂量的^(99)Tc^(m)-DTPA注射液经尾静脉注射于小鼠体内,分别于注射后10~15min及24h测定小鼠体内的放射性活度,计算24h小鼠体内的残留率。评估测定结果及实验方法的可靠性。结果小鼠静脉注射740kBq(20μCi)的^(99)Tc^(m)-DTPA,肾脏、肝脏、血液、膀胱在注射后2min、15min、30min的放射性计数均在测量仪器的检出限以上,而24h血液和膀胱中的放射性计数低于测量仪器的检出限;静脉注射6.606~7.646 MBq(179~207μCi)后24h小鼠体内的放射性活度在测量仪器的检出限以上。静脉注射^(99)Tc^(m)-DTPA后2min肾脏的摄取率各药盒差异很大,15min与30min的差异减小,15min与30min肾脏的摄取率分别在2.10%ID~4.41%ID与1.65%ID~2.11%ID;24h小鼠体内残留率在1.635%~4.141%,符合美国药典(USP41)的标准。结论肾脏15min和30min的摄取率各厂家的药盒差异较小,可作为药盒质量标准;24h小鼠体内残留率测定的注射剂量在6.606~7.646MBq结果较为可靠,可选择≤5%作为质量标准。Objective To provide the methodological basis and to obtain the reference values of the biological distribution of ^(99)Tc^(m)-DTPA injection for the edition of Chinese Pharmacopoeias,the method to test the biological distribution of ^(99)Tc^(m)-DTPA injection was established and the biological distribution was measured.Methods The detectable ranges of the instruments used for testing the biological distribution were measured.DTPA kits from 3 domestic manufactures commonly used in the hospitals of our country were selected and labeled with ^(99)Tc^(m) to obtain ^(99)Tc^(m)-DTPA injection.^(99)Tc^(m)-DTPA injection was conducted as i.v.injection into mice and the uptake values(%ID)in blood,kidney,liver and bladder were measured at different time points during post-injection.Different doses of ^(99)Tc^(m)-DTPA injection were i.v.injected into mice and radioactivities of the mice at 10-15 min and 24 h were measured.The percentage of injected radioactivity retained 24 hours after administration(24 h retention)was calculated.The reliability of the method and the biological distribution data were evaluated.Results When 740 kBq(20μCi)^(99)Tc^(m)-DTPA was i.v.injected into mice,the radioactive counts for kidney,liver,blood and bladder at 2 min,15 min and 30 min were above the detectable limit,whereas the counts of blood and bladder at 24 h post-injection were under the detectable limit.The radioactivity of the mouse total body at 24h post-injection of 6.606-7.646 MBq(179-207μCi)^(99)Tc^(m)-DTPA injection was above the detectable limit.The kidney uptake had large variations among different kits at 2 min post-injection,but the differences were decreased at 15 min and 30 min.The kidney uptake was 2.10%ID-4.41%ID and 1.65%ID-2.11%ID at 15 min and 30 min post-injection,respectively.The 24 h retention was 1.635%-4.141%,which met the requirement of USP41.Conclusion Kidney uptake at 15 min and 30 min post-injection has a little variation among different kits and can be used as the reference standards.The 24h retention measured

关 键 词：锝[^(99)Tc^(m)]喷替酸盐 放射性药物 生物分布 肾脏摄取率 24h体内残留率 

分 类 号：R817-3[医药卫生—影像医学与核医学]