锝[^(99m)Tc]二巯丁二酸盐注射液的生物分布测定方法研究  

Biological Distribution of^(99m)Tc-DMSA Injection

作　　者：贾娟娟 孙葭北 张文在 孙得洋 施亚琴 黄海伟 JIA Juanjuan;SUN Jiabei;ZHANG Wenzai;SUN Deyang;SHI Yaqin;HUANG Haiwei(Institute for Chemical Drug Control,National Institutes for Food and Drug Control,Beijing 102629,China)

机构地区：[1]中国食品药品检定研究院化学药品检定所,北京102629

出　　处：《中国药物警戒》2025年第1期47-52,共6页Chinese Journal of Pharmacovigilance

基　　金：国家科技重大专项重大新药创制(2017ZX0910-1001);国家药典委员会药品标准制修订研究课题(2019H01)。

摘　　要：目的建立锝[^(99m)Tc]二巯丁二酸盐(^(99m)Tc-DMSA)注射液的生物分布测定方法,测定^(99m)Tc-DMSA注射液的生物分布,为该品种的质量评价提供方法学参考。方法考察生物分布测定所需仪器(放射性活度计、γ计数器)的测量范围及适用性。以大鼠为实验动物,采用2个企业的注射用亚锡二巯丁二钠(DMSA)药盒制备99mTc-DMSA注射液,考察注入剂量对生物分布的影响。比较不同企业相同剂量的99mTc-DMSA注射液在大鼠体内各脏器的摄取值,以考察不同企业的生物分布差异。结果放射性活度计的测量范围为≥1.6μCi;γ计数器测量的线性范围为400~3570000 CPM,对应的最大放射性活度为2.6μCi。注入剂量0.04 mCi~1.7 mCi的样品,生物分布无显著差异。采用建立的生物分布测定方法考察,结果显示2个企业的样品在大鼠体内的生物分布有差异,A企业药盒制备的^(99m)Tc-DMSA注射液在大鼠体内的代谢速度比B企业药盒快。注射1 h后,A制剂经尿液排出19.23%,B制剂排出10.29%;每克肾组织的摄取值也存在显著差异,分别为17.00%和26.95%。结论建立了锝[^(99m)Tc]二巯丁二酸盐注射液的生物分布测定方法,为该药品的质量评价及其他锝[^(99m)Tc]标记药物的质量评价提供参考。Objective To establish a biodistribution determination method for^(99m)Tc-DMSA injection,and measure the biological distribution of^(99m)Tc-DMSA injection in order to contribute to quality evaluation of this drug methodologically.Methods The measurement range and applicability of the instruments(dose calibrator andγcounter)required for biological distribution tests were examined.Using rats as experimental animals,^(99m)Tc-DMSA injection was prepared using DMSA kits from 2 manufacturers to examine the impact of the injection dose on biological distribution.The uptake values of the same dose of^(99m)Tc-DMSA injection from different manufacturers were compared in various organs of rats to study the differences in biological distribution between different manufacturers.Results The measurement range of the dose calibrator was≥1.6μCi.The linear range of theγcounter measurement was 400 to 3570000 CPM,which corresponded to a maximum radioactivity of 2.6μCi.There was no significant difference in biodistribution of samples injected with doses of 0.04 mCi to 1.7 mCi.Using the established biodistribution assay,the results showed differences in the biodistribution of the samples from 2 manufacturers in rats.The^(99m)Tc-DMSA injection prepared using the kit from manufacturer A was metabolized faster compared with manufacturer B in rats.One hour after injection,19.23%of preparation A and 10.29%of preparation B were excreted in urine.There was also a significant difference in the uptake values per gram of renal tissue,which were 17.00%and 26.95%,respectively.Conclusion A biological distribution method for^(99m)Tc-DMSA injection has been established that offers data for quality evaluation of this drug and sparks ideas for quality evaluation of other^(99m)Tc labeled drugs.

关 键 词：锝[^(99m)Tc]二巯丁二酸盐 注射液 肾显像 放射性药品 SD大鼠 生物分布 质量评价 

分 类 号：R965[医药卫生—药理学]