^(223)RaCl_(2)注射液肌肉注射给药方法的建立及实用性与安全性评估  

Establishment of the Protocol of Intramuscular ^(223)RaCl_(2) Injection and the Corresponding Evaluation on Feasibility and Safety

作　　者：李晓红 左长京 李潇 LI Xiaohong;ZUO Changjing;LI Xiao(Department of Nuclear Medicine,First Affiliated Hospital of Naval Medical University,Shanghai 200433,China;Department of Applied Chemistry,Shanghai Institute of Applied Physics,Chinese Academy of Sciences,Shanghai 201800,China)

机构地区：[1]海军军医大学第一附属医院核医学科,上海200433 [2]中国科学院上海应用物理研究所应用化学技术部,上海201800

出　　处：《同位素》2023年第4期429-434,共6页Journal of Isotopes

基　　金：上海市卫生健康委先进适宜技术推广项目(2019SY029);海军军医大学第一附属医院“234学科攀峰计划”(2019YPT002)。

摘　　要：用于前列腺癌骨转移的^(223)RaCl_(2)注射液已经获得临床上市许可,并且获得较好的临床效果,但是在实际使用过程中存在部分缺陷待解决。改变药物给药途径是调节药代动力学的重要方式,本研究通过在大鼠右侧大腿肌肉注射的方式进行^(223)RaCl_(2)注射液的给药,通过SPECT/CT扫描动态记录该方案与经静脉注射方案在靶向效率及代谢清除方面的区别。结果表明,^(223)RaCl_(2)注射液经肌肉注射后12 h内完成注射点的药物扩散,经肌肉注射途径得到的骨沉积比在12 h后仍显著高于静脉注射组,且全身清除速率更快。在9 d观察期后,未观察到由^(223)RaCl_(2)注射液直接引起的皮肤灼伤或者血象改变,初步证明该方案的安全性。因此,在严格控制药物体积的条件下,^(223)RaCl_(2)注射液经肌肉注射可以提高药物骨沉积效率,避免部分副作用的发生。^(223)RaCl_(2) injection for bone metastasis of prostate cancer has been approved for clinical marketing and achieved good clinical effects.However,there are some defects to be solved in the actual use process.Changing the route of drug administration is an important way to regulate the metabolic distribution of drugs in vivo.In this study,^(223)RaCl_(2) injection was administered by intramuscular injection in the right thigh of rats.SPECT/CT scanning was used to dynamically record the differences in targeting efficiency and metabolic clearance between intramuscular protocol and intravenous protocol.The results showed that the drug diffusion of ^(223)RaCl_(2) injection at the injection site was completed within 12 hours after intramuscular injection,and the proportion of bone deposition obtained by intramuscular injection was significantly higher than that of intravenous injection group,while the systemic clearance rate was faster.After the completion of the 9 days observation period,no skin burns or blood changes directly caused by ^(223)RaCl_(2) injection were observed,preliminarily manifesting the safety of the protocol.Therefore,under the premise of strict control of drug volume,^(223)RaCl_(2) injection can improve the drug efficiency of bone deposition and avoid some side effects by intramuscular injection.

关 键 词：^(223)RaCl_(2)注射液 肌肉注射 骨沉积 前列腺癌 辐射损伤 

分 类 号：TL923[核科学技术—核燃料循环与材料]