(羟基-膦酰甲基)膦酸锝 | 72945-61-0

• 分子结构分类: 有机化合物 - 有机酸及其衍生物
• 中文名称: (羟基-膦酰甲基)膦酸锝
• 英文名称: Technetium Tc 99m oxidronate
• 英文别名: [hydroxy(phosphono)methyl]phosphonic acid;technetium-99
• CAS: 72945-61-0
• 化学式: CH6O7P2Tc
• 分子量: 290.91
• InChiKey: SIJNDWFHVBDXDY-IEOVAKBOSA-N

物化性质

• 沸点：
  100ºC (reconstituted)
• 熔点：
  0ºC (reconstituted)
• 溶解度：
  Soluble

计算性质

• 辛醇/水分配系数(LogP)：
  -1.38
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  135
• 氢给体数：
  5
• 氢受体数：
  7

ADMET

代谢

锝 Tc-99m 氧化罗酸盐是一种双磷酸盐。有报道称双磷酸盐能够形成非常稳定的锝(IV)络合物，这使得它们在体内具有极高的稳定性以及非常低的降解率。

Technetium Tc-99m oxidronate is a diphosphonate. There have been reports showing that diphosphonates form very stable Tc(IV) complexes which provide them with a very high in vivo stability and a very low degradation.

来源:DrugBank

毒理性

• 在妊娠和哺乳期间的影响

哺乳期间使用总结：本记录中的信息指的是氧化锝酸99mTc复合物（Tc99m-羟基亚甲基二磷酸盐；Tc99m-HDP）作为诊断剂的使用。美国核能管理委员会的一个小组委员会建议，在给予所有锝Tc 99m诊断产品后，为了简化指导建议，应停止哺乳24小时，尽管这个时间间隔可能比必要的要长。其他来源指出，在给予哺乳母亲Tc 99m HDP后，不需要中断哺乳。然而，为了遵循将暴露“尽可能合理地降至最低”的原则，一些专家建议在给予放射性药物前哺乳婴儿，并在剂量后中断哺乳3到6小时，然后完全挤出一次乳汁并丢弃，或者储存至少60小时（10个半衰期）后再给婴儿。如果母亲在检查前已经挤出并储存了乳汁，她可以在哺乳中断期间用它喂养婴儿。 担心乳汁中放射性水平的母亲可以要求在医院核医学科进行检测。当放射性水平安全时，她可以恢复哺乳。已经发布了一种测量乳汁放射性并确定母亲可以安全恢复哺乳的时间的方法。 对于在工作场所接触Tc 99m物质的哺乳母亲，除了适当的辐射防护措施外，不需要采取任何预防措施。 ◉ 对哺乳婴儿的影响：截至修订日期，未找到相关已发布信息。 ◉ 对泌乳和乳汁的影响：截至修订日期，未找到相关已发布信息。

◉ Summary of Use during Lactation:Information in this record refers to the use of oxidronic acid 99mTc-complex (Tc99m-hydroxymethylene diphosphonate; Tc99m-HDP) as a diagnostic agent. A US Nuclear Regulatory Commission subcommittee has recommended that nursing be discontinued for 24 hours after administration of all technetium Tc 99m diagnostic products to simplify guidance recommendations, although this time interval may be longer than necessary. Other sources state that breastfeeding need not be interrupted after administration of Tc 99m HDP to nursing mothers. However, to follow the principle of keeping exposure "as low as reasonably achievable", some experts recommend nursing the infant just before administration of the radiopharmaceutical and interrupting breastfeeding for 3 to 6 hours after the dose, then expressing the milk completely once and discarding it or store it for at least 60 hours (10 half-lives) before giving it to the infant. If the mother has expressed and saved milk prior to the examination, she can feed it to the infant during the period of nursing interruption. Mothers concerned about the level of radioactivity in their milk could ask to have it tested at a nuclear medicine facility at their hospital. When the radioactivity is at a safe level, she may resume breastfeeding. A method for measuring milk radioactivity and determining the time when a mother can safely resume breastfeeding has been published. For nursing mothers who work with Tc 99m substances in their workplace, there is no need to take any precautions other than those appropriate for general radiation protection. ◉ Effects in Breastfed Infants:Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk:Relevant published information was not found as of the revision date.

来源:Drugs and Lactation Database (LactMed)

毒理性

• 蛋白质结合

蛋白质结合率在静脉给药2-3小时后报告为大约20-30%。

The protein binding has been reported to be around 20-30% after 2-3 hours of intravenous administration.

来源:DrugBank

吸收、分配和排泄

• 吸收

锝 Tc-99m 氧化镧盐可以迅速被吸收并从血液中清除，到达骨骼。静脉给药后27分钟，大约45-50%的锝 Tc-99m 氧化镧盐在骨骼中积累，在注射后1小时达到最大积累量，并在注射后72小时内保持恒定。

Technetium Tc-99m oxidronate is rapidly absorbed and cleared from blood plasma to reach the skeleton. After 27 min of intravenous administration, a range of 45-50% of the technetium Tc-99m oxidronate is accumulated in the skeleton, reaching maximum accumulation at 1-hour post injection and remaining constant until 72 hours postinjection.

来源:DrugBank

吸收、分配和排泄

• 消除途径

建议在注射锝Tc-99m氧化镝前完全排空膀胱。同样建议饮用大量水分，并尽可能频繁地排空膀胱，以减少膀胱壁的辐射暴露。血液中总放射性在5分钟到24小时之间分别从40%降至2.3%。24小时后，锝Tc-99m氧化镝的全身体内保留率为36.6%，这表明与其他骨放射性药物相比，这种药物的摄取量更大。锝Tc-99m氧化镝的肾小球滤过率在初始剂量后6小时可达到给药剂量的60%。24小时后，尿液中的累积活动量大约为59%，提示股骨与肌肉的比例为35。

It is recommended to empty bladder completely just prior to technetium Tc-99m oxidronate administration. It is as well recommended to drink abundant water and to empty bladder as often as possible to reduce radiation exposure in the bladder wall. The total radioactivity in blood between 5 min and 24 hours goes from 40% to 2.3% respectively. Technetium Tc-99m oxidronate whole body retention after 24 hours is a ratio of 36.6% which indicates that this drug, unlike other bone radiopharmaceuticals, presents a greater uptake. The glomerular filtration of technetium Tc-99m oxidronate can reach a 60% of the administered dose after 6 hours of the initial dose. The cumulative activity excreted in the urine after 24 hours is of approximately 59% suggesting a ratio of femur-to-muscle of 35.

来源:DrugBank

吸收、分配和排泄

• 分布容积

术后1小时technetium Tc-99m氧化锝的分布主要是骨骼，其次是肝脏和肾脏。

The distribution of technetium Tc-99m oxidronate at 1-hour post injection is mainly in the bones and secondary in the liver and kidneys.

来源:DrugBank

吸收、分配和排泄

• 清除

在给予锝Tc-99m氧化锶的前24小时内，观察到血液和非骨骼组织中迅速清除。剂量在骨骼和尿液中积累。

During the first 24 hours of technetium Tc-99m oxidronate administration, it is observed a rapid clearance from blood and non-osseous tissues. The dosage gets accumulated in skeleton and urine.

来源:DrugBank