使用自制冻干乙二胺四甲叉膦酸（EDTMP）试剂盒制备的铥-乙二胺四甲叉膦酸（Tm-EDTMP）的放射化学研究、临床前研究及初步临床评估。
Radiochemical studies, pre-clinical investigation and preliminary clinical evaluation of Tm-EDTMP prepared using in-house freeze-dried EDTMP kit.
作者信息
Das Tapas, Shinto Ajit, Kamaleshwaran Koramadai K, Sarma Haladhar D, Mohammed Sahiralam Khan, Mitra Arpit, Lad Sangita, Rajan M G R, Banerjee Sharmila
机构信息
Radiopharmaceuticals Chemistry Section, Radiochemistry and Isotope Group, Bhabha Atomic Research Centre, Trombay, Mumbai 400085, India; Homi Bhabha National Institute, Anushaktinagar, Mumbai 400094, India.
Department of Nuclear Medicine & PET, Kovai Medical Centre and Hospital, Coimbatore, Tamil Nadu 641014, India.
出版信息
Appl Radiat Isot. 2017 Apr;122:7-13. doi: 10.1016/j.apradiso.2016.12.058. Epub 2017 Jan 5.
The objective of the present work is to formulate Tm-EDTMP using an in-house freeze-dried EDTMP kit and evaluate its potential as a bone pain palliation agent. Patient dose of Tm-EDTMP was prepared with high radiochemical purity using the lyophilized kit at room temperature within 15min. Pre-clinical evaluation in normal Wistar rats revealed selective skeletal accumulation with extended retention. Preliminary clinical investigation in 8 patients with disseminated skeletal metastases exhibited selective uptake in the bone and retention therein for a long duration.
本研究的目的是使用自制的冻干依替膦酸二钠（EDTMP）试剂盒制备钐-153依替膦酸二钠（Tm-EDTMP），并评估其作为骨痛缓解剂的潜力。使用冻干试剂盒在室温下15分钟内制备出具有高放射化学纯度的患者用Tm-EDTMP剂量。在正常Wistar大鼠中的临床前评估显示出选择性骨骼蓄积且滞留时间延长。对8例播散性骨转移患者的初步临床研究表明，其在骨骼中有选择性摄取并能长时间滞留。
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