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Technetium-99m labeled propyl zoledronic acid composition and preparation method thereof

A technology of -99m and complexes, applied in the field of radiopharmaceuticals and nuclear medicine, to achieve the effect of fast tissue clearance

Inactive Publication Date: 2010-04-14
JIANGSU INST OF NUCLEAR MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

We now performed bone imaging with technetium-99m-labeled 1-hydroxy-2-(2-propyl-1H-imidazol-1-yl)-ethane-1,1-bisphosphonic acid (PIDP) complex, and Compared with MDP and ZL labeled with technetium-99m, it was found that the bone tissue uptake (Am, bone) (%ID / g) and (Am, bone / Am, blood) of this product were higher than those of MDP reported in the literature. High, and the tissue clearance rate is significantly better than that of MDP and ZL, which has not been reported at home and abroad

Method used

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  • Technetium-99m labeled propyl zoledronic acid composition and preparation method thereof
  • Technetium-99m labeled propyl zoledronic acid composition and preparation method thereof
  • Technetium-99m labeled propyl zoledronic acid composition and preparation method thereof

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Embodiment 1

[0027] Technetium-99m-labeled 1-hydroxy-2-(2-propyl-1H-imidazol-1-yl)-ethane-1,1-bisphosphonic acid complex ( 99 Tc m -PIDP) preparation and performance measurement

[0028] 1) 99 Tc m - Preparation of PIDP

[0029] (a) Preparation of 1-hydroxyl-2-(2-propyl-1H-imidazol-1-yl)-ethane-1,1-diphosphonic acid (PIDP) ligand: 2-propylimidazole as raw material , according to the following three-step reaction to obtain the target new compound.

[0030]

[0031] Synthetic reaction route of PIDP

[0032] Melting point: The melting point of the product is 229-231°C.

[0033] Elemental analysis (C 8 h 16 N 2 o 7 P 2 )

[0034] C H N

[0035] Calculated value (%) 30.75 5.33 9.13

[0036] Actual value (%) 30.58 5.61 8.92

[0037] Mass Spectrum (FAB): 313 (M-1)

[0038] Infrared (IR): 3148(v C-H ), 3500-2600 (v O-H ), 1603 (v C＝C ), 1337 (v C-N ), 1098 (v P＝O )

[0039] 1 H NMR spectrum ( 1 HNMR):

[0040]

[0041] δ0.9, 3H (3Ha)

[0042] δ1.7, 2H ...

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Abstract

The invention relates to a technetium-99m labeled propyl zoledronic acid composition and a preparation method thereof, belonging to the fields of radiopharmaceuticals and nuclear medicines. The propyl zoledronic acid composition is technetium-99m labeled 1-hydroxy-2-(propyl-1H-iminazole-1-base)-ethane-1, 1-diphosphic acid (99Tcm-PIDP). The preparation method of the composition comprises the step of reacting the ligand PIDP, a reducing agent SnCI2.2H2O and a pH buffer solution with a pertechnetic acid (99TcmO4-) solution to obtain the technetium-99m labeled PIDP composition. The 99Tcm-PIDP is used for diagnostic imaging. The product of the 99Tcm-PIDP has higher bone tissue intake (Am, bone) (% ID / g) and (Am, bone / Am, blood) than a document value and rapid tissue removal speed, which shows that the product has the potential of being used as a bone developing agent.

Description

technical field [0001] A technetium-99m-labeled propylazoledbisphosphonic acid complex and a preparation method thereof, specifically relating to technetium-99m-labeled 1-hydroxyl-2-(2-propyl-1H-imidazol-1-yl)-ethyl The invention relates to an alkane-1,1-bisphosphonic acid (PIDP) complex and a preparation method thereof, belonging to the fields of radiopharmaceuticals and nuclear medicine. Background technique [0002] Bone scintigraphy is a common method for evaluating bone metabolic activity. Bone tissue is composed of inorganic salts, organic matter and water, and the main component of inorganic salts is hydroxyapatite [Ca 10 (PO 4 ) 6 (OH) 2 ] Crystals, accounting for 2 / 3 of the weight of the adult backbone; organic matter is mainly collagen fibers and bone mucin. The bone imaging agent may enter the bone tissue through two ways: one is to conduct ion exchange or chemical adsorption with the inorganic components in the bone tissue; the other is to combine with the o...

Claims

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Application Information

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IPC IPC(8): C07F13/00A61K51/04A61K103/10
Inventor 林建国罗世能邱玲陈传青王燕杨敏叶万忠
Owner JIANGSU INST OF NUCLEAR MEDICINE
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