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Bone-seeking 99mTc-IPrDP coordination compound as well as preparation method and application thereof

A complex, osteophilic technology, applied in the fields of radiopharmaceuticals and nuclear medicine, which can solve the problem of slow removal rate of non-targeted tissues

Inactive Publication Date: 2011-03-16
JIANGSU INST OF NUCLEAR MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0019] Zoledronic acid is currently the bisphosphonic acid with the best comprehensive curative effect, but there are also some shortcomings, such as the slow rate of non-targeted tissue clearance, and it can only be used clinically 2-3 hours after administration.

Method used

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  • Bone-seeking 99mTc-IPrDP coordination compound as well as preparation method and application thereof
  • Bone-seeking 99mTc-IPrDP coordination compound as well as preparation method and application thereof
  • Bone-seeking 99mTc-IPrDP coordination compound as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Technetium-99m-labeled 1-hydroxy-3-(1H-imidazol-1-yl)-propane-1,1-bisphosphonic acid complex ( 99m Tc-IPrDP) preparation and performance measurement.

[0036] 1) 99m Preparation of Tc-IPrDP

[0037] (a) Preparation of 1-hydroxy-3-(1H-imidazol-1-yl)-propane-1,1-bisphosphonic acid (IPrDP) ligand: using imidazole as raw material, the target new compound.

[0038]

[0039] The synthetic reaction route of IPrDP

[0040] Confirmation of the structure of the target IPrDP:

[0041] Melting point: the melting point of the product is 242-245°C;

[0042] Elemental analysis (C 6 h 12 N 2 o 7 P 2 ):

[0043] element

C

H

N

Calculated(%)

25.19

4.23

9.79

Measured value (%)

25.27

4.38

9.84

[0044] Mass spectrum (FAB): 285 (M-1);

[0045] Infrared (IR): 3148(v C-H ), 3500-2600 (v O-H ), 1603 (v C＝C ), 1337 (v C-N ), 1098 (v P＝O );

[0046] 1 H NMR spectrum ( 1 HNMR):

[0047]

[0048] ...

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Abstract

The invention relates to a bone-seeking 99mTc-IPrDP coordination compound, belonging to the fields of radiopharmaceuticals and nuclear medicine. The structural formula of the bone-seeking 99mTc-IPrDP coordination compound is shown in the specification. The preparation method of the coordination compound is as follows: mixing ligand IPrDP, reducing agent, pH buffer solution and pertechnetic acid (99mTcO<4->) solution to react to obtain an IPrDP coordination compound labeled by technetium-99m. The 99mTc-IPrDP coordination compound is used for nuclear medical diagnostic imaging. Through comparison, the product provided by the invention has the advantages of good product specificity, high bone / tissue intake (Am, bone) (% ID / g) and (Am, bone / Am, blood) and good tissue clearance rate, thus being expected to become novel bone imaging agent.

Description

technical field [0001] The invention relates to the field of radiopharmaceuticals and nuclear medicine, in particular to a technetium-99m labeled bisphosphonic acid complex, a preparation method and application thereof. Background technique [0002] 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. [0003] Bone scintigraphy is a common method for evaluating bone metabolic activity. 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 organic components in the bone tissue. When the bone is damaged, the bone in the lesion area can undergo two changes of osteogenesis or osteolysis depending on the a...

Claims

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Application Information

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IPC IPC(8): C07F19/00C07F13/00A61K51/04A61K103/10
Inventor 邱玲林建国程文罗世能王燕叶万忠
Owner JIANGSU INST OF NUCLEAR MEDICINE
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