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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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

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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