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Radiopharmaceutical for diagnostic imaging containing a technetium-99m nitride heterocomplex

a technology of nitride and radiopharmaceutical, which is applied in the field of radiopharmaceutical for diagnostic imaging containing a technetium-99m nitride heterocomplex, can solve the problem of difficult to obtain a single complex stoichiometrically having a specific physiologically active ligand, and achieve the effect of radioodiagnostic imaging

Inactive Publication Date: 2008-10-30
NIHON MEDI PHYSICS CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, it has been difficult to obtain a single complex stoichiometrically having a specific physiologically active ligand.

Method used

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  • Radiopharmaceutical for diagnostic imaging containing a technetium-99m nitride heterocomplex

Examples

Experimental program
Comparison scheme
Effect test

example 1

Synthesis of 99mTc(N) Heterocomplexes

[0081]99mTc(N) heterocomplexes were synthesized by the following three methods. The 99mTc(N) heterocomplexes could be similarly obtained by any of the methods and all of them had a radiochemical purity of 90 to 98% as determined by TLC.

Method 1:

[0082]0.250 mL of Na[99mTcO4] (50.0 MBq to 3.0 GBq) eluted from a 99Mo-99mTc generator was placed in a vial containing 5 mg of SDH, 5 mg of EDTA, SnCl2 (suspended in 0.1 mL of physiological saline) and 1 mL of ethanol. After the vial was kept at room temperature for 30 min. a solution of 1 mg of PNP3, PNP5 or PNP6 in 0.250 mL of ethanol was added thereto and the vial was heated at 100° C. for 15 minutes. A solution of 1.0 mg of each predetermined bidentate ligand in 0.1 mL of physiological saline was added thereto and then the vial was heated at 100° C. for 15 minutes. Thus, monocationic 99mTc(N) heterocomplexes were obtained. The radiochemical purity of these complexes was 94 to 98% as determined by TLC.

M...

example 2

Measurement of Log k′

Partition Ratio

[0086]For the various 99mTc(N) heterocomplexes synthesized using PNP3 as a bisphosphinoamine compound in Example 1, Log k′ values were determined at various compositions of a mobile phase for HPLC. As the mobile phase, mixtures of methanol and phosphate buffer (0.02M, pH=7.4) were used at a flow rate of 1.0 mL / min. For each sample, the retention time was measured at a minimum of three different methanol concentrations in the mobile phase. The Log k′ values at 0% organic solvent (Log k′0) were extrapolated from the linear part of the curve Log k′=a+bC, where C is the methanol concentration, and Log k′ is Log (tR−to) / to wherein tR is HPLC retention time (min). The column void time (t0) was regarded as being equal to the elution time of pertechnetic acid.

[0087]For the 99mTc(N) heterocomplex of DTC, partition coefficient Log P was determined. The HPLC conditions were as follows; A: CH3COONH4 (0.01 M, pH=5) 10%, B: CH3CN (THF 0.1%) 90%, C18, 0.5 mL / min...

example 3

Experiment for Confirming the Stability of the 99mTc (N) Heterocomplexes

[0088]The stability of the 99mTc(N) heterocomplexes obtained using PNP3 as a bisphosphinoamine compound in Example 1 was confirmed by ligand exchange reaction with cysteine or glutathione.

[0089]250.0 μL of phosphate buffer solution (0.20 M, pH=7.4), 100 μL of water and 100 μL of each of the 99mTc(N) heterocomplexes purified were mixed with 50 μL of each of cysteine solutions having different concentrations of 10 mM and 1.0 mM, and the resulting mixture was placed in a polypropylene test tube and incubated in a thermostat at 37° C. A blank solution was obtained by mixing an equal volume of water without addition of cysteine. Aliquots of the resulting solutions were withdrawn at 15 min, 30 min, 60 min and 2 hours after the start of the incubation, and analyzed by TLC. The same experiment as above was carried out except for using glutathione in place of cysteine. All the 99mTc(N) heterocomplex samples were found st...

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Abstract

A process for diagnostic imaging of heart or adrenal glands of a human being comprises administering to the human being a radiopharmaceutical containing as an active ingredient a technetium-99m nitride heterocomplex comprising technetium-99m nitride and two different ligands coordinated therewith, i.e., a bisphosphinoamine compound and a bidentate ligand and represented by the formula (1): [99mTc(N)(PNP)(XY)]+. In this formula, 99mTc(N) is technetium-99m nitride, PNP is a bisphosphinoamine compound and XY is a bidentate ligand as described in the specification. The compound of the formula is markedly accumulated in heart and adrenal glands and hence is used for radiodiagnostic imaging of heart and adrenal glands.

Description

CROSS REFERENCE TO RELATED APPLICATIONS[0001]This application is a divisional of U.S. application Ser. No. 10 / 332,707 filed on Sep. 4, 2003, which is a National Stage of International Application No. PCT / JP01 / 06402 filed on Jul. 25, 2001, the disclosures of all of which are hereby incorporated by reference.TECHNICAL FIELD[0002]The present invention relates to a radiopharmaceutical for diagnostic imaging containing a technetium-99m nitride heterocomplex as an active ingredient. More particularly, the present invention relates to a radiopharmaceutical for diagnostic imaging which contains as an active ingredient a technetium-99m nitride heterocomplex comprising technetium-99m nitride and two different ligands coordinated therewith, i.e., a diphosphine compound as a π n electron acceptor and a bidentate ligand as a π electron donor, and is suitable especially for radiodiagnostic imaging of heart and adrenal glands.BACKGROUND ART[0003]Of radioactive transition metals used in radiopharma...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K51/00A61K51/02A61K51/04
CPCA61K51/02A61K51/0476A61K51/04
Inventor DUATTI, ADRIANOBOLZATI, CRISTINAUCCELLI, LICIABOSCHI, ALESSANDRAREFOSCO, FIORENZOTISATO, FRANCESCO
Owner NIHON MEDI PHYSICS CO LTD
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