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Claims for Patent: 4,208,398

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Claims for Patent: 4,208,398

Title: Technetium-labeled complexes, production and use thereof
Abstract:Novel chemical complexes containing a radioactive technetium isotope are kidney specific when the complexing agents are certain ionic, water-soluble mercaptans. The complexes can be made by reducing pertechnetate ion and reacting the reduced technetium species with the mercaptan. The complexes are normally used in a biologically sterile, substantially isotonic aqueous medium, for diagnostic purposes.
Inventor(s): Kubiatowicz; David O. (Arden Hills, MN), Bolles; Theodore F. (Woodbury, MN)
Assignee: Hoffman-La Roche Inc. (Nutley, NJ)
Application Number:05/570,254
Patent Claims: 1. A complex of Tc-99m with a compound of the group consisting of dimercaptosuccinic acid, mercaptosuccinic acid, mercaptoacetic acid, mercaptopropionic acid, 3-mercaptopropylsulfonic acid, thioglucose or thiolactic acid.

2. A complex according to claim 1, in which the complex contains from about 1 to 100 millicuries of Tc-99m for each milligram of complexing agent.

3. A composition comprising an isotonic solution of complexing agent according to claim 1 in a pharmaceutically acceptable parenteral diluent.

4. Composition according to claim 3, in which the parenteral diluent is sterile aqueous isotonic saline solution.

5. A complex according to claim 1, in which the complexing agent is dimercaptosuccinic acid.

6. A complex according to claim 1, in which the complexing agent is thioglucose.

7. A complex according to claim 1, in which the complexing agent is mercaptoacetic acid.

8. A complex according to claim 1, in which the complexing agent is 3-mercaptopropanoic acid.

9. A radiopharmaceutical complex of technetium-99m with a complexing agent selected from the group consisting of mercaptoacetic acid, dimercaptosuccinic acid, mercaptosuccinic acid and mercaptopropionic acid, said complex prepared in the presence of stannous chloride reducing agent.

10. The radiopharmaceutical complex of claim 9 wherein said agent is dimercaptosuccinic acid.

11. A radiopharmaceutical complex of technetium-99m with a complexing agent selected from the group consisting of mercaptoacetic acid, dimercaptosuccinic acid, mercaptosuccinic acid and mercaptopropionic acid, said complex prepared in the presence of a pharmaceutically-acceptable reducing agent for pertechnetate.

12. A radiopharmaceutical complex of reduced technetium-99m with a complexing agent selected from the group consisting of mercaptoacetic acid, dimercaptosuccinic acid and mercaptopropionic acid, wherein the technetium-99m is reduced by stannous chloride.

13. The radiopharmaceutical complex of claim 12 wherein said agent is dimercaptosuccinic acid.
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