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Claims for Patent: 5,384,113

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Claims for Patent: 5,384,113

Title: Stabilizers to prevent autoradiolysis of radiolabeled peptides and proteins
Abstract:Gentisic acid and its derivatives substantially inhibit peptide autoradiolysis. Gentisic acid or its derivatives may also be used in combination with other stabilizers such as inositol and ascorbic acid to inhibit autoradiolysis of radiolabeled peptides.
Inventor(s): Deutsch; Edward A. (Maryland Heights, MO), Goedemans; Wilhelmus T. (Bergen, NL), Maria de Jong; Martinus T. (Hoogkarspel, NL), Miller; Kathleen M. (St. Louis, MO), Brodack; James W. (Florissant, MO)
Assignee: Mallinckrodt Medical, Inc. (St. Louis, MO)
Application Number:08/135,882
Patent Claims: 1. A method of preventing autoradiolysis of radiolabeled peptides by including a stabilizer selected from the group consisting of gentisic acid, genetisyl alcohol and water soluble salts, esters, and mixtures thereof in a pharmaceutically acceptable carrier containing a biologically active peptide radiolabeled with a radionuclide selected from the group consisting of .sup.111 In, .sup.67 Ga, .sup.169 Yb, .sup.125 I, .sup.123 I, and .sup.201 Tl, wherein said stabilizer is present in an amount effective to prevent autoradiolysis of the radiolabeled biologically active peptide.

2. A method of preventing autoradiolysis of radiolabeled peptides as defined in claim 1, wherein the radiolabeled biologically active peptide is labeled with a radionuclide by use of a bifunctional chelate.

3. A method of preventing autoradiolysis of radiolabeled peptides as defined in claim 1, wherein the radiolabeled biologically active peptide is labeled with a radionuclide by direct labeling of the peptide.

4. A method of preventing autoradiolysis of radiolabeled peptides as defined in claim 1, wherein the pharmaceutically acceptable carrier further comprises a second stabilizer.

5. A method of preventing autoradiolysis of radiolabeled peptides as defined in claim 4, wherein the second stabilizer includes inositol.

6. A method of preventing autoradiolysis of radiolabeled peptides as defined in claim 4, wherein the second stabilizer includes ascorbic acid.

7. A method of preventing autoradiolysis of radiolabeled peptides as defined in claim 1, wherein the pharmaceutically acceptable carrier contains a buffer.

8. A method of preventing autoradiolysis of radiolabeled peptides as defined in claim 1, wherein the radionuclide is .sup.111 In.

9. A method of preventing autoradiolysis of radiolabeled peptides as defined in claim 8, wherein the peptide is octreotide.

10. A method of preventing autoradiolysis of radiolabeled proteins by including a stabilizer selected from the group consisting of gentisic acid, gentisyl alcohol and water soluble salts, esters, and mixtures thereof in a pharmaceutically acceptable carrier containing a biologically active protein radiolabeled with a radionuclide selected from the group consisting of .sup.111 In, .sup.67 Ga, .sup.169 Yb, .sup.125 I, .sup.123 I, and .sup.201 Tl, wherein said stabilizer is present in an amount effective to prevent autoradiolysis of the radiolabeled biologically active protein.

11. A method of preventing autoradiolysis of radiolabeled proteins as defined in claim 10, wherein the radiolabeled biologically active protein is labeled with a radionuclide by use of a bifunctional chelate.

12. A method of preventing autoradiolysis of radiolabeled proteins as defined in claim 10, wherein the radiolabeled biologically active protein is labeled with a radionuclide by direct labeling of the protein.

13. A method of preventing autoradiolysis of radiolabeled proteins as defined in claim 10, wherein the pharmaceutically acceptable carrier contains a buffer.

14. A method of preventing autoradiolysis of radiolabeled proteins as defined in claim 10, wherein the radionuclide is .sup.111 In.

15. A composition for preparing a radiolabeled octreotide preparation stable to autoradiolysis comprising:

a quantity of DTPA-octreotide, wherein the DTPA-octreotide is labeled with .sup.111 In; and

a stabilizer selected from the group consisting of gentisic acid, gentisyl alcohol, and the water soluble salts, esters, derivatives, and mixtures thereof.

16. A composition as defined in claim 15, further comprising a second stabilizer.

17. A composition as defined in claim 16, wherein the second stabilizer includes inositol.

18. A composition as defined in claim 16, wherein the second stabilizer includes ascorbic acid.

19. A composition as defined in claim 16, further comprising a buffer.

20. A composition as defined in claim 19, wherein the composition is in the form of a lyophilized kit.

21. A composition as defined in claim 15, wherein the composition is a liquid formulation.
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