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Details for Patent: 4,247,534

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Details for Patent: 4,247,534

Title: Radiographic scanning agent
Abstract:A composition and method for the preparation of a technetium-99m-based scanning agent are disclosed. The scanning agent is prepared from .sup.99m Tc, in a +3, +4 and/or +5 oxidation state, and a methanehydroxydiphosphonate bone-seeking agent which carries the radionuclide to bone mineral. The methanehydroxydiphosphonate agent provides scan sharpness equivalent or superior to commercial scanning agents, and is superior for detecting myocardial infarcts, as compared with commercial scanning agents such as ethane-1-hydroxy-1,1-diphosphonate and methanediphosphonate.
Inventor(s): Bevan; John A. (Cincinnati, OH)
Assignee: The Procter & Gamble Company (Cincinnati, OH)
Filing Date:Jul 31, 1978
Application Number:05/929,472
Claims:1. A composition of matter for the preparation of a technetium-based bone mineral or infarct scanning agent, comprising:

(1) a water-soluble reducing agent for radioactive pertechnetate in an amount sufficient to reduce a unit dose of pertechnetate to a lower valence state; and

(2) a methanehydroxydiphosphonate bone material-seeking agent which is selected from methanehydroxydiphosphonic acid, and the water-soluble salts and esters thereof, in an amount sufficient to carry a unit dose of tri-, tetra-, or pentavalent radioactive technetium to bone mineral in the body of a human or lower animal with minimal absorption of technetium in uncalcified tissue and wherein said amount of methanehydroxydiphosphonic acid or water-soluble salt or ester thereof, sufficient to carry said unit dose is less than about 0.1 mg./kg. body weight of said human or lower animal.

2. A composition according to claim 1 wherein the reducing agent is selected from ferrous, chromous, titanous and stannous salts.

3. A composition according to claim 2 wherein the reducing agent is a stannous salt.

4. A composition according to claim 3 wherein the stannous salt is selected from stannous chloride, stannous sulfate, stannous tartrate and stannous maleate.

5. A composition according to claim 1 wherein the methanehydroxydiphosphonate bone mineral-seeking agent is selected from the alkali metal and ammonium salts of methanehydroxydiphosphonic acid.

6. A composition according to claim 1 which is in dry powder mix form.

7. A composition according to claim 1 which is in freeze-dried form.

8. A composition according to claim 1 which is in aqueous solution.

9. A composition according to claim 1 wherein the weight ratio of methanehydroxydiphosphonate bone mineral-seeking agent:reducing agent is in the range of from about 8:1 to about 30:1.

10. A composition according to claim 9 wherein the weight ratio of methanehydroxydiphosphonate bone mineral-seeking agent:reducing agent is in the range of about 10:1 to about 13:1.

11. A composition according to claim 10 wherein the reducing agent is a water-soluble stannous salt and the methanehydroxydiphosphonate bone mineral-seeking agent is a sodium salt of methanehydroxydiphosphonate.

12. A composition according to claim 9 which comprises: from about 0.1 mg. of about 0.5 mg. of a water-soluble stannous salt selected from stannous chloride, stannous sulfate, stannous maleate, and stannous tartrate; and from about 0.1 mg. to about 5 mg. of a sodium salt of methanehydroxydiphosphonate.

13. A composition according to claim 1 which contains, as an additional ingredient, a stabilizing, non-interfering amount of a water-soluble stabilizer.

14. A composition according to claim 13 wherein the stabilizer is selected from gentisic acid, and the water-soluble salts and esters thereof.

15. A composition according to claim 14 wherein the stabilizer is selected from gentisic acid and sodium gentisate.

16. A composition according to claim 13 wherein the stabilizer is selected from ascorbic acid, erythorbic acid, and the water-soluble salts and esters of ascorbic and erythorbic acid.

17. A composition according to claim 16 wherein the stabilizer is selected from ascorbic acid and sodium ascorbate.

18. A composition according to claim 13 wherein the weight ratio of methanehydroxydiphosphonate bone mineral-seeking agent:stabilizer is in the range from about 1:1 to about 20:1.

19. A composition according to claim 18 wherein the weight ratio of methanehydroxydiphosphonate bone mineral-seeking agent:stabilizer is in the range of about 3:1 to about 5:1.

20. A composition according to claim 13 wherein:

(1) the weight ratio of methanehydroxydiphosphonate bone mineral-seeking agent:stabilizer is in the range of from about 2:1 to about 20:1, and

(2) the weight ratio of methanehydroxydiphosphonate bone mineral-seeking agent:reducing agent is in the range of from about 8:1 to about 13:1.

21. A composition according to claim 20 wherein the methanehydroxydiphosphonate bone mineral-seeking agent is selected from methanehydroxydiphosphonic acid and the water-soluble alkali metal and ammonium salts thereof; the stabilizer is selected from gentisic acid, ascorbic acid, erythorbic acid, and the water-soluble alkali metal and ammonium salts thereof; and the reducing agent is selected from water-soluble stannous, chromous and ferrous salts.

22. A composition according to claim 21 comprising:

(1) from about 0.1 mg. to about 0.5 mg. of the stannous reducing agent;

(2) from about 0.25 mg. to about 1.0 mg. of the gentisate or ascorbate stabilizer; and

(3) from about 1 mg. to about 5 mg. of the methanehydroxydiphosphonate agent.

23. The composition of claim 1 in combination with radioactive technetium.

24. The composition of claim 13 in combination with radioactive technetium.

25. The composition of claim 20 in combination with radioactive technetium.

26. The composition of claim 21 in combination with radioactive technetium.

27. A method for imaging myocardial infarcts by administering to a patient in need of such treatment the composition of claim 1 or claim 13.
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