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US4133872A
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Compositions for preparation of aqueous solutions of salts of lower valence 99 technetium
Assignee: Henkel AG and Co KGaA
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Filing: 1976-09-23
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Granted: 1979-01-09
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Expires: 1996-09-23
Abstract
Abstract Aqueous solutions of 99 technetium salts wherein the 99 technetium is in reduced valencey state, when administered to mammals, permit identification of the skeleton and of calcareous tumors by scintigraphy (radiographic scanning). The solutions are conveniently prepared by mixing one ore more phosphonic acids (or their salts) with one or more reducing salts, and adding the mixture to an aqueous solution of a pharmaceutically acceptable 99 pertechnetate salt. Reduction of the valence of the technetium occurs rapidly, and the resulting solution is adequately stable for use in scintigraphy. The phosphonic acid and reducing salt components can be premixed. Aqueous solutions of the premix are stable for long periods of time in the absence of free oxygen and the premix is stable to air so long as it is dry.
Inventors
- 👤 Manfred Schmidt-Dunker
- 👤 Wolfgang Greb
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-27 16:25
CPC Classifications
A; A61; A61K; A61K51/00; A61K51/02; A61K51/04; G; G21; G21H; G21H5/00; G21H5/02; A61K2123/00
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
157 words
A composition for use in the preparation of aqueous solutions containing 99m technetium for use in the detection by scintigraphy of bones and calcareous tumors, comprising: (A) one or more water-soluble carboxyphosphonic compounds having three carboxylic acid groups selected from the group consisting of compounds of the formula: ##STR4## wherein R represents a substituent selected from the group consisting of H and C 1-3 alkyl; R 1 represents a substituent selected from the group consisting of --PO 3 H 2 , and ##STR5## R 2 represents a substituent selected from the group consisting of ##STR6## with the proviso that when R 1 is --PO 3 H 2 , R 2 is other than H or C 1-3 alkyl; and the pharmaceutically-acceptable water-soluble salts of the above acids; and (B) a pharmaceutically acceptable water-soluble salt selected from the group consisting of tin (II), iron (II) or chromium (II) salts in less than stoichiometric quantities based on component (A).
Claim 2
Dependent Claim
157 words
A composition for use in the preparation of aqueous solutions containing 99m technetium for use in the detection by scintigraphy of bones and calcareous tumors, comprising: (A) one or more water-soluble carboxyphosphonic compounds having three carboxylic acid groups selected from the group consisting of compounds of the formula: ##STR4## wherein R represents a substituent selected from the group consisting of H and C 1-3 alkyl; R 1 represents a substituent selected from the group consisting of --PO 3 H 2 , and ##STR5## R 2 represents a substituent selected from the group consisting of ##STR6## with the proviso that when R 1 is --PO 3 H 2 , R 2 is other than H or C 1-3 alkyl; and the pharmaceutically-acceptable water-soluble salts of the above acids; and (B) a pharmaceutically acceptable water-soluble salt selected from the group consisting of tin (II), iron (II) or chromium (II) salts in less than stoichiometric quantities based on component (A).
Claim 3
Dependent Claim
22 words
A composition according to claim 1 wherein the weight of component (B) is 1% to 5% of the weight of component (A).
Claim 4
Dependent Claim
14 words
A composition according to claim 1 wherein the phosphonic compound is a partial salt.
Claim 5
Dependent Claim
25 words
A composition according to claim 1 wherein the phosphonic component comprises a material selected from the group consisting of 2-phosphono-butane-1,2,4-tricarboxylic acid and its trisodium salt.
Claim 6
Dependent Claim
13 words
A compound according to claim 1 wherein component (B) is tin (II) chloride.
Claim 7
Dependent Claim
11 words
A composition according to claim 1 in dry mix tableted form.
Claim 8
Dependent Claim
11 words
A composition according to claim 1 in sterile aqueous solution form.
Claim 9
Dependent Claim
30 words
A sterile aqueous solution of a composition according to claim 1 and a 99m technetate salt, substantially all the technetium content of said technetate having a valence less than 7.
Claim 10
Dependent Claim
58 words
A method of preparing a stable solution of a water-soluble salt of 99m technetium which is preferentially absorbed by bone and by calcareous tumors which comprises adding to an aqueous solution of a 99m pertechnetate salt a sufficient amount of a composition according to claim 1 to reduce the technetium in said pertechnetate salt to a lower valency.
Claim 11
Dependent Claim
19 words
A method according to claim 9 wherein said composition is added to said pertechnetate solution in dry tableted form.
Claim 12
Dependent Claim
64 words
A composition for use in the preparation of aqueous solutions containing 99m technetium for use in the detection by scintigraphy of bones and calcareous tumors, comprising (A) 2-phosphono-butane-1,2,4-tricarboxylic acid, and its pharmaceutically-acceptable water-soluble salts; and (B) a pharmaceutically acceptable water-soluble salt selected from the group consisting of tin (II), iron (II) or chromium (II) salts in less than stoichiometric quantities based on component (A).
Claim 13
Dependent Claim
64 words
A composition for use in the preparation of aqueous solutions containing 99m technetium for use in the detection by scintigraphy of bones and calcareous tumors, comprising (A) 2-phosphono-butane-1,2,4-tricarboxylic acid, and its pharmaceutically-acceptable water-soluble salts; and (B) a pharmaceutically acceptable water-soluble salt selected from the group consisting of tin (II), iron (II) or chromium (II) salts in less than stoichiometric quantities based on component (A).
Claim 14
Dependent Claim
22 words
A composition according to claim 11 wherein the weight of component (B) is 1% to 5% of the weight of component (A).
Claim 15
Independent Claim
196 words
A method of preparing a composition in unit dosage form for the detection by scintigraphy of bones and calcareous tumors by means of 99m technetium consisting essentially of (a) introducing into an ampoule under nitrogen or vacuum an aqueous solution of (A) one or more water-soluble carboxyphosphonic compounds having three carboxylic acid groups selected from the group consisting of compounds of the formula ##STR7## wherein R represents a substituent selected from the group consisting of H and C 1-3 alkyl; R 1 represents a substituent selected from the group consisting of --PO 3 H 2 , and ##STR8## R 2 represents a substituent selected from the group consisting of H, C 1-3 alkyl, --CH 2 --CHR--COOH, and ##STR9## with the proviso that when R 1 is --PO 3 H 2 , R 2 is other than H or C 1-3 alkyl; and the pharmaceutically-acceptable water-soluble salts of the above acids; and (B) a pharmaceutically acceptable water-soluble salt selected from the group consisting of tin (II), iron (II), or chromium (II) salts in less than stoichiometric quantities based on component (A), and (b) thereafter lyophilizing and sealing said aqueous solution in said ampoule under nitrogen or vacuum.
Claim 16
Independent Claim
196 words
A method of preparing a composition in unit dosage form for the detection by scintigraphy of bones and calcareous tumors by means of 99m technetium consisting essentially of (a) introducing into an ampoule under nitrogen or vacuum an aqueous solution of (A) one or more water-soluble carboxyphosphonic compounds having three carboxylic acid groups selected from the group consisting of compounds of the formula ##STR7## wherein R represents a substituent selected from the group consisting of H and C 1-3 alkyl; R 1 represents a substituent selected from the group consisting of --PO 3 H 2 , and ##STR8## R 2 represents a substituent selected from the group consisting of H, C 1-3 alkyl, --CH 2 --CHR--COOH, and ##STR9## with the proviso that when R 1 is --PO 3 H 2 , R 2 is other than H or C 1-3 alkyl; and the pharmaceutically-acceptable water-soluble salts of the above acids; and (B) a pharmaceutically acceptable water-soluble salt selected from the group consisting of tin (II), iron (II), or chromium (II) salts in less than stoichiometric quantities based on component (A), and (b) thereafter lyophilizing and sealing said aqueous solution in said ampoule under nitrogen or vacuum.
Claim 17
Independent Claim
196 words
A method of preparing a composition in unit dosage form for the detection by scintigraphy of bones and calcareous tumors by means of 99m technetium consisting essentially of (a) introducing into an ampoule under nitrogen or vacuum an aqueous isotonic solution of (A) one or more water-soluble carboxyphosphonic compounds having three carboxylic acid groups selected from the group consisting of compounds of the formula ##STR10## wherein R represents a substituent selected from the group consisting of H and C 1-3 alkyl; R 1 represents a substituent selected from the group consisting of --PO 3 H 2 , and ##STR11## R 2 represents a substituent selected from the group consisting of H, C 1-3 alkyl, --CH 2 --CHR--COOH, and ##STR12## with the proviso that when R 1 is --PO 3 H 2 , R 2 is other than H or C 1-3 alkyl; and the pharmaceutically-acceptable water-soluble salts of the above acids; and (B) a pharmaceutically acceptable water-soluble salt selected from the group consisting of tin (II), iron (II), or chromium (II) salts in less than stoichiometric quantities based on component (A), and (b) thereafter sealing said aqueous isotonic solution in said ampoule under nitrogen or vacuum.
Claim 18
Independent Claim
196 words
A method of preparing a composition in unit dosage form for the detection by scintigraphy of bones and calcareous tumors by means of 99m technetium consisting essentially of (a) introducing into an ampoule under nitrogen or vacuum an aqueous isotonic solution of (A) one or more water-soluble carboxyphosphonic compounds having three carboxylic acid groups selected from the group consisting of compounds of the formula ##STR10## wherein R represents a substituent selected from the group consisting of H and C 1-3 alkyl; R 1 represents a substituent selected from the group consisting of --PO 3 H 2 , and ##STR11## R 2 represents a substituent selected from the group consisting of H, C 1-3 alkyl, --CH 2 --CHR--COOH, and ##STR12## with the proviso that when R 1 is --PO 3 H 2 , R 2 is other than H or C 1-3 alkyl; and the pharmaceutically-acceptable water-soluble salts of the above acids; and (B) a pharmaceutically acceptable water-soluble salt selected from the group consisting of tin (II), iron (II), or chromium (II) salts in less than stoichiometric quantities based on component (A), and (b) thereafter sealing said aqueous isotonic solution in said ampoule under nitrogen or vacuum.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1982-01-08 | 1982-07-10 | 1983-01-09 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-01-08 | 1986-07-10 | 1987-01-09 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-01-08 | 1990-07-10 | 1991-01-09 | $7700.00 | Window Closed / Lapsed |