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US4031214A Expired / Lapsed US ⏱️ 0.0 years remaining

Sulphonamide and 2,4-diaminopyrimidine injectable suspension

Assignee: SmithKline Beecham Corp
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Filing: 1975-04-07
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Granted: 1977-06-21
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Expires: 1995-04-07
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Abstract

Abstract An injectable suspension of a sulphonamide/2,4-diaminopyrimidine combination formed utilizing a strong base and basic pH conditions which is suitable for the treatment of bacterial infections in mammals or birds.

Inventors

  • 👤 Michael George Easterbrook

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-03 19:03
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/63; A61K31/635

Claims Analysis

Total Claims: 18
Claim 1
Independent Claim 131 words
An aqueous injectable preparation which comprises a suspension of a finely divided potentiator of the formula ##STR3## wherein R 1 , R 2 , R 3 and R 4 are the same or different and can each be a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group or a benzyloxy group or, when R 1 , and R 2 are each hydrogen atoms, R 3 and R 4 taken together can be a methylene dioxy group substantially all of the particles of potentiator in the suspension having a largest dimension less than 50μ m, in an aqueous solution of a pharmaceutically acceptable water soluble salt of a sulphonamide with a strong base, and wherein the pH of the preparation is in the range of from 9.75 to 12.0.
Claim 2
Dependent Claim 131 words
An aqueous injectable preparation which comprises a suspension of a finely divided potentiator of the formula ##STR3## wherein R 1 , R 2 , R 3 and R 4 are the same or different and can each be a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group or a benzyloxy group or, when R 1 , and R 2 are each hydrogen atoms, R 3 and R 4 taken together can be a methylene dioxy group substantially all of the particles of potentiator in the suspension having a largest dimension less than 50μ m, in an aqueous solution of a pharmaceutically acceptable water soluble salt of a sulphonamide with a strong base, and wherein the pH of the preparation is in the range of from 9.75 to 12.0.
Claim 3
Dependent Claim 22 words
An aqueous injectable preparation as claimed in claim 1 wherein the pH of the preparation is equal to or greater than 10.
Claim 4
Dependent Claim 23 words
An aqueous injectable preparation as claimed in claim 1 wherein the pH of the preparation is in the range from 10 to 10.5.
Claim 5
Dependent Claim 83 words
An aqueous injectable preparation, as claimed in claim 1, which comprises a suspension of a finely divided potentiator selected from the group consisting of trimethoprim; diaveridine; 2,4-diamino-5-(3,4,6-trimethoxy benzyl)pyrimidine; 2,4-diamino-5-(4-chlorobenzyl)-6-ethylpyrimidine; ormetoprim; 2,4-diamino-5-(3,4-dimethoxy-5-bromobenzyl)pyrimidine and pyrimethamine, substantially all of the particles of the potentiator in the suspension having a largest diameter less than 50μ m, in an aqueous solution of a pharmaceutically acceptable water soluble salt of a sulphonamide selected from the group consisting of sulphadiazine; sulphadoxine; sulphadimethoxine, sulphamethoxazole; sulphaquinoxaline and sulphadimidine, with a strong base.
Claim 6
Dependent Claim 34 words
An aqueous injectable preparation as claimed in claim 1 wherein the sulphonamide is of general formula: ##STR4## wherein Q is a substituted or unsubstituted pyrimidin-2-yl or -4-yl group or is a substituted isoxazolyl group.
Claim 7
Dependent Claim 24 words
An aqueous injectable preparation as claimed in claim 1 wherein 90% of the particles by number have a largest dimension less than 20μ m.
Claim 8
Dependent Claim 26 words
An aqueous injectable preparation as claimed in claim 1 wherein at least 95% by number of the particles have a largest dimension less than 20μ m.
Claim 9
Dependent Claim 24 words
An aqueous injectable preparation as claimed in claim 1 wherein at least 99% of the particles have a largest dimension less than 20μ m.
Claim 10
Dependent Claim 24 words
An aqueous injectable preparation as claimed in claim 1 wherein at least 99.5% of the particles have a largest dimension less than 5μ m.
Claim 11
Dependent Claim 21 words
An aqueous injectable preparation as claimed in claim 1 wherein the pharmaceutically acceptable salt of the sulphonamide is a sodium salt.
Claim 12
Dependent Claim 23 words
An aqueous injectable preparation as claimed in claim 1 wherein the ratio of sulphonamide to potentiator by weight is from 20:1 to 0.1:1.
Claim 13
Dependent Claim 16 words
An aqueous injectable preparation as claimed in claim 1 containing up to 84% w/v of medicaments.
Claim 14
Dependent Claim 16 words
An aqueous injectable preparation as claimed in claim 1 which additionally contains a non-ionic wetting agent.
Claim 15
Dependent Claim 34 words
A method of treating bacterial infections in birds or mammals other than humans which comprises subcutaneously or intramuscularly injecting an effective dosage of the preparation claimed in claim 1 into the bird or mammal.
Claim 16
Dependent Claim 16 words
The preparation of claim 11 in which the potentiator is trimethoprim and the sulphonamide is sulphadoxine.
Claim 17
Dependent Claim 16 words
The preparation of claim 11 in which the potentiator is trimethoprim and the sulphonamide is sulphadiazine.
Claim 18
Dependent Claim 16 words
The preparation of claim 11 in which the potentiator is trimethoprim and the sulphonamide is sulphamethoxazole.

References Cited (Backward Citations)

US3551564A Cited
US3728452A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1980-06-20 1980-12-20 1981-06-21 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1984-06-20 1984-12-20 1985-06-21 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1988-06-20 1988-12-20 1989-06-21 $7700.00 Window Closed / Lapsed

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