US3985876A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Chemotherapeutic solutions containing a sulphur and a salt of a 2,4-diamino-5-benzylpyrimidine
Assignee: SmithKline Beecham Corp
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Filing: 1975-05-07
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Granted: 1976-10-12
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Expires: 1995-05-07
Abstract
Abstract A clear solution suitable for oral or parenteral chemotherapy of microbial, especially bacterial, infections containing a sulfonamide in an organic solvent and a mono acid addition salt of a sulfonamide potentiator (e.g. trimethoprim) in water, the solution having a pH in the range 2 to 7.
Inventors
- 👤 John R. Hazlett
- 👤 Elvin A. Holstius
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-03 13:41
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0012; A61K9/0019; A61K31/00; A61K31/63; A61K31/635; A61K47/00; A61K47/06; A61K47/08; A61K47/10; A61K47/16; A61K47/18; A61K47/20
Claims Analysis
Total Claims: 16
Claim 1
Independent Claim
127 words
A clear solution which includes 1 to 40 per cent (w/v) of sulfamethoxazole, 1 to 10 percent (w/v) of trimethoprim calculated as base in the form of a water soluble pharmaceutically acceptable acid addition mono salt, 10 to 60 percent water (v/v) and 30 to 90 percent (v/v) of a water miscible organic solvent for the sulfamethoxazole, the solution having a pH of 4.0 to 7.0, and a solution in which the organic solvent is selected from the class consisting of N, N-dimethylacetamide, polyethylene glycols having average molecular weights from about 190 to 7500 and containing 2 to 159 ethylene glycol monomer units, 1, 2-propylene glycol, glycerin, hexamethylene glycol, 1,3-butylene glycol, ethanol, diethylacetamide, dimethylsulfoxide, dimethylformamide, di 1,2-propylene glycol, glycerin formal, polyethylene-glycoethers of tetrahydrofurfuryl alcohol and diethylene glycol.
Claim 2
Dependent Claim
127 words
A clear solution which includes 1 to 40 per cent (w/v) of sulfamethoxazole, 1 to 10 percent (w/v) of trimethoprim calculated as base in the form of a water soluble pharmaceutically acceptable acid addition mono salt, 10 to 60 percent water (v/v) and 30 to 90 percent (v/v) of a water miscible organic solvent for the sulfamethoxazole, the solution having a pH of 4.0 to 7.0, and a solution in which the organic solvent is selected from the class consisting of N, N-dimethylacetamide, polyethylene glycols having average molecular weights from about 190 to 7500 and containing 2 to 159 ethylene glycol monomer units, 1, 2-propylene glycol, glycerin, hexamethylene glycol, 1,3-butylene glycol, ethanol, diethylacetamide, dimethylsulfoxide, dimethylformamide, di 1,2-propylene glycol, glycerin formal, polyethylene-glycoethers of tetrahydrofurfuryl alcohol and diethylene glycol.
Claim 3
Dependent Claim
14 words
A solution according to claim 1 in which the salt is the lactate salt.
Claim 4
Dependent Claim
19 words
A solution according to claim 1 wherein the ratio of sulfamethoxazole to trimethoprim as base is 20:1 to 0.1:1.
Claim 5
Dependent Claim
21 words
A solution according to claim 3 in which the solution contains from 0.5 to 3.5 percent of a pharmaceutically acceptable acid.
Claim 6
Dependent Claim
13 words
The solution of claim 1 which has a pH between 4 to 6.
Claim 7
Dependent Claim
13 words
The solution of claim 1 which has a pH of 4.5 to 5.5.
Claim 8
Dependent Claim
198 words
A clear solution for oral or parenteral use including (a) 1 to 40 per cent (w/v) of a sulphonamide selected from the group consisting of sulfadimethoxine, sulphadiazine, sulfadoxine, sulphadimethoxine, sulphamethoxazol, sulphaquinoxaline, sulphadimidine, sulfafurazole and sulfacetamide; (b) 30 to 90 percent (v/v) of a medicinally acceptable water miscible organic solvent for the sulphonamide, said organic solvent is selected from the class consisting of N,N-dimethylacetamide, polyethylene glycols having average molecular weights from about 190 to 7500 and containing 2 to 159 ethylene glycol monomer units, 1,2-propylene glycol, glycerin, hexamethylene glycol, 1,3-butylene glycol, ethanol, diethylacetamide, dimethylsulfoxide, dimethylformamide, di 1,2-propylene glycol, glycerin formal, polyethylene-glycoethers of tetrahydrofurfuryl alcohol and diethylene glycol; (c) 1 to 10 percent (w/v) of sulphonamide potentiator calculated as a base, in the form of a water soluble, pharmaceutically acceptable mono acid addition salt, said sulphonamide potentiator being of formula I ##SPC4## wherein R 1 is hydrogen or lower alkyl, wherein R 3 and R 4 are hydrogen, halogen, lower alkyl, lower alkoxy and wherein one or both R 5 and R 6 are halogen, lower alkyl and lower alkoxy; and (d) 10 to 60 percent water (v/v) said solution having a pH in the range of 2 to 7.
Claim 9
Dependent Claim
198 words
A clear solution for oral or parenteral use including (a) 1 to 40 per cent (w/v) of a sulphonamide selected from the group consisting of sulfadimethoxine, sulphadiazine, sulfadoxine, sulphadimethoxine, sulphamethoxazol, sulphaquinoxaline, sulphadimidine, sulfafurazole and sulfacetamide; (b) 30 to 90 percent (v/v) of a medicinally acceptable water miscible organic solvent for the sulphonamide, said organic solvent is selected from the class consisting of N,N-dimethylacetamide, polyethylene glycols having average molecular weights from about 190 to 7500 and containing 2 to 159 ethylene glycol monomer units, 1,2-propylene glycol, glycerin, hexamethylene glycol, 1,3-butylene glycol, ethanol, diethylacetamide, dimethylsulfoxide, dimethylformamide, di 1,2-propylene glycol, glycerin formal, polyethylene-glycoethers of tetrahydrofurfuryl alcohol and diethylene glycol; (c) 1 to 10 percent (w/v) of sulphonamide potentiator calculated as a base, in the form of a water soluble, pharmaceutically acceptable mono acid addition salt, said sulphonamide potentiator being of formula I ##SPC4## wherein R 1 is hydrogen or lower alkyl, wherein R 3 and R 4 are hydrogen, halogen, lower alkyl, lower alkoxy and wherein one or both R 5 and R 6 are halogen, lower alkyl and lower alkoxy; and (d) 10 to 60 percent water (v/v) said solution having a pH in the range of 2 to 7.
Claim 10
Dependent Claim
40 words
A solution as claimed in claim 7 wherein R 3 is hydrogen, and R 4 , R 5 and R 6 are the same or different and represent an alkyl or alkoxy group having from 1 to 4 carbon atoms.
Claim 11
Dependent Claim
46 words
A solution according to claim 7 in which the sulphonamide potentiator is represented by the formula: ##STR2## where R 1 , R 2 and R 3 are the same or different and can each represent alkyl or alkoxy groups having from 1 to 4 carbon atoms.
Claim 12
Dependent Claim
19 words
A solution according to claim 9 in which R 1 , R 2 , and R 3 are methoxy.
Claim 13
Dependent Claim
11 words
A solution according to claim 9 wherein the sulphonamide is sulfamethoxazole.
Claim 14
Dependent Claim
34 words
A solution according to claim 7 in which the sulphonamide is present in an effective antibacterial or antiprotozoal treatment amount and in which the sulphonamide potentiator is present in an effective sulphonamide potentiating amount.
Claim 15
Dependent Claim
36 words
A method of treating an animal or mammal suffering from bacterial or protazoal infections which comprises administering to said animal or mammal a therapeutically effective antibacterial or antiprotozoal treatment amount of the solution of claim 7.
Claim 16
Dependent Claim
17 words
A method according to claim 13 in which the sulphonamide is sulfamethoxazole and the potentiator is trimethoprim.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1979-10-12 | 1980-04-12 | 1980-10-12 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1983-10-12 | 1984-04-12 | 1984-10-12 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1987-10-12 | 1988-04-12 | 1988-10-12 | $7700.00 | Window Closed / Lapsed |