GB2082063A - Antibacterial drug - Google Patents

Antibacterial drug Download PDF

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Publication number
GB2082063A
GB2082063A GB8125077A GB8125077A GB2082063A GB 2082063 A GB2082063 A GB 2082063A GB 8125077 A GB8125077 A GB 8125077A GB 8125077 A GB8125077 A GB 8125077A GB 2082063 A GB2082063 A GB 2082063A
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GB
United Kingdom
Prior art keywords
drug
antibacterial
dapsone
trimethoprim
inhibition
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
GB8125077A
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Individual
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Individual
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Publication date
Application filed by Individual filed Critical Individual
Priority to GB8125077A priority Critical patent/GB2082063A/en
Publication of GB2082063A publication Critical patent/GB2082063A/en
Withdrawn legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/63—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

In a drug formulation which contains a "sulphone" and a pyrimidine, a synergistic effect results in mutual potentiation of the antibacterial activity of the components. The preferred "sulphone" is thiambutosine, clofazimine, solapsone or dapsone and the pyrimidine is preferably trimethoprim.

Description

SPECIFICATION Antibacterial drug This invention relates to an antibacterial drug.
This invention provides a drug combination of known antibacterial drugs which act synergistically resulting in mutual potentiation of the antibacterial activities of the individual components of the com bination.
According to the present invention there is pro vided an antibacterial drug comprising a synergistic mixture of a sulphone and a pyrimidine derivative, each having antibacterial activity.
The sulphone may be dapsone, thiambutosine, clofazimine or solapsone and of these the most pref erable is dapsone. The most preferred pyrimidine based antibacterial is trimethoprim.
The preferred weight ratio of sulphone to pyrimidine derivative is from 100:1 to 5:1. However, advantage may still be observed at ratios of 500:1 to 1:100.
The antibacterial drug ofthis invention is effective against gram-positive and gram-negative microor ganisms.
The drug may be administered parenterally by intramammary or intramuscular injection or orally in the form of tablets, solutions or emulsions.
The main envisaged area of application is in the treatment of bacterial infection in cattle.
A preferred solution for intramuscular injection is as follows: Dapsone 209 Trimethoprim 49 Dimethylacetamide 50ml Water 20ml Benzyl Alcohol 1ml Propylene glycol to 100ml A preferred formulation for intramammary injection is as follows: Dapson 19 Trimethoprim 0.2g Paraffin base to 5g The potentiation of the drug combination of the invention against staphylococcus aureus is evidenced by the following results which were obtained using a zone inhibition measurement as indication of activity.Dapsone alone at a concentration of 0.05% produced no detectable inhibition, trimethoprim alone at 0.01% produced a 17.8mm diameter zone of inhibition and a combination containing 0.05% dapsone and 0.01% trimethoprim gave a zone of inhibition of 23.7 mm.
The antibacterial activity of the drug ofthis invention has been tested using standard techniques in which the zone of inhibition of a plate culture of microorganisms was measured for a range of drug concentrations. The results are given in the table below which includes, for comparison, results obtained for dapsone alone, sulphamethazine alone and sulphamethazine in combination with trimethoprim.
Sulphamethazine is a sulphonamide drug commonly used as an antibacterial.
TABLE Range of zones of inhibition (mm) for range of concs. tested Drug Range of concs. S. Aureus E. Coli B. Punilus Bordetella Spp.
D (0.01%-0.1%) 0-16.6 0-13.8 27.9-40.0 0 S (0.01%-0.1%) 0-24.9 0 18.8-41.0 0 S+T S(0.01%-0.1%) 23.8-31.4 16.6-23.4 33.5-37.1 0-13.2 T (0.01%) D+T D(0.01%-0.1%) 21.0-31.2 19.2-23.4 31.8-49.2 12.0-15.0 T (0.01%) D = Dapsone S = Sulphamethazine T = TrimethoDrim
CLAIMS 1. An antibacterial drug comprising an admixture of a sulphone and a pyrimidine derivative each of which has antibacterial activity.
2. A drug as claimed in claim 1, in which the pyrimidine derivative is trimethoprim.
3. A drug as claimed in claim 1 or 2, in which the sulphone is thiambutosine, clofazimine, solapsone or dapsone.
4. A drug as claimed in claim 3, in which the sul phone is dapsone.
5. A pharmaceutical preparation comprising the antibacterial drug claimed in claim 1 in conjunction with a pharmaceutically acceptable liquid vehicle for parenteral or oral administration.
6. A pharmaceutical preparation comprising the antibacterial drug claimed in claim 1, in conjunction with a pharmaceutically acceptable solid carrier, for administration in the form of a tablet or powder.
7. A pharmaceutical preparation comprising the antibacterial drug claimed in claim 1, in conjunction with a pharmaceutical unguent base, for topical application.
**WARNING** end of DESC field may overlap start of CLMS **.

Claims (7)

**WARNING** start of CLMS field may overlap end of DESC **. SPECIFICATION Antibacterial drug This invention relates to an antibacterial drug. This invention provides a drug combination of known antibacterial drugs which act synergistically resulting in mutual potentiation of the antibacterial activities of the individual components of the com bination. According to the present invention there is pro vided an antibacterial drug comprising a synergistic mixture of a sulphone and a pyrimidine derivative, each having antibacterial activity. The sulphone may be dapsone, thiambutosine, clofazimine or solapsone and of these the most pref erable is dapsone. The most preferred pyrimidine based antibacterial is trimethoprim. The preferred weight ratio of sulphone to pyrimidine derivative is from 100:1 to 5:1. However, advantage may still be observed at ratios of 500:1 to 1:100. The antibacterial drug ofthis invention is effective against gram-positive and gram-negative microor ganisms. The drug may be administered parenterally by intramammary or intramuscular injection or orally in the form of tablets, solutions or emulsions. The main envisaged area of application is in the treatment of bacterial infection in cattle. A preferred solution for intramuscular injection is as follows: Dapsone 209 Trimethoprim 49 Dimethylacetamide 50ml Water 20ml Benzyl Alcohol 1ml Propylene glycol to 100ml A preferred formulation for intramammary injection is as follows: Dapson 19 Trimethoprim 0.2g Paraffin base to 5g The potentiation of the drug combination of the invention against staphylococcus aureus is evidenced by the following results which were obtained using a zone inhibition measurement as indication of activity.Dapsone alone at a concentration of 0.05% produced no detectable inhibition, trimethoprim alone at 0.01% produced a 17.8mm diameter zone of inhibition and a combination containing 0.05% dapsone and 0.01% trimethoprim gave a zone of inhibition of 23.7 mm. The antibacterial activity of the drug ofthis invention has been tested using standard techniques in which the zone of inhibition of a plate culture of microorganisms was measured for a range of drug concentrations. The results are given in the table below which includes, for comparison, results obtained for dapsone alone, sulphamethazine alone and sulphamethazine in combination with trimethoprim. Sulphamethazine is a sulphonamide drug commonly used as an antibacterial. TABLE Range of zones of inhibition (mm) for range of concs. tested Drug Range of concs. S. Aureus E. Coli B. Punilus Bordetella Spp. D (0.01%-0.1%) 0-16.6 0-13.8 27.9-40.0 0 S (0.01%-0.1%) 0-24.9 0 18.8-41.0 0 S+T S(0.01%-0.1%) 23.8-31.4 16.6-23.4 33.5-37.1 0-13.2 T (0.01%) D+T D(0.01%-0.1%) 21.0-31.2 19.2-23.4 31.8-49.2 12.0-15.0 T (0.01%) D = Dapsone S = Sulphamethazine T = TrimethoDrim CLAIMS
1. An antibacterial drug comprising an admixture of a sulphone and a pyrimidine derivative each of which has antibacterial activity.
2. A drug as claimed in claim 1, in which the pyrimidine derivative is trimethoprim.
3. A drug as claimed in claim 1 or 2, in which the sulphone is thiambutosine, clofazimine, solapsone or dapsone.
4. A drug as claimed in claim 3, in which the sul phone is dapsone.
5. A pharmaceutical preparation comprising the antibacterial drug claimed in claim 1 in conjunction with a pharmaceutically acceptable liquid vehicle for parenteral or oral administration.
6. A pharmaceutical preparation comprising the antibacterial drug claimed in claim 1, in conjunction with a pharmaceutically acceptable solid carrier, for administration in the form of a tablet or powder.
7. A pharmaceutical preparation comprising the antibacterial drug claimed in claim 1, in conjunction with a pharmaceutical unguent base, for topical application.
GB8125077A 1980-08-15 1981-08-17 Antibacterial drug Withdrawn GB2082063A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
GB8125077A GB2082063A (en) 1980-08-15 1981-08-17 Antibacterial drug

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB8026631 1980-08-15
GB8125077A GB2082063A (en) 1980-08-15 1981-08-17 Antibacterial drug

Publications (1)

Publication Number Publication Date
GB2082063A true GB2082063A (en) 1982-03-03

Family

ID=26276572

Family Applications (1)

Application Number Title Priority Date Filing Date
GB8125077A Withdrawn GB2082063A (en) 1980-08-15 1981-08-17 Antibacterial drug

Country Status (1)

Country Link
GB (1) GB2082063A (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2531861A1 (en) * 1982-07-29 1984-02-24 Hoffmann La Roche SYNERGISTIC PHARMACEUTICAL PREPARATION BASED ON DDS AND BRODIMOPRIM, FOR THE TREATMENT OF LEPROSY

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2531861A1 (en) * 1982-07-29 1984-02-24 Hoffmann La Roche SYNERGISTIC PHARMACEUTICAL PREPARATION BASED ON DDS AND BRODIMOPRIM, FOR THE TREATMENT OF LEPROSY
GB2125293A (en) * 1982-07-29 1984-03-07 Hoffmann La Roche Pharmaceutical preparation containing diaminodiphenylsulphone and brodimoprim
DE3326165A1 (en) * 1982-07-29 1984-04-12 F. Hoffmann-La Roche & Co AG, 4002 Basel PHARMACEUTICAL PREPARATION

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