Classifications

• • A—HUMAN NECESSITIES
  • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
  • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
  • A01N33/00—Biocides, pest repellants or attractants, or plant growth regulators containing organic nitrogen compounds
  • A01N33/02—Amines; Quaternary ammonium compounds
  • A01N33/12—Quaternary ammonium compounds

Definitions

• the invention relates to antiseptic compositions, and in particular to ready to use antiseptic compositions.
• compositions containing such compounds and suitable for application to the human, or animal, body are generally referred to as antiseptics.
• antiseptic compositions have been produced, and provided to the public, in concentrated form to be diluted at the time of use. This has a number of drawbacks, including the unavailability of water when antisepsis is required, unclean or
• an aqueous, topical, ready to use, antiseptic composition comprising
• each R 1 is independently selected from hydrogen, a C 1-4 alkyl group, a C 1-4 alkoxy group, a halogen or a hydroxy group;
• n 0 to 3 ;
• R 2 and R 3 are independently selected from C 1-4 alkyl groups
• R 4 is a C 6-22 alkyl chain (or a mixture thereof) , and X is an anion;
• composition further comprising substantially no monohydric alcohols.
• the monohydric alcohols to be excluded from the compositions of the invention include ethanol and methanol.
• R 1 is hydrogen, n is 1 or 2 (most preferably 1) , R 2 and R 3 are each methyl, R 4 is an alkyl chain of C 8 . 1B length (or a mixture thereof) and X is a halogen.
• the compound of formula I is a mixture of alkyldimethylbenzyl ammonium chlorides (commercially available as "benzalkonium chloride”) .
• the concentration of the compound of formula I is from 0.1 to 0.5 % w/v, more preferably 0.15 to 0.3% w/v.
• the chelating agents are selected from ethylenediamine tetraacetic acid (EDTA) or a derivative or a salt thereof, or ethylene glycol bis [ ⁇ -aminoethyl ether] -N,N,N', N' -tetraacetic acid (EGTA) or a derivative or salt thereof.
• EDTA ethylenediamine tetraacetic acid
• EGTA ethylene glycol bis [ ⁇ -aminoethyl ether] -N,N,N', N' -tetraacetic acid
• the chelating agent is EDTA or a sodium or potassium salt thereof, or EGTA or a sodium or potassium salt thereof; most preferably it is a sodium salt of EDTA.
• the concentration of the chelating agent is from 0.005 to 0.1% w/v, more preferably 0.01 to 0.05% w/v (expressed as the free acid where appropriate)
• the polyhydric alcohol is selected from polyethylene glycols of average molecular weight 200 to 1000 (particularly 200 to 600) , propylene glycol, ethylene glycol or mixtures thereof. Most preferably the polyhydric alcohol is propylene glycol.
• the amount of polyhydric alcohol in a composition of the invention is from 2 to 4% w/v, more preferably 2 to 3% w/v.
• compositions of the invention are suitable (and are intended) to be used directly on the skin of humans or animals without further dilution. Therefore preferably the compositions of the invention are substantially free of any compound which may cause irritation to the skin.
• compositions of the invention contain substantially no biocidal phenolic compounds (other than compounds of formula I, where appropriate) . More preferably the compositions of the invention are substantially free of any biocidal compounds other than compounds of formula I . For the avoidance of doubt, we do not consider EDTA or EGTA (or salts thereof) to be biocidal compounds.
• compositions of the invention may further contain conventional ingredients of antiseptic compositions, as appropriate. However, it is preferred that the compositions of the invention contain substantially no nonionic surfactants and most preferably they contain substantially no surfactants at all (other than quaternary ammonium biocides of Formula I)
• a preferred extra component in the compositions of the invention is a topical anaesthetic.
• the topical anaesthetic is lignocaine or the hydrochloride salt thereof.
• the lignocaine When present, the lignocaine will be present at an amount of from 1 to 5% w/v, more preferably from 2 to 3.5% w/v. Further according to the invention there is provided an aqueous, topical, ready to use, antiseptic composition comprising
• composition further containing substantially no biocidal phenolic compounds (and preferably no further biocides) ;
• buffering and pH control agents for example sodium acid phosphate and sodium phosphate
• perfumes and colouring agents for example sodium acid phosphate and sodium phosphate
• the balance of the compositions of the invention will be water.
• the water is softened, distilled or deionised water, most preferably it is softened water.
• compositions of the invention may be produced by any conventional manufacturing process; for example by simply mixing all of the ingredients at room temperature, or whilst heating the mixture, until a solution is formed.
• the compositions may be produced directly in dilute form or as concentrates to be diluted before packaging.
• compositions of the invention may be packaged in any conventional form.
• examples include in sprayable form such as aerosols (also comprising a propellant) or so called pump packs; dispersed onto cloths as antiseptic wipes; in ampoules as single use packs or in conventional (multiple dose) bottles.
• compositions of the invention are in a ready to use form, are simple to produce, none irritant and have effective antiseptic properties on the skin.
• a composition was made up at 25°C by mixing the following components together
• a composition was made up at 25°C by mixing the following components together
• compositions of Examples 1 and 2 can be applied to the skin "neat” and have good antiseptic properties .
• a composition was made up at 25°C by mixing the following components together.
• Example 2 The microbiological activity of the composition of Example 2 was tested using the Proposed Suspension Test for the Evaluation of Antimicrobial Efficacy of
• Staphylococcus aureus ATCC 6538 Methicillin Resistant S . aureus (MRSA) , Enterococcus hirae ATCC 10541, Escherichia coli ATCC 10536, CitroJbacter freundii ATCC 8090, Klebsiella pneumoniae ATCC 13883, Proteus mirabilis ATCC 14153 and Pseudomonas aeruginosa ATCC 15442 was assessed in the presence of 1% combined albumin/yeast extract (CAY) . Under the test conditions the maximum concentration of product that can be tested is 80% v/v.
• CAY albumin/yeast extract
• Example 2 achieved excellent activity, log reductions in excess of 5, against all the challenge organisms, see Table 1.
• Example 2 Twenty-six human volunteers of either sex aged between 18 and 65 took part in the trial. The composition of Example 2 was applied to the skin undiluted. Deionised water and a blank untreated site were included as controls. Each sample was applied to the upper outer arm via an occlusive aluminium Finn chamber which provided a test area of 50 mm 2 and a volume of 25 ⁇ l . Patches were applied for an initial period of 6 hours, then removed and assessed using a numerical scoring system.

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• Life Sciences & Earth Sciences (AREA)
• Wood Science & Technology (AREA)
• General Health & Medical Sciences (AREA)
• Plant Pathology (AREA)
• Health & Medical Sciences (AREA)
• Zoology (AREA)
• Dentistry (AREA)
• Pest Control & Pesticides (AREA)
• Agronomy & Crop Science (AREA)
• Engineering & Computer Science (AREA)
• Environmental Sciences (AREA)
• Medicinal Preparation (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Agricultural Chemicals And Associated Chemicals (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Cosmetics (AREA)
• Detergent Compositions (AREA)

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• 1996
  • 1996-01-05 GB GBGB9600140.9A patent/GB9600140D0/en active Pending
  • 1996-12-10 GB GB9625759A patent/GB2308812B/en not_active Expired - Lifetime
  • 1996-12-11 AU AU11033/97A patent/AU715706B2/en not_active Expired
  • 1996-12-11 NZ NZ323980A patent/NZ323980A/xx unknown
  • 1996-12-11 CN CN96180186A patent/CN1120662C/zh not_active Expired - Lifetime
  • 1996-12-11 WO PCT/GB1996/003037 patent/WO1997024927A1/en not_active Application Discontinuation
  • 1996-12-11 EP EP96941752A patent/EP0877553A1/de not_active Withdrawn
  • 1996-12-23 ZA ZA9610838A patent/ZA9610838B/xx unknown

Non-Patent Citations (1)

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