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
  • A01N31/00—Biocides, pest repellants or attractants, or plant growth regulators containing organic oxygen or sulfur compounds
  • A01N31/02—Acyclic compounds
• • 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
  • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
  • A01N43/34—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom
  • A01N43/40—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P17/00—Drugs for dermatological disorders
  • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics

Definitions

• the present invention relates to an aqueous wound and mucous membrane disinfectant on the basis of octenidine dihydrochloride, which contains further ingredients from the group ethanol, propan-1-ol, propan-2-ol, undecylene amidopropyl trimonium methosulfate, sodium hydroxymethylglycinate, and 3-(4-chlorophenoxy)-1,2 propanediol.
• the disinfectant according to the present invention has a pH value of from 5 to 7 and is free of phenoxyethanol, phenoxypropanol, phenoxyisopropanol and organic acids.
• a wound and mucous membrane disinfectant should primarily meet certain microbiological requirements, which are described, for example, in F.-A. Pitten, H.-P. Werner, A. Kramer, “A standardized test to assess the impact of different organic challenges on the antimicrobial activity to antiseptics,” Journal of Hospital Infection (2003) 55, 108-115. However, increasing importance is also being attached to the wound, skin or mucous membrane tolerance of a corresponding disinfectant.
• Iodine and PVP-iodine frequently trigger allergies with hypersensitivity, moreover, the skin is strongly colored and iodine, particularly from alcoholic solutions, penetrates through the skin and even more markedly through the mucous membrane, which can lead to hyperthyroidosis and even iodism in sensitive persons. Although these side effects are slighter with PVP-iodine, they are likewise manifest.
• chlorhexidine and salts thereof are the most important active ingredients in antiseptics worldwide, although these compounds are viewed critically from a toxicological standpoint. Chlorhexidine is positive in the Ames Test and in the DNA Repair Test. Both results indicate a mutagenic potential.
• the breakdown products 4-chloraniline and 4-chlorophenyl isocyanate have a great affinity to the skin and concentrate there with frequent use. Triclosan, a chlorinated phenol, penetrates through the skin to a great extent and is a potential dioxin former.
• Octenidine dihydrochloride is known as an active ingredient in mucous membrane and wound antiseptics and can be described by the limiting structure formulae below:
• the raw material octenidine dihydrochloride has a good microbicidal effectiveness with relatively good tolerance.
• an aqueous mucous membrane antiseptic is described, which contains phenoxyethanol and/or phenoxypropanol in addition to octenidine dihydrochloride to increase effectiveness.
• a preparation of this type is commercially available, e.g., under the name “Octenisept” and is often used in gynecology and andrology.
• Octenisept e.g., under the name “Octenisept”
• recent tests have shown that the combination of octenidine dihydrochloride and phenoxyethanol has a high cytotoxicity, so that considerable reservations are justified regarding use on open wounds.
• wound and mucous membrane disinfectants which, in addition to octenidine dihydrochloride, now contain ethanol and a physiologically tolerated organic acid instead of the above-referenced combination.
• organic acids lactic acid, glycolic acid, malonic acid, succinic acid, malic acid, tartaric acid, or citric acid.
• the pH value of these solutions is 2.5 to 3.0. Acid preparations in this very low range can definitely be tolerated with infrequent use, but represent a noxa with longer-term application.
• microbicidal active ingredients have a certain irritative potential, to which the mucous membranes react with particular sensitivity.
• the object of the invention was therefore to develop a wound and mucous membrane disinfectant based on octenidine dihydrochloride, which on the one hand meets the microbicidal requirements—particularly with respect to the effectiveness regarding Candida albicans —but on the other hand has a more favorable pH value compared with the formulas of the prior art and thus a better wound, skin or mucous membrane tolerance.
• Particularly preferred components according to the invention according to b) are 1-propanol and ethanol.
• Particularly preferred ingredients according to the invention according to c) are glycerin, 1,2-propanediol, 1,2-butanediol, 1,2-pentanediol and/or 1,2-hexanediol.
• the content of octenidine dihydrochloride is selected from the range of 0.05 to 0.2% by weight. Particularly preferably, the content of octenidine dihydrochloride is approx. 0.1% by weight, in order to achieve a very good microbicidal effectiveness with at the same time excellent skin tolerance.
• the wound and mucous membrane disinfectant according to the invention contains
• a wound and mucous membrane disinfectant according to the invention is particularly preferred which consists of:
• a wound and mucous membrane disinfectant is particularly preferred according to the invention.
• the wound and mucous membrane disinfectants according to the invention can in addition contain other substances such as dyestuffs, perfumes, emulsifiers, solubilizers, pH regulators, thickeners and/or surfactants.
• substances such as dyestuffs, perfumes, emulsifiers, solubilizers, pH regulators, thickeners and/or surfactants.
• dyestuffs perfumes, emulsifiers, solubilizers, pH regulators, thickeners and/or surfactants.
• surfactants Preferably according to the invention, only those substances are taken into consideration for this purpose that have no or only a very low additional irritative potential.
• Surfactants and emulsifiers are accordingly particularly suitable for an application for the purposes of the present invention which show no or only a very low irritative potential in the red blood cell test (RBC test) code 11035 and/or in the hen's egg test chorioaallantoic membrane code 11087 (HET-CAM test).
• RBC test red blood cell test
• HET-CAM test hen's egg test chorioaallantoic membrane code 11087
• Surfactants that are suitable and accordingly advantageously to be used for the purpose of the present invention are, for example, ethoxylated glyceryl palmitate (INCI name: PEG-200 hydrogenated glyceryl palmate), ethoxylated sorbitan laurate (INCI: PEG-80 sorbitan laurate), ethoxylated glyceryl isostearate (INCI: PEG-90 glyceryl isostearate), ethoxylated lauryl alcohol (INCI: laureth-2) or also betaines such as, e.g., cocamidopropyl betaine (INCI), a concentration between 0 and 1.0% by weight having proven advantageous.
• the emulsifiers reference is made by way of example to the ethoxylated fatty alcohols or also fatty acid esters (INCI: ceteareth-20, glyceryl stearate).
• the wound and mucous membrane disinfectants according to the invention are clear solutions with a pH value of from 5 to 7.
• This pH value results, for example, in the particularly preferred formula “by itself,” as it were. In other cases it may be necessary to adjust the pH value accordingly.
• aqueous sodium hydroxide or phosphoric acid have proven useful for this purpose.
• the wound and mucous membrane disinfectants can advantageously also contain thickeners for the purpose of the present invention.
• Synthetic polymers on a polyacrylic acid basis or natural thickeners, such as xanthan gum or modified natural types of thickeners, such as, e.g., cellulose derivatives, are preferably to be used according to the invention.
• wound and mucous membrane disinfectant according to the invention can be used in different application forms, e.g., per se (i.e., in the form of an aqueous solution), as a gel or as an impregnation solution for wipes and/or bandages.
• the wound or mucous membrane disinfectant for the purpose of the present invention can furthermore preferably also represent the aqueous phase of an emulsion that furthermore contains as oil phase those lipids that are known to be particularly well tolerated by wounds and mucous membranes, such as, e.g., natural oils or modified oils and fats (e.g., almond oil, hydrogenated castor oil).
• the subject of the present invention are therefore also O/W or W/O emulsions—e.g., in the form of a cream, lotion or a spray—which comprise the aqueous mucous membrane disinfectant.
• O/W or W/O emulsions e.g., in the form of a cream, lotion or a spray—which comprise the aqueous mucous membrane disinfectant.
• Var. Var. Var. Var. Var. Var. Var. Var. Var. Var. Var. Var. Var. Var. Var. Var. Var. Var. Var. Phosphoric acid solution Var. Var. Var. Var. Var. Var. Var. Var. Var. Var. Var. Var. Water ad ad ad ad ad ad ad ad ad ad ad ad 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 Quantities in % by weight

Landscapes

• Life Sciences & Earth Sciences (AREA)
• Health & Medical Sciences (AREA)
• General Health & Medical Sciences (AREA)
• Engineering & Computer Science (AREA)
• Environmental Sciences (AREA)
• Zoology (AREA)
• Wood Science & Technology (AREA)
• Dentistry (AREA)
• Plant Pathology (AREA)
• Pest Control & Pesticides (AREA)
• Agronomy & Crop Science (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Pharmacology & Pharmacy (AREA)
• Animal Behavior & Ethology (AREA)
• Chemical & Material Sciences (AREA)
• Organic Chemistry (AREA)
• Medicinal Chemistry (AREA)
• General Chemical & Material Sciences (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Dermatology (AREA)
• Oncology (AREA)
• Communicable Diseases (AREA)
• Medicinal Preparation (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Agricultural Chemicals And Associated Chemicals (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Applications Claiming Priority (5)

Related Parent Applications (1)

Related Child Applications (1)

Publications (1)

Family

ID=37067642

Family Applications (2)

Family Applications After (1)

Country Status (5)

Cited By (3)

Families Citing this family (7)

Citations (5)

Family Cites Families (9)

• 2005
  • 2005-12-09 DE DE102005058978A patent/DE102005058978A1/de not_active Withdrawn
• 2006
  • 2006-07-31 US US12/064,746 patent/US20090076084A1/en not_active Abandoned
  • 2006-07-31 PL PL06792607T patent/PL1924144T5/pl unknown
  • 2006-07-31 WO PCT/EP2006/064836 patent/WO2007023066A1/fr active Application Filing
  • 2006-07-31 EP EP06792607.1A patent/EP1924144B2/fr not_active Not-in-force
• 2011
  • 2011-09-20 US US13/236,847 patent/US8465766B2/en active Active

Patent Citations (5)

Also Published As

Similar Documents

Legal Events