Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K9/00—Medicinal preparations characterised by special physical form
  • A61K9/10—Dispersions; Emulsions
  • A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K9/00—Medicinal preparations characterised by special physical form
  • A61K9/10—Dispersions; Emulsions
  • A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
  • A61K9/1075—Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
  • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
  • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
  • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
  • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
  • A61K47/24—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
  • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
  • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P13/00—Drugs for disorders of the urinary system

Definitions

• Emulsion-like water-soluble concentrates are provided.
• the present invention relates to emulsion-like transparent to translucent water-soluble concentrates with the features of claim 1 and their use for cosmetic, pharmaceutical or dietetic purposes.
• Lipophilic or fat-like substances in the pharmaceutical, cosmetic and dietetic field usually have to be converted into a form which can be used without problems.
• the classic emulsion is a form that can be used without any problems, in which emulsifiers reduce the interfacial tension at the interface of the fat droplets and thus ensure a fine, stable distribution of fat in water.
• emulsions of creamy to milky consistency with emulsifier amounts of 0.5% -10% being used.
• the particle size of the fat droplets of a conventional emulsion depends on many factors, such as fat, emulsifier, energy input and is normally in the three-digit nm range (100-1000 nm).
• Perfumes also predominantly contain fat-like fragrances dissolved in a clear, transparent form. Poorly water-soluble pharmaceuticals are also processed into transparent formulations when administered orally and parenterally.
• the aim of a topical, oral or parenteral product is to apply the lipophilic active ingredient.
• Emulsifiers or co-emulsifiers are undesirable but technologically necessary auxiliary substances.
• Emulsifiers must be used in large quantities for solubilization, so that considerable amounts of auxiliary substances must always be carried along to use the actual active ingredient.
• a 25% (w / w) ethanolic solution is required; or in order to solubilize 20 g of vitamin E acetate in a conventional manner, 44 g of PEG-36 castor oil and 25 g of propylene glycol in an aqueous solution are required.
• To solubilize the lipophilic vitamins A, E and D in a conventional manner for example, about 10 times the excess of a mixture of glycocholic acid and phosphatidylcholine is required.
• the emulsifier / coemulsifier system used is exclusively a mixture of lecithin and ethoxylated emulsifiers, lecithin / emulsifiers with a high HLB value or lecithin / volatile alcohols.
• the object of the present invention is now to convert water-soluble substances which are difficult to water into transparent or translucent emulsion-like water-soluble ones
• Ethoxylated surfactants or other strong solubilizers can with the invention through a system of natural
• the invention only requires 5-100% of the mass of the fat body as a solubilizer (lecithin / phospholipid). With previous methods, the relationship is reversed.
• Solvents ethanol, isopropanol, etc. can be dispensed with.
• emulsion-like solution concentrates are produced according to the invention, which, after dilution with water, give opaque to transparent, finely dispersed emulsions that were not or only much more difficult to produce bypassing the emulsion-like concentrate.
• the concentrates according to the invention can be used directly as a product for, for example, medical or cosmetic oil baths, mouthwashes, perfumes, drinks or food supplements or else by dilution with water or other water-containing solutions (for example juices) in finely dispersed, transparent - opaque O / W - Emulsions (nanoemulsions) with very small particle size distributions in the two to three-digit nm range are transferred. Due to the very good solubility in water, these transparent emulsion-like concentrates can be easily incorporated into cosmetic products (gels, creams, lotions, etc.), pharmaceutical or dietary products.
• An emulsion-like solution concentrate from lecithins and / or phospholipids, lipids and highly concentrated solutions of polyols or carbohydrates is produced according to the following criteria:
• the ratio of lecithin / phospholipid to fat-like substance should be chosen so that a transparent concentrate is created that can be easily diluted with water and the water content of the polyol or carbohydrate solutions should be chosen so that not only a transparent concentrate is created, but also - due to the low water value - a self-preserving system, so that the addition of synthetic or natural preservatives can be dispensed with.
• the processing temperature should be adapted to the lecithms / phospholipids used or the lipids to be solubilized. his. With hydrogenated
• Lecithms / phospholipids are naturally processing temperatures between 40 and 80 ° C. with unsaturated lecithms / phospholipids it is possible to work at room temperature, the lecithms / phospholipids preferably m the polar phase, i. H. be incorporated into the polyol or carbohydrate solutions.
• a phospholipid fraction from soy with a PC content of 70% are dispersed in 75 g of a 70% fructose solution with stirring. After adding 20 g of a medium-chain triglyceride and high pressure homogenizing this mixture, a transparent emulsion-like solution of honey-like viscosity is formed.

Landscapes

• Health & Medical Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Public Health (AREA)
• General Health & Medical Sciences (AREA)
• Veterinary Medicine (AREA)
• Pharmacology & Pharmacy (AREA)
• Medicinal Chemistry (AREA)
• Animal Behavior & Ethology (AREA)
• Epidemiology (AREA)
• Engineering & Computer Science (AREA)
• General Chemical & Material Sciences (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Oil, Petroleum & Natural Gas (AREA)
• Molecular Biology (AREA)
• Biophysics (AREA)
• Dispersion Chemistry (AREA)
• Biochemistry (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Urology & Nephrology (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Organic Chemistry (AREA)
• Medicinal Preparation (AREA)
• Cosmetics (AREA)
• Colloid Chemistry (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• General Preparation And Processing Of Foods (AREA)
• Coloring Foods And Improving Nutritive Qualities (AREA)
• Detergent Compositions (AREA)
• Soft Magnetic Materials (AREA)
• Edible Oils And Fats (AREA)

Priority Applications (16)

Applications Claiming Priority (2)

Publications (2)

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ID=32308727

Family Applications (1)

Country Status (20)

Cited By (4)

Families Citing this family (15)

Family Cites Families (22)

• 2002
  • 2002-11-27 DE DE10255195A patent/DE10255195A1/de not_active Withdrawn
• 2003
  • 2003-11-25 CN CN2003801084362A patent/CN1738603B/zh not_active Expired - Lifetime
  • 2003-11-25 US US10/536,384 patent/US20060159633A1/en not_active Abandoned
  • 2003-11-25 SI SI200332138T patent/SI1565163T1/sl unknown
  • 2003-11-25 PT PT03785529T patent/PT1565163E/pt unknown
  • 2003-11-25 KR KR1020057009707A patent/KR101153757B1/ko not_active Expired - Lifetime
  • 2003-11-25 AU AU2003294633A patent/AU2003294633B2/en not_active Expired
  • 2003-11-25 BR BR0316731-3A patent/BR0316731A/pt not_active Application Discontinuation
  • 2003-11-25 DE DE10394113T patent/DE10394113D2/de not_active Expired - Fee Related
  • 2003-11-25 ES ES03785529T patent/ES2381461T3/es not_active Expired - Lifetime
  • 2003-11-25 CA CA2507688A patent/CA2507688C/en not_active Expired - Lifetime
  • 2003-11-25 RU RU2005120159/15A patent/RU2358715C2/ru active
  • 2003-11-25 EP EP03785529A patent/EP1565163B1/de not_active Revoked
  • 2003-11-25 DK DK03785529.3T patent/DK1565163T3/da active
  • 2003-11-25 AT AT03785529T patent/ATE543487T1/de active
  • 2003-11-25 WO PCT/DE2003/003887 patent/WO2004047791A2/de not_active Ceased
  • 2003-11-25 MX MXPA05005720A patent/MXPA05005720A/es active IP Right Grant
  • 2003-11-25 UA UAA200506238A patent/UA86756C2/ru unknown
  • 2003-11-25 JP JP2004554223A patent/JP2006513172A/ja active Pending
• 2005
  • 2005-05-26 IL IL168826A patent/IL168826A/en active IP Right Grant
• 2012
  • 2012-03-19 JP JP2012062525A patent/JP5762340B2/ja not_active Expired - Lifetime
  • 2012-04-25 CY CY20121100392T patent/CY1112824T1/el unknown

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