WO1997000666A1 - Composition renfermant du goudron et preparation pharmaceutique et cosmetique contenant cette composition - Google Patents

Composition renfermant du goudron et preparation pharmaceutique et cosmetique contenant cette composition Download PDF

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Publication number
WO1997000666A1
WO1997000666A1 PCT/EP1996/002710 EP9602710W WO9700666A1 WO 1997000666 A1 WO1997000666 A1 WO 1997000666A1 EP 9602710 W EP9602710 W EP 9602710W WO 9700666 A1 WO9700666 A1 WO 9700666A1
Authority
WO
WIPO (PCT)
Prior art keywords
composition according
tar
composition
derivative
pharmaceutical preparation
Prior art date
Application number
PCT/EP1996/002710
Other languages
German (de)
English (en)
Inventor
José Maria DE MORAGAS VINAS
Pedro Gonzales Ensenat
Günther Maierhofer
Original Assignee
Dianorm G. Maierhofer Gmbh
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Dianorm G. Maierhofer Gmbh filed Critical Dianorm G. Maierhofer Gmbh
Priority to EP96923887A priority Critical patent/EP0833607A1/fr
Publication of WO1997000666A1 publication Critical patent/WO1997000666A1/fr

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K35/00—Medicinal preparations containing materials or reaction products thereof with undetermined constitution
    • A61K35/02—Medicinal preparations containing materials or reaction products thereof with undetermined constitution from inanimate materials
    • A61K35/04—Tars; Bitumens; Mineral oils; Ammonium bituminosulfonate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/14—Liposomes; Vesicles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/55—Phosphorus compounds
    • A61K8/553—Phospholipids, e.g. lecithin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/63—Steroids; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A61K9/127—Liposomes
    • A61K9/1271—Non-conventional liposomes, e.g. PEGylated liposomes, liposomes coated with polymers
    • A61K9/1272—Non-conventional liposomes, e.g. PEGylated liposomes, liposomes coated with polymers with substantial amounts of non-phosphatidyl, i.e. non-acylglycerophosphate, surfactants as bilayer-forming substances, e.g. cationic lipids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q5/00—Preparations for care of the hair
    • A61Q5/02—Preparations for cleaning the hair

Definitions

  • the present invention relates to a new tar-containing composition, a cosmetic preparation containing the same, its use, and pharmaceutical preparations containing the composition according to the invention.
  • Tars are mixtures with different chemical constituents and consist primarily of hydrocarbon mixtures with a high proportion of aromatic hydrocarbons with antiproliferative properties. Their therapeutic usability, especially in dermatological indications, has been known for decades. Topically applied, tars have an anti-inflammatory, antipruritic and weakly infectious effect. They have long been successful in the treatment of flaky and chronic skin diseases that are associated with more or less severe itching, e.g. Neurodermatitis, psoriasis, chronic eczema, etc., used. Coal tar distillates (Pix lithantracis) are most commonly used, either undiluted in the form of tar envelopes or as a component of ointments and pastes
  • Balneum Hermal 10 with tar as part of balneotherapy use up to 30% coal tar distillate. In comparison, the tar concentration in dermatics is considerably lower at 2% by weight.
  • the object of the present invention is therefore to find a way by which the absolute dose of the applied tar derivatives can be reduced without reducing the positive therapeutic effects.
  • composition comprising the following components:
  • nanodisperse systems can be formed which, when applied locally, topically penetrate the skin much better than conventional carrier systems and are distributed much more quickly and homogeneously in the cornea and epidermis.
  • concentration of the active ingredient mixture can be reduced to 0.1 to 0.01% of conventional tar-containing preparations.
  • the tar concentration of preparations which have been produced with the compositions according to the invention is therefore a factor of 20 to 200 lower than in currently approved dermatics.
  • nanodisperse carrier systems such as, for example, nanoemulsions or liposomes, there are generally fewer side effects of drugs.
  • the phospholipid contained in the composition according to the invention is preferably a phosphatidylcholine of pharmaceutical quality, the aliphatic residues of the phospholipid preferably comprising 12 to 22 carbon atoms with up to 4 cis double bonds. Unbranched aliphatic radicals are preferred. A phospholipid in which the aliphatic radicals have 16 to 20 carbon atoms and a maximum of 3 cis double bonds, as in natural vegetable lecithins, for example soybean lecithin, is particularly preferred.
  • the aliphatic radicals R 1 and R 2 can have the same or different number of carbon atoms. According to the invention, the phospholipid can be natural, semi-synthetic or fully synthetic.
  • the bile acid and / or its derivatives can also be of natural, semi-synthetic or fully synthetic origin.
  • Preferred derivatives are bile acid salts, especially sodium salts.
  • the composition according to the invention comprises one or more sodium salts from the group consisting of sodium cholate, sodium deoxycholate, sodium glycocholate, sodium taurocholate, sodium taurodeoxycholate, sodium tauroursocholate and sodium chenoxycholate and / or one or more of the corresponding bile acids.
  • the tar derivative is preferably a coal tar derivative.
  • coal tar distillate is used in the composition.
  • ethanol 96% ethanol according to DAB10 is preferably used as ethanol.
  • Ethanol imparts long-term stability to the finely dispersed system formed with the composition according to the invention and also appears to enhance the effect of the therapeutically active tar derivative.
  • the water used should be of the quality required for pharmaceutical or cosmetic products.
  • the composition according to the invention is preferably provided as a concentrate in which the phospholipid is contained in a concentration of 10 to 200 mg / ml, preferably 40 to 100 mg / ml, and the bile acid and / or its derivative (s) ) is (are) in a molar ratio of 2 to 10 to 1 (lipid to cholate).
  • Ethanol is preferably in a ratio of between 1: 2 and 1: 0.5 (v / w, ie volume / weight), based on the phospholipid, particularly preferably in a ratio of 1: 1.
  • the concentrate according to the invention is diluted for use in a ratio of 1: 1 to 1: 200, preferably 1: 5 to 1: 125 and particularly preferably 1:20 to 1: 100.
  • Water or salt solutions serve as diluents, preferably those with 0.1 to 0.9% by weight of common salt.
  • composition is preferably used as a finely dispersed system based on lipid mixtures, micelles, mixed micelles, reverse micelles, uni-, oligo- or multilamelar liposomes, nanoemulsions, nanoparticles or nanocolloids.
  • Finely disperse systems are understood here to mean systems with particles whose diameter is approximately 4 to 500 nm. The average diameter of the particles is preferably less than 250 nm.
  • one or more pharmaceutical and / or cosmetic auxiliaries can be added to the composition.
  • one or more unsaturated phosphatidylcholines are used as the phospholipid, it is advisable to add antioxidants to the composition.
  • tocopherol is used as an antioxidant.
  • salts in particular table salt or buffer substances, can also be added.
  • auxiliaries such as cosurfactants, for example polysorbate or free fatty acids, usually contained in medicinal products and / or cosmetics can be acids, as well as thickening agents and also preservatives.
  • composition according to the invention is particularly suitable for producing a cosmetic preparation. Additional cosmetic additives and perfuming agents can be added to this.
  • composition according to the invention serves as the basis of a pharmaceutical preparation.
  • a pharmaceutical preparation typically contains
  • the pharmaceutical preparation according to the invention is particularly suitable for the therapy of flaking and chronic skin diseases.
  • diseases are psoriasis, in particular psoriasis guttata, psoriasis en plaques, psoriasis inversa, psoriasis erythrodermica, psoriasis pustulosa, in particular psoriasis pustulosa palmaris et plantari ⁇ , psoriasis on the hairy head and psoriasis on the nails.
  • the pharmaceutical preparation according to the invention can also be used for the therapy of neurodermatitis, for the therapy of allergic contact eczema and for the therapy of seborrhoeic eczema. Its effectiveness has also been shown to be useful in the therapy of Lying Simplex Chronicus (Lying Vidal, Neurodermatitis circumscripta), the eczema cornea and the keratodermica rykteria Hatchausen.
  • the preparation according to the invention is thin-liquid and can be sprayed onto diseased areas using commercially available atomizers. This makes it very easy and convenient to use both on the skin and on the hairy head.
  • the preparation can be applied very quickly and evenly to the entire surface of the diseased area. It penetrates quickly into the cornea. A tedious washing off as with the conventional tar-containing ointments, e.g. Linola
  • Fett N ® is omitted because excess hair can be easily rinsed out with water.
  • the preparation produces neither itching nor burning and is well tolerated. It is low in odor and does not stain the skin or clothing. So far it has been well received by all patients.
  • the finely dispersed systems according to the invention in the form of pharmaceutical or cosmetic preparations according to the invention can be produced from the composition according to the invention described above by adding mechanical energy, for example by optimized mixing in a static mixer, pressure filtration, stirring, homogenization or filtration.
  • Commercially available devices can be used for this, such as, for example, static mixing systems or homogenizers from Gaulin or a microfluidizer. If more than 100 mg / ml of oil, based on the composition, is added in these processes, the process leads to nanoemulsions or nanocolloids, and without the addition of oils or an oil concentration of ⁇ 30 mg / ml, based on the composition, leads to liposomes.
  • Examples 1 to 3 show three different basic formulations for preparations according to the invention.
  • Example 4 the results of the use of pharmaceutical preparations according to the invention are reported.
  • Example 3 The two solutions from Example 1 are combined and homogenized with a household mixer, eg SG rod. The resulting finely dispersed system is brought to the desired application concentration by dilution with water. Depending on the requirements, sterile filtration is carried out or not.
  • a household mixer eg SG rod.
  • the resulting finely dispersed system is brought to the desired application concentration by dilution with water. Depending on the requirements, sterile filtration is carried out or not.
  • Example 1 500 g of lecithin as in Example 1 are dissolved in 500 ml of 96% ethanol together with 100 g of tar distillate. 15 g of cooking salt and 80 g of sodium cholate are dissolved in 4 kg of water. Both solutions are combined and in a standard agitator, e.g. Staphan UMC 12, stirred. The resulting finely dispersed system is brought to the desired final concentration by dilution with water. If necessary, a sterile filtration is connected.
  • a standard agitator e.g. Staphan UMC 12
  • the preparation according to the invention has a good to very good effect in the treatment of the diseases described.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical & Material Sciences (AREA)
  • Birds (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Biophysics (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Dispersion Chemistry (AREA)
  • Biotechnology (AREA)
  • Botany (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Medicinal Preparation (AREA)
  • Cosmetics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne une composition qui contient au moins un dérivé de goudron, une préparation cosmétique qui contient cette préparation, son utilisation et des préparations pharmaceutiques qui contiennent cette composition. Les préparations classiques au goudron se sont révélées cancérigènes en expérimentation animale. La composition décrite permet de produire des préparations cosmétiques et pharmaceutiques sous forme de systèmes finement dispersés qui ont une meilleure efficacité et moins d'effets secondaires que les préparations classiques, tout en présentant une concentration en goudron 20 à 200 fois inférieure à la concentration en goudron de celles-ci.
PCT/EP1996/002710 1995-06-22 1996-06-21 Composition renfermant du goudron et preparation pharmaceutique et cosmetique contenant cette composition WO1997000666A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
EP96923887A EP0833607A1 (fr) 1995-06-22 1996-06-21 Composition renfermant du goudron et preparation pharmaceutique et cosmetique contenant cette composition

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19522694A DE19522694A1 (de) 1995-06-22 1995-06-22 Teerhaltige Zusammensetzung und diese enthaltende pharmazeutische und kosmetische Zubereitung
DE19522694.1 1995-06-22

Publications (1)

Publication Number Publication Date
WO1997000666A1 true WO1997000666A1 (fr) 1997-01-09

Family

ID=7764998

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP1996/002710 WO1997000666A1 (fr) 1995-06-22 1996-06-21 Composition renfermant du goudron et preparation pharmaceutique et cosmetique contenant cette composition

Country Status (4)

Country Link
EP (1) EP0833607A1 (fr)
CA (1) CA2225415A1 (fr)
DE (1) DE19522694A1 (fr)
WO (1) WO1997000666A1 (fr)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19834814A1 (de) * 1998-08-01 2000-02-03 Beiersdorf Ag Kosmetische und dermatologische Zubereitungen mit einem wirksamen Gehalt an Gallensäuren, ihren Salzen und/oder ihren Derivaten
IT201700004019A1 (it) * 2017-01-16 2018-07-16 Gk Pharma Consultans Sa Composizione comprendente carnitina, colato di sodio, acetato di sodio ed eventualmente argento per uso nel trattamento di psoriasi, vitiligine e rosacea

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1020613A (en) * 1962-06-06 1966-02-23 Michael Johnathan & Company Lt Improvements in or relating to preparations for the treatment of skin diseases
BE756104A (fr) * 1970-09-14 1971-03-15 Britz Peter Preparation pour le traitement du psoriasis.
WO1994001089A1 (fr) * 1992-07-08 1994-01-20 Dianorm-Geräte G. Maierhofer Liposomes, procede concernant leur fabrication, et leur utilisation dans la fabrication d'un medicament
EP0615746A1 (fr) * 1993-03-15 1994-09-21 Rhone-Poulenc Rorer Gmbh Système aqueux de liposomes et procédé pour la préparation d'un tel système de liposomes

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1020613A (en) * 1962-06-06 1966-02-23 Michael Johnathan & Company Lt Improvements in or relating to preparations for the treatment of skin diseases
BE756104A (fr) * 1970-09-14 1971-03-15 Britz Peter Preparation pour le traitement du psoriasis.
WO1994001089A1 (fr) * 1992-07-08 1994-01-20 Dianorm-Geräte G. Maierhofer Liposomes, procede concernant leur fabrication, et leur utilisation dans la fabrication d'un medicament
EP0615746A1 (fr) * 1993-03-15 1994-09-21 Rhone-Poulenc Rorer Gmbh Système aqueux de liposomes et procédé pour la préparation d'un tel système de liposomes

Also Published As

Publication number Publication date
DE19522694A1 (de) 1997-01-02
EP0833607A1 (fr) 1998-04-08
CA2225415A1 (fr) 1997-01-09

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