EP0458924A1 - Preparations pharmaceutiques - Google Patents

Preparations pharmaceutiques

Info

Publication number
EP0458924A1
EP0458924A1 EP91900173A EP91900173A EP0458924A1 EP 0458924 A1 EP0458924 A1 EP 0458924A1 EP 91900173 A EP91900173 A EP 91900173A EP 91900173 A EP91900173 A EP 91900173A EP 0458924 A1 EP0458924 A1 EP 0458924A1
Authority
EP
European Patent Office
Prior art keywords
skin
pharmaceutical preparations
preparations
treatment
liposome
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Withdrawn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
EP91900173A
Other languages
German (de)
English (en)
Inventor
Georg Rössling
Andreas Sachse
Rolf Peter Zaumseil
Jutta Riedl
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bayer Pharma AG
Original Assignee
Schering AG
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 Schering AG filed Critical Schering AG
Publication of EP0458924A1 publication Critical patent/EP0458924A1/fr
Withdrawn legal-status Critical Current

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
    • A61Q19/08—Anti-ageing preparations
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • 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
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36—Carboxylic acids; Salts or anhydrides thereof
    • A61K8/362—Polycarboxylic acids
    • 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—Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
    • 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

Definitions

  • the invention relates to pharmaceutical preparations which are characterized by a content of ⁇ , ⁇ -n-alkanedicarboxylic acids with 7 to 13 carbon atoms in liposome dispersions, their physiologically tolerable salts and their esters which can be cleaved by means of skin enzymes.
  • These preparations are preferably prepared in the form of a lotion, a gel or an ointment and are used in particular for the topical treatment of skin diseases.
  • compositions contain the .alpha.,. Omega.-n-alkanedicarboxylic acids having 7 to 13 carbon atoms, their physiologically tolerable salts or their esters cleavable by means of enzymes in the skin - preferably in a concentration of 5 to 30 percent by weight - for the treatment of skin diseases such as for example, acne, hyperpigmentary dermatoses, skin hyperpigmentation, non-inflammatory dermatoses and for the treatment of aging skin (DE-A 28 17 133, EP-A 0229654, EP-A 0336880. US-A 4,292,326, US-A 4,386,104 and UNITED STATES
  • liposomes which are known per se to the person skilled in the art.
  • the ⁇ , ⁇ -n-alkanedicarboxylic acids and liposome-forming substances can be dissolved in an organic solvent, the solution introduced into an aqueous phase and, if appropriate, after homogenization. remove the solvent by distillation. Usually 1 to 10 times the amount by weight of liposome-forming substance per g of active ingredient is used.
  • Suitable liposome-forming substances are in particular phospholipids, such as the sphingomyeline, the plasmalogens, the phosphatidylcholines, the phosphatidylethanolamines, the phosphatidylserines, the phosphatidylinosites and the cardiolipins or else mixtures of these lipids (Dr. Otto-Albert Neumüller: Römpps Chemie-Lexikon; Franck see publishing house , Stuttgart (DE) 2665, 3159, 3920 and 4045) and mixtures of these phospholipids with cholesterol and / or charge carriers such as, for example, stearylamine, phosphatidic acid, stearic acid or dicetyl phosphate.
  • phospholipids such as the sphingomyeline, the plasmalogens, the phosphatidylcholines, the phosphatidylethanolamines, the phosphatidylserines, the phosphatidylinosite
  • phospholipid or mixture based on the aqueous phase preferably 0.1 to 40 percent by weight and in particular 1 to 20 percent by weight of phospholipid or mixture based on the aqueous phase are used. Suitable mixtures contain up to 60 percent by weight of cholesterol and up to 15 percent by weight of charge carriers. Solvents for the phospholipids or mixtures and active ingredients are preferably used
  • the process is advantageously carried out under an inert gas atmosphere, such as nitrogen or argon, and the aqueous liposome solution obtained is stabilized by adding antioxidants, such as sodium ascorbate, tocopherol or sodium hydrogen sulfite.
  • antioxidants such as sodium ascorbate, tocopherol or sodium hydrogen sulfite.
  • aqueous liposome solutions can also contain additional auxiliaries, such as bactericides, preservatives, buffer substances or also active ingredients, in order to produce combination preparations.
  • Combination preparations of this type are, for example, those which additionally contain keratolytics such as salicylic acid or urea.
  • the encapsulation of the active ingredients in liposomes can be carried out under the same conditions as the previously known methods of this type (Pharmacy in our time 11, 1982, 97-108, Pure Appl. Chem., 53, 1981, 2241-2254).
  • the process for encapsulating the antiandrogenic active substances is suitable both for the production of multilamellar liposomes and for the production of unilamellar liposomes.
  • the drug-containing liposomes suspensions thus prepared can be diluted by water and / or thickeners such as hydroxyethyl cellulose, methyl cellulose, Aerosil ® (manufacturer Degussa AG, DE-6000 Frankfurt) Carbopol ® if necessary (BF Goodrich Chem., USA 44131 Cleveland / Ohio), etc. are added to produce spreadable gels.
  • thickeners such as hydroxyethyl cellulose, methyl cellulose, Aerosil ® (manufacturer Degussa AG, DE-6000 Frankfurt) Carbopol ® if necessary (BF Goodrich Chem., USA 44131 Cleveland / Ohio), etc. are added to produce spreadable gels.
  • the optimal active ingredient concentration in the finished pharmaceutical preparations depends on the type of active ingredient and the galenical preparation and must be determined in individual cases using the usual preliminary tests. As a rule, it will be sufficient to use pharmaceutical preparations that use 1 mg to 250 mg of active ingredient per gram of the preparation.
  • Microfluidizer ® the company Micro fluid Corp., USA
  • the liposome dispersion prepared according to Example 1 are freeze-dried.
  • the dried liposome cake is crushed with a cross beater mill and the resulting powder is triturated in portions with an ointment base consisting of petroleum jelly which contains 0.02% 2,6-di-tert-butyl-4-methylphenol (-BHT) as an anti-artidant that the active ingredient concentration in the finished ointment is 100 mg / g.
  • an ointment base consisting of petroleum jelly which contains 0.02% 2,6-di-tert-butyl-4-methylphenol (-BHT) as an anti-artidant that the active ingredient concentration in the finished ointment is 100 mg / g.

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)
  • Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Dermatology (AREA)
  • Birds (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Emergency Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Gerontology & Geriatric Medicine (AREA)
  • Dispersion Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Il est décrit des préparations pharmaceutiques qui sont caractérisées par une teneur en acides alpha,omega-n-alcane-dicarboxyliques avec 7 à 13 atomes de carbone, se trouvant dans des dispersions de liposomes; ces préparations comprennent également les sels physiologiquement compatibles de ces acides, ou leurs esters dissociables par les enzymes de la peau. Ces préparations sont utilisées avantageusement pour le traitement, par application locale, des affections cutanées, ainsi que pour le traitement de la peau ayant subi un vieillissement.
EP91900173A 1989-12-14 1990-12-07 Preparations pharmaceutiques Withdrawn EP0458924A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE3941582 1989-12-14
DE3941582A DE3941582A1 (de) 1989-12-14 1989-12-14 Pharmazeutische praeparate

Related Child Applications (1)

Application Number Title Priority Date Filing Date
EP93250225.5 Division-Into 1993-08-16

Publications (1)

Publication Number Publication Date
EP0458924A1 true EP0458924A1 (fr) 1991-12-04

Family

ID=6395592

Family Applications (1)

Application Number Title Priority Date Filing Date
EP91900173A Withdrawn EP0458924A1 (fr) 1989-12-14 1990-12-07 Preparations pharmaceutiques

Country Status (4)

Country Link
EP (1) EP0458924A1 (fr)
JP (1) JPH04503677A (fr)
DE (1) DE3941582A1 (fr)
WO (1) WO1991008735A1 (fr)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE9312509U1 (de) * 1993-08-20 1993-10-28 Euro-Celtique S.A., Luxemburg/Luxembourg Präparate zur äußeren Verabreichung von antiseptischen und/oder die Wundheilung fördernden Wirkstoffen
DE10131796A1 (de) * 2001-06-30 2003-01-16 Beiersdorf Ag Verwendung von Cardiolipin in kosmetischen oder dermatologischen Zubereitungen

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3542773A1 (de) * 1985-12-04 1987-06-11 Roehm Pharma Gmbh Hautwirksame pharmaka mit liposomen als wirkstofftraeger
FR2591105B1 (fr) * 1985-12-11 1989-03-24 Moet Hennessy Rech Composition pharmaceutique, notamment dermatologique, ou cosmetique, a base de phases lamellaires lipidiques hydratees ou de liposomes contenant un retinoide ou un analogue structural dudit retinoide tel qu'un carotenoide.
FR2627385B3 (fr) * 1988-02-23 1991-08-23 Serobiologiques Lab Sa Composition notamment utile comme matiere de base pour la preparation de compositions pharmaceutiques, notamment dermatologiques et/ou cosmetiques
DE3811081A1 (de) * 1988-03-30 1989-10-12 Schering Ag Verwendung von topisch applizierbaren praeparaten zur behandlung der altershaut

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO9108735A1 *

Also Published As

Publication number Publication date
JPH04503677A (ja) 1992-07-02
WO1991008735A1 (fr) 1991-06-27
DE3941582A1 (de) 1991-06-20

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