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WO1993020817A1 - Nouvelle utilisation de nitroimidazoles - Google Patents

Nouvelle utilisation de nitroimidazoles Download PDF

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Publication number
WO1993020817A1
WO1993020817A1 PCT/SE1993/000276 SE9300276W WO9320817A1 WO 1993020817 A1 WO1993020817 A1 WO 1993020817A1 SE 9300276 W SE9300276 W SE 9300276W WO 9320817 A1 WO9320817 A1 WO 9320817A1
Authority
WO
WIPO (PCT)
Prior art keywords
compound
formula
treatment
pharmaceutical composition
preparation
Prior art date
Application number
PCT/SE1993/000276
Other languages
English (en)
Inventor
Eilert SJÖLUND
Original Assignee
Hydro Pharma Sverige Ab
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 Hydro Pharma Sverige Ab filed Critical Hydro Pharma Sverige Ab
Publication of WO1993020817A1 publication Critical patent/WO1993020817A1/fr

Links

Classifications

    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles

Definitions

  • the present invention relates to a novel pharmaceutical use of a specific group of imidazoles known per se in th past and also known in a medical context. More particularly, the invention relates to the use of the above compounds for the preparation of a pharmaceutical composition for the treatment of inflammatory and/or infectious skin conditions.
  • Acne vulgaris is a disease state which is distinguished infected and blocked up sebaceous glands with inflammati in the surrounding tissue.
  • Rosacea previously known as acne rosacea, is a disease state which is distinguished by superficial inflamation, especially in the face.
  • rosacea is treated inter alia with metronidazole.
  • Seborrhoea is a disease state which is distinguished by desquamating skin, often in conjunction with itching. In severe cases, a crust is formed which gives rise to mixed infections. Seborrhoeic eczema can be regarded partly as an inflammatory reaction and partly as an infection of Pitosporum ovale. Treatment nowadays is with steroids and in simpler cases with selenium sulphide and metronidazole.
  • the present invention relates to a novel medical use of known pharmaceutically active substances and more particularly to the use of these for the preparation of pharmaceutical composition for the treatment or prophylaxis of inflammatory and/or infectious skin conditions or diseases of the type mentioned above.
  • the compounds used in accordance wi the present invention also enable the elimination or at least reduction of the drawbacks or side effects arising in relation to the known remedies. They are, moreover, o particular interest against a combination of infection a inflammation.
  • compositions for the treatment especially the topical treatment, of inflammatory and/or infectious skin conditions.
  • ethyl(2-(2-methyl-5- nitro-l-imidazolyl)ethyl)sulfone is particularly preferred.
  • the compounds used in the practice of the invention are known per se from the past and therefor can be obtained direct from commercial sources or prepare by techniques that are in themselves known, e.g. by analogy to the preparative methods recited in the above mentioned references.
  • the amount or concentration of the compound used is, of course, selected on the basis of the infectious or inflammatory condition which is to be treated. However, a preferred concentration of the compounds in question is 0.25 to 5 weight percent, calculated on the total weight of the composition, a particularly favoured concentration regime being 0.5 to 2 weight percent, calculated on the same basis.
  • the pharmaceutical composition can be prepared by techniques that are in themselves known using known additives, depending on the desired mode of application.
  • Topical application is considered of primary importance in this connection with the preferred modes of application being creams, gels and emulsions.
  • Preparative methods for these dosage forms are, of course, described in innumerable references and need not be further recited here.
  • a particularly preferred dosage form is one employing "hydrophilic solid crystals". Production of these is described, inter alia, in British patent publication 1,174,672 to which reference is made in this connection.
  • the latter process requires blending a polar lipid which has the capacity to form sai hydrophilic crystals with water or any other polar liquid with corrresponding properties such as glycerol, ethylene glycol or propylene glycol to form a mixture with a concentration of water or other polar liquid of 50 to 59 weight percent.
  • This mixture is brought to a temperature over the "transition temperature" for the particular lipid, this temperature being defined as the lowest temperature at which a lipid particle in contact with excess water or said polar liquid can absorb water or said polar liquid and be converted to cylindrical or spherical particles, "liposomes", exhibiting strong birefringency.
  • the mixture is maintained over said temperature, with agitation, until conversion has taken place and then cooled under continued agitation to room or some other desired temperature, such that surface active solid crystals are formed.
  • the compound of formula (I) used in accordance with the invention can be added before the lipid in question has been converted to liposomes or while it is still in liposome form.
  • Examples of conventional additives which can be incorporated in the pharmaceutical composition used in accordance with the invention are conventional carriers, consistency agents or regulators, pH regulators etc.
  • Particularly preferred embodiments of the invention involve the use of a compound of formula (I) for the treatment of inflammatory and/or infectious skin conditions of the eczema, acne and/or rosacea type.
  • a compound of formula (I) for the treatment of inflammatory and/or infectious skin conditions of the eczema, acne and/or rosacea type.
  • One type of eczema which has been treated effectively in this way is the seborrhoeic variety.
  • the use of the invention can be employed against conditions having their origin in an infectious and an inflammatory component.
  • a cream preparation containing the following components was prepared:
  • Buffering systems, tensides and consistency agents can be incorporated in the cream for cosmetic purposes.
  • the cream was prepared in the following manner. The ingredients were mixed and the mixture heated to 70°C. After 15 minutes at this temperature, the mixture was cooled to room temperature at a rate of 1 - 3°C per minute.
  • a gel containing the following ingredients was prepared in the same manner as described in Example 1.
  • the gel was given to patients with seborrhoeic eczema on the scalp. Earlier therapy with known agents had not had any result. When using the gel of Example 2, the patients became symptom free with 2 to 3 applications per week.
  • the liquid paraffin was mixed with the sorbitan mono- oleate, heated to 70°C and tinidazole then mixed in.
  • the polyoxyethylene (20) stearate, water and carbomer were mixed, homogenized and heated to 70°C. Under vigourous homogenizing, the different partial mixtures were mixed and the temperature allowed to drop to room temperature.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Composés de formule (I) dans laquelle R représente: a) -(CH2)mSO2(CH2)nCH3 où m = 2-3 et n = 0-1; ou b) -(CH2)mSO2CH(CH3)2 où m = 2-3. Ce composé entre dans la préparation d'une composition pharmaceutique pour traiter, notamment en traitement local, des troubles inflammatoires et/ou infectieux de la peau.
PCT/SE1993/000276 1992-04-14 1993-03-31 Nouvelle utilisation de nitroimidazoles WO1993020817A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
SE9201188-1 1992-04-14
SE9201188A SE506509C2 (sv) 1992-04-14 1992-04-14 Användning av imidazoler för framställning av en farmaceutisk formulering för behandling av inflammatoriska och/eller infektiösa hudsjukdomar

Publications (1)

Publication Number Publication Date
WO1993020817A1 true WO1993020817A1 (fr) 1993-10-28

Family

ID=20385961

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/SE1993/000276 WO1993020817A1 (fr) 1992-04-14 1993-03-31 Nouvelle utilisation de nitroimidazoles

Country Status (3)

Country Link
AU (1) AU3964093A (fr)
SE (1) SE506509C2 (fr)
WO (1) WO1993020817A1 (fr)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998027960A3 (fr) * 1996-12-20 1998-09-11 Bioglan Ireland R & D Ltd Composition gelifiee a base de nitro-imidazole
US5972993A (en) * 1998-03-20 1999-10-26 Avon Products, Inc. Composition and method for treating rosacea and sensitive skin with free radical scavengers
EP1206937A4 (fr) * 1999-07-16 2005-01-19 Shoei Co Ltd Preparations de nitroimidazole a usage externe pour traiter la dermatose

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1988006888A1 (fr) * 1987-03-20 1988-09-22 Curatek Pharmaceuticals, Inc. Nouvelles formations topiques a base de metronidazole et leurs utilisations therapeutiques
WO1992003133A1 (fr) * 1990-08-16 1992-03-05 Bloom, Leonard Traitement local de la blepharite

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1988006888A1 (fr) * 1987-03-20 1988-09-22 Curatek Pharmaceuticals, Inc. Nouvelles formations topiques a base de metronidazole et leurs utilisations therapeutiques
WO1992003133A1 (fr) * 1990-08-16 1992-03-05 Bloom, Leonard Traitement local de la blepharite

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998027960A3 (fr) * 1996-12-20 1998-09-11 Bioglan Ireland R & D Ltd Composition gelifiee a base de nitro-imidazole
US6348203B1 (en) * 1996-12-20 2002-02-19 Biogland Ireland (R&D) Limited Nitroimidazole gel composition
US5972993A (en) * 1998-03-20 1999-10-26 Avon Products, Inc. Composition and method for treating rosacea and sensitive skin with free radical scavengers
EP1206937A4 (fr) * 1999-07-16 2005-01-19 Shoei Co Ltd Preparations de nitroimidazole a usage externe pour traiter la dermatose

Also Published As

Publication number Publication date
SE506509C2 (sv) 1997-12-22
SE9201188D0 (sv) 1992-04-14
SE9201188L (sv) 1993-10-15
AU3964093A (en) 1993-11-18

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