EP0440715A1 - Topical ointment - Google Patents

Topical ointment

Info

Publication number
EP0440715A1
EP0440715A1 EP89912240A EP89912240A EP0440715A1 EP 0440715 A1 EP0440715 A1 EP 0440715A1 EP 89912240 A EP89912240 A EP 89912240A EP 89912240 A EP89912240 A EP 89912240A EP 0440715 A1 EP0440715 A1 EP 0440715A1
Authority
EP
European Patent Office
Prior art keywords
weight
percent
cholesterol
ointment
patients
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.)
Pending
Application number
EP89912240A
Other languages
German (de)
French (fr)
Inventor
Gabriele Flender
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.)
Weck Wolfgang Dr-Med
Original Assignee
Weck Wolfgang Dr-Med
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Filing date
Publication date
Application filed by Weck Wolfgang Dr-Med filed Critical Weck Wolfgang Dr-Med
Publication of EP0440715A1 publication Critical patent/EP0440715A1/en
Pending legal-status Critical Current

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Classifications

    • 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
    • A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions

Definitions

  • the invention relates to a topical ointment for the treatment of dermatoses, in particular psoriasis (psoriasis), based on petroleum jelly, jojoba oil and beeswax as an ointment base.
  • psoriasis psoriasis
  • ointments for the treatment of dermatological disorders are known which are applied to the diseased skin areas.
  • ointments are preferably used which contain corticosteroids or salicylic acid as pharmaceutically active substances.
  • corticosteroids or salicylic acid as pharmaceutically active substances.
  • corticosteroids or salicylic acid as pharmaceutically active substances.
  • striae stripes
  • infections worsening and other permanent skin damage telangiectasias.
  • Other possible side effects of conventional ointments and creams are: so-called steroid acne, blotchy to surface skin bleeding and skin ulcers in the area of the application.
  • DE-PS 638 859 discloses a process for the preparation of an aqueous-alcoholic solution which contains cholesterol and is said to be suitable for therapeutic purposes, in particular for the treatment of the scalp.
  • DE-OS 35 26 669 discloses in Example 6 there a moisturizing cream which has petroleum jelly oil and cholesterol as components. Such an emulsion system can be used for the production of cosmetic and pharmaceutical emulsions.
  • DE-OS 31 25 710 describes a cosmetic agent, inter alia in the form of oil-in-water dispersions.
  • Example 4 there relates to a nourishing fluid which also contains cholesterol, among other things.
  • Cosmetic products which contain cholesterol dissolved in oil are also known from FR-PS 9 280 337.
  • DE-OS 37 13 492 proposes a concentrate for the treatment of irritated skin which, in addition to a lipid, water and glycerol, also contains cholesterol.
  • DE-OS 33 19 304 describes a medicament with an antineoplastic effect which, in addition to a lipophilic solvent, also contains cholesterol.
  • CH-PS 1 43 520 describes the cosmetic properties of cholesterol, which is contained in an aqueous or aqueous-alcoholic solution.
  • the object of the present invention is therefore to create a highly effective ointment free of side effects for the treatment of dermatoses, in particular psoriasis.
  • the ointment according to the invention consists of 10 to 50 percent by weight of petroleum jelly, 10 to 50 percent by weight of jojoba oil, 1 to 10 percent by weight of cholesterol, 1 to 10 percent by weight of beeswax or walnut or walnut substitute, and 10 to 40 percent by weight of water.
  • Vaseline is a soft to ointment-like mixture of solid and liquid petroleum hydrocarbons with a melting range between 35 and 60 degrees Celsius.
  • Yellow petroleum jelly (Vaselinum flavum) and bleached white petroleum jelly (Vaselinum album) are commercially available.
  • the white, highly purified petroleum jelly preferred here serves as an inert carrier substance for the ointment.
  • the oil obtained from the jojoba plant also serves, together with the petroleum jelly, as a carrier, but also has a healing effect.
  • the essential pharmaceutically active substance is cholesterol, which is contained in the ointment with a relatively high proportion by weight.
  • Cholesterol as a pharmaceutical active ingredient in a topical ointment for the treatment of dermatoses, in particular psoriasis, is not known from the prior art document dealt with above. Chemically, cholesterol is a steroid but does not have the anti-inflammatory activity of the adrenal gland hormones derived from steroids. This does not mean that their well-known side effects are acceptable.
  • the cholesterol is preferably used in a highly pure form (Cholesterinum purissimum). Cholesterol obtained from wool fat in the form of crystallized powder can be used to produce the ointment.
  • the cholesterol contained in the ointment of the composition according to the invention acts as a lipid emulsifying.
  • the ointment according to the invention thus represents the ideal alternative preparation for the treatment of dermatoses for those patients who cannot tolerate any of the conventional preparations on the skin.
  • the proposed ointment represents a new perspective.
  • the ointment according to the invention is the only option known until now of achieving therapeutic effects without side effects.
  • An ointment consisting of 20 to 40 percent by weight of petroleum jelly, 25 to 45 percent by weight of jojoba oil, 2 to 6 percent by weight of cholesterol, 2 to 8 percent by weight of beeswax, walnut or walnut substitute and 15 to 30 percent has proven particularly effective for the treatment of psoriasis Weight pro there is water.
  • a composition of 25 to 35 percent by weight of petroleum jelly, 35 to 42 percent by weight of jojoba oil, 3 to 5 percent by weight of cholesterol, 4 to 7 percent by weight of beeswax, walnut or walnut substitute and 20 to 25 percent by weight of water is preferred.
  • the ointment is produced in the usual way by carefully mixing the ingredients at elevated temperature.
  • Vaseline, jojoba oil, cholesterol and beeswax are preferably heated together to about 75 degrees Celsius. With careful stirring, a thin, two-phase mixture is formed. Depending on the desired consistency, a corresponding amount of distilled water is added. The subsequent cooling to ambient temperature should be carried out with constant stirring.
  • Devices suitable for this manufacturing process are known and include heat exchangers and mixers.
  • the ointment according to Example 1 above was tested in tests carried out under medical supervision on patients suffering from chronic therapy-resistant psoriasis.
  • a total of 27 patients were treated in a first clinical examination.
  • one half of the patient's body was treated at the affected skin areas with ointment of the composition given in Example 1, while the other half of the body was treated with a salicylic ointment.
  • the ointment was applied twice a day.
  • the success of the treatment was checked by the investigator after one, two and three weeks. Of the 27 patients treated, 24 were free of symptoms after one or two weeks. Although the other three patients showed an effect, there was no complete healing of the skin changes.

Abstract

PCT No. PCT/EP89/01276 Sec. 371 Date Apr. 30, 1991 Sec. 102(e) Date Apr. 30, 1991 PCT Filed Oct. 26, 1989 PCT Pub. No. WO90/04967 PCT Pub. Date May 17, 1990.This invention relates to topical ointments containing cholesterol for the treatment of dermatoses, in particular psoriasis.

Description

Topische Salbe Topical ointment
Beschreibungdescription
Die Erfindung betrifft eine topische Salbe zur Behandlung von Dermatosen, insbesondere Psoriasis (Schuppenflechte), auf der Basis von Vaseline, Jojobaöl und Bienenwachs als Salbengrund¬ lage.The invention relates to a topical ointment for the treatment of dermatoses, in particular psoriasis (psoriasis), based on petroleum jelly, jojoba oil and beeswax as an ointment base.
Es sind vielerlei Salben zur Behandlung dermatologischer Stö¬ rungen bekannt, welche auf die erkrankten Hautstellen aufge¬ tragen werden. Zur Behandlung von Psoriasis und Ekzemen wer¬ den vorzugsweise Salben verwendet, welche Corticosteroide oder Salicylsäure als pharmazeutisch wirksame Substanzen ent¬ halten. Es hat sich jedoch immer wieder gezeigt, daß diese Salben oftmals nicht die gewünschte heilende Wirkung haben. Zudem kommt es bei Patienten, die mit cortisonhaltigen Exter- na behandelt wurden, zu gravierenden Nebenwirkungen, wie zum Beispiel einer nicht heilbaren Hautalterung (Atrophie). Eben¬ falls häufig sind Hautstreifen (Striae), Infektionsverschlim¬ merungen und andere bleibende Hautschäden (Teleangiektasien). Weitere mögliche Nebenwirkungen herkömmlicher Salben und Cre¬ mes sind: sogenannte Steroid-Akne, fleckförmige bis flächen¬ hafte Hautblutungen und Hautgeschwüre im Bereich des Auf¬ trags.Various ointments for the treatment of dermatological disorders are known which are applied to the diseased skin areas. For the treatment of psoriasis and eczema, ointments are preferably used which contain corticosteroids or salicylic acid as pharmaceutically active substances. However, it has been shown time and again that these ointments often do not have the desired healing effect. In addition, there are serious side effects in patients who have been treated with cortisone-containing exteriors, such as incurable skin aging (atrophy). Also common are stripes (striae), infections worsening and other permanent skin damage (telangiectasias). Other possible side effects of conventional ointments and creams are: so-called steroid acne, blotchy to surface skin bleeding and skin ulcers in the area of the application.
Aus der DE-PS 638 859 ist ein Verfahren zur Herstellung einer wässerig-alkoholischen Lösung bekannt, welche Cholesterin enthält und für therapeutische Zwecke, insbesondere für die Behandlung der Kopfhaut, geeignet sein soll. Die DE-OS 35 26 669 offenbart in dem dortigen Beispiel 6 eine feuchtigkeitsspendende Creme, die als Bestandteile Vaseline- Öl und Cholesterol aufweist. Ein solches Emulsionssystem könne zur Herstellung von kosmetischen und pharmazeutischen Emulsionen verwendet werden.DE-PS 638 859 discloses a process for the preparation of an aqueous-alcoholic solution which contains cholesterol and is said to be suitable for therapeutic purposes, in particular for the treatment of the scalp. DE-OS 35 26 669 discloses in Example 6 there a moisturizing cream which has petroleum jelly oil and cholesterol as components. Such an emulsion system can be used for the production of cosmetic and pharmaceutical emulsions.
In der DE-OS 31 25 710 ist ein kosmetisches Mittel, unter anderem in Form von Öl-in-Wasser-Dispersionen, beschrieben. Das dortige Beispiel 4 betrifft ein pflegendes Fluid, das unter anderem auch Cholesterin enthält.DE-OS 31 25 710 describes a cosmetic agent, inter alia in the form of oil-in-water dispersions. Example 4 there relates to a nourishing fluid which also contains cholesterol, among other things.
Kosmetische Produkte, die in Öl gelöstes Cholesterin enthal¬ ten, sind ferner auch aus der FR-PS 9 280 337 bekannt.Cosmetic products which contain cholesterol dissolved in oil are also known from FR-PS 9 280 337.
In der DE-OS 37 13 492 wird ein Konzentrat für die Behandlung gereizter Haut vorgeschlagen, welches neben einem Lipid, Was¬ ser und Glyzerin auch Cholesterin enthält.DE-OS 37 13 492 proposes a concentrate for the treatment of irritated skin which, in addition to a lipid, water and glycerol, also contains cholesterol.
In der DE-OS 33 19 304 ist ein Arzneimittel mit antineo- plastischer Wirkung beschrieben, welches neben einem lipophi- len Lösungsmittel auch Cholesterin enthält.DE-OS 33 19 304 describes a medicament with an antineoplastic effect which, in addition to a lipophilic solvent, also contains cholesterol.
In der CH-PS 1 43 520 finden sich die kosmetischen Eigenschaf¬ ten von Cholesterin, das in einer wässerigen bzw. wässerig¬ alkoholischen Lösung enthalten ist, beschrieben.CH-PS 1 43 520 describes the cosmetic properties of cholesterol, which is contained in an aqueous or aqueous-alcoholic solution.
In "Pharmazeutische Technologie", herausgegeben von Sucker, Fuchs und Speiser, Stuttgart 1978, Seiten 305 - 310, wird Cholesterin als Emulgator in Dermatika erwähnt. Auf Seite 659 findet sich zudem der Hinweis, daß Wollfett auf der Haut ver¬ streichbar ist und einen erweichenden Effekt auf der Horn- schicht bewirkt.In "Pharmaceutical Technology", edited by Sucker, Fuchs and Speiser, Stuttgart 1978, pages 305-310, cholesterol is mentioned as an emulsifier in dermatics. On page 659 there is also a note that wool fat can be spread on the skin and has a softening effect on the horny layer.
Schließlich enthält Janistyn: "Handbuch der Kos etika und Riechstoffe", I. Band, Heidelberg 1969, Seite 538, den Hin¬ weis, daß Jojoba-Öl als Wundheilmittel und als Haaröl Verwen¬ dung findet. Die Gruppe der Patienten, bei denen die eingangs geschilder¬ ten Nebenwirkungen auftreten, nimmt in jüngerer Zeit aufgrund umweltbedingten Belastungen rapide zu. Solche Patienten sind, auch infolge von allergischen Reaktionen auf die üblicherwei¬ se verwendeten Konservierungsstoffe, mit den bekannten pharma¬ zeutischen Externa nicht mehr therapierbar.Finally, Janistyn: "Handbook of Cosmetics and Fragrances", I. Volume, Heidelberg 1969, page 538, contains the information that jojoba oil is used as a wound healing agent and as a hair oil. The group of patients who experience the side effects described at the outset has increased rapidly in recent times due to environmental pollution. Such patients, also as a result of allergic reactions to the preservatives normally used, can no longer be treated with the known pharmaceutical externalities.
Aufgabe der vorliegenden Erfindung ist somit die Schaffung einer hochwirksamen und nebenwirkungsfreien Salbe zur Behand¬ lung von Dermatosen, insbesondere Psoriasis.The object of the present invention is therefore to create a highly effective ointment free of side effects for the treatment of dermatoses, in particular psoriasis.
Die erfindungsgemäße Salbe besteht aus 10 bis 50 Gewichtspro¬ zent Vaseline, 10 bis 50 Gewichtsprozent Jojobaöl, 1 bis 10 Gewichtsprozent Cholesterin, 1 bis 10 Gewichtsprozent Bienen¬ wachs oder Walrat bzw. Walratersatz sowie 10 bis 40 Gewichts¬ prozent Wasser.The ointment according to the invention consists of 10 to 50 percent by weight of petroleum jelly, 10 to 50 percent by weight of jojoba oil, 1 to 10 percent by weight of cholesterol, 1 to 10 percent by weight of beeswax or walnut or walnut substitute, and 10 to 40 percent by weight of water.
Vaseline ist ein weiches bis salbenartig festes Gemisch aus festen und flüssigen Erdölkohlenwasserstoffen mit einem Schmelzbereich zwischen 35 und 60 Grad Celsius. Handelsüblich sind gelbe Vaseline (Vaselinum flavum) und gebleichte weiße Vaseline (Vaselinum album). Die hier bevorzugte weiße, hochge¬ reinigte Vaseline dient als inerte Trägersubstanz der Salbe.Vaseline is a soft to ointment-like mixture of solid and liquid petroleum hydrocarbons with a melting range between 35 and 60 degrees Celsius. Yellow petroleum jelly (Vaselinum flavum) and bleached white petroleum jelly (Vaselinum album) are commercially available. The white, highly purified petroleum jelly preferred here serves as an inert carrier substance for the ointment.
Das aus der Jojoba-Pflanze gewonnene Öl dient ebenfalls, gemeinsam mit der Vaseline, als Trägersubstanz, entfaltet darüber hinaus jedoch auch heilende Wirkung.The oil obtained from the jojoba plant also serves, together with the petroleum jelly, as a carrier, but also has a healing effect.
Wesentliche pharmazeutisch wirksame Substanz ist Cholesterin, das mit einem relativ hohen Gewichtsanteil in der Salbe ent¬ halten ist. Cholesterin als pharmazeutischer Wirkstoff in einer topischen Salbe zur Behandlung von Dermatosen, insbeson¬ dere Psoriasis, ist aus dem vorstehend abgehandelten druck¬ schriftlichen Stand der Technik nicht bekannt. Das Cholesterin gehört chemisch zu den Steroiden, hat jedoch nicht die antiinflam atorische Aktivität der Nebennierenrin- denhormone, die sich aus Steroiden ableiten. Damit sind auch nicht deren hinreichend bekannte Nebenwirkungen in Kauf zu nehmen. Das Cholesterin wird bevorzugt in hochreiner Form (Cholesterinum purissimum) verwendet. Zur Herstellung der Sal¬ be kann aus Wollfett gewonnenes Cholesterin in Form von kri¬ stallisiertem Pulver verwendet werden.The essential pharmaceutically active substance is cholesterol, which is contained in the ointment with a relatively high proportion by weight. Cholesterol as a pharmaceutical active ingredient in a topical ointment for the treatment of dermatoses, in particular psoriasis, is not known from the prior art document dealt with above. Chemically, cholesterol is a steroid but does not have the anti-inflammatory activity of the adrenal gland hormones derived from steroids. This does not mean that their well-known side effects are acceptable. The cholesterol is preferably used in a highly pure form (Cholesterinum purissimum). Cholesterol obtained from wool fat in the form of crystallized powder can be used to produce the ointment.
Weißes oder gelbes Bienenwachs oder auch Walrat bzw. Walrater¬ satz sowie der Anteil an Wasser (Agua dest.) beeinflussen die Konsistenz als gut streichfähige Salbe. Walrat (Cetaceum) ist eine weiße wachsartige Masse, die aus der Kopfhöhle des Pott¬ wals gewonnen wird und chemisch vorwiegend aus Palmetinsäure- acetylester besteht. Heute wird anstelle echten Walrats meist künstlich hergestellter Walratersatz gleicher chemischer Zu¬ sammensetzung verwendet.White or yellow beeswax or also walrate or walrater set and the proportion of water (Agua dest.) Influence the consistency as a spreadable ointment. Walrat (Cetaceum) is a white, wax-like mass, which is obtained from the head cavity of the Pott¬ whale and chemically consists mainly of acetic esters of palmetic acid. Nowadays, instead of real walruses, artificially produced substitutes for the same chemical composition are used.
Das in der Salbe erfindungsgemäßer Zusammensetzung enthaltene Cholesterin wirkt als Lipid emulgierend. Als körperähnliche Substanz führt der Auftrag auf erkrankte Hautflächen nicht zu Unverträglichkeiten oder allergischen Reaktionen. Die erfin¬ dungsgemäße Salbe stellt somit das ideale Ausweichpräparat zur Behandlung von Dermatosen für solche Patienten dar, die keine der herkömmlichen Präparate auf der Haut vertragen. Für die mit den herkömmlichen Präparaten nicht mehr therapierba- ren Patienten stellt die vorgeschlagene Salbe eine neue Per¬ spektive dar. Für eine wachsende Anzahl von Patienten ist die Salbe gemäß der Erfindung die einzige, bisher bekanntgewor¬ dene Möglichkeit, einen nebenwirkungsfreien Therapieerfolg zu erzielen.The cholesterol contained in the ointment of the composition according to the invention acts as a lipid emulsifying. As a body-like substance, application to diseased skin areas does not lead to intolerance or allergic reactions. The ointment according to the invention thus represents the ideal alternative preparation for the treatment of dermatoses for those patients who cannot tolerate any of the conventional preparations on the skin. For the patients who can no longer be treated with the conventional preparations, the proposed ointment represents a new perspective. For an increasing number of patients, the ointment according to the invention is the only option known until now of achieving therapeutic effects without side effects.
Besonders wirksam für die Behandlung von Psoriasis hat sich eine Salbe erwiesen, die aus 20 bis 40 Gewichtsprozenten Vaseline, 25 bis 45 Gewichtsprozent Jojobaöl, 2 bis 6 Ge¬ wichtsprozent Cholesterin, 2 bis 8 Gewichtsprozent Bienen¬ wachs, Walrat oder Walratersatz sowie 15 bis 30 Gewichtspro- zent Wasser besteht. Insbesondere wird eine Zusammensetzung aus 25 bis 35 Gewichtsprozent Vaseline, 35 bis 42 Gewichts¬ prozent Jojobaöl, 3 bis 5 Gewichtsprozent Cholesterin, 4 bis 7 Gewichtsprozent Bienenwachs, Walrat oder Walratersatz und 20 bis 25 Gewichtsprozent Wasser bevorzugt.An ointment consisting of 20 to 40 percent by weight of petroleum jelly, 25 to 45 percent by weight of jojoba oil, 2 to 6 percent by weight of cholesterol, 2 to 8 percent by weight of beeswax, walnut or walnut substitute and 15 to 30 percent has proven particularly effective for the treatment of psoriasis Weight pro there is water. In particular, a composition of 25 to 35 percent by weight of petroleum jelly, 35 to 42 percent by weight of jojoba oil, 3 to 5 percent by weight of cholesterol, 4 to 7 percent by weight of beeswax, walnut or walnut substitute and 20 to 25 percent by weight of water is preferred.
Die Salbe wird in üblicher Weise hergestellt durch sorgfälti¬ ges Mischen der Bestandteile bei erhöhter Temperatur. Vorzugs¬ weise wird Vaseline, Jojobaöl, Cholesterin und Bienenwachs ge¬ meinsam auf etwa 75 Grad Celsius erhitzt. Unter sorgfältigem Rühren entsteht ein dünnflüssiges zweiphasiges Gemisch. Je nach gewünschter Konsistenz wird eine entsprechende Menge de¬ stillierten Wassers hinzugegeben. Die anschließende Abkühlung auf Umgebungstemperatur sollte unter ständigem Weiterrühren erfolgen. Für dieses Herstellungsverfahren geeignete Geräte sind bekannt und umfassen Wärmetauscher und Mischer.The ointment is produced in the usual way by carefully mixing the ingredients at elevated temperature. Vaseline, jojoba oil, cholesterol and beeswax are preferably heated together to about 75 degrees Celsius. With careful stirring, a thin, two-phase mixture is formed. Depending on the desired consistency, a corresponding amount of distilled water is added. The subsequent cooling to ambient temperature should be carried out with constant stirring. Devices suitable for this manufacturing process are known and include heat exchangers and mixers.
Der Salbe der vorgeschlagenen Zusammensetzung müssen keine Konservierungsstoffe zugesetzt werden. Eine ausreichende Haltbarkeit kann beispielsweise schon durch Vakuumverpackung erzielt werden. Für eine längere Haltbarkeit können jedoch auch übliche Konservierungsstoffe zugesetzt werden.No preservatives need be added to the ointment of the proposed composition. Adequate shelf life can already be achieved, for example, by vacuum packaging. However, conventional preservatives can also be added for a longer shelf life.
Die nachstehenden Beispiele erläutern die erfindungsgemäße Zusammensetzung der Salbe:The following examples illustrate the composition of the ointment according to the invention:
Beispiel 1example 1
Vaseline 32 GewichtsprozentVaseline 32 percent by weight
Jojobaöl 38 GewichtsprozentJojoba oil 38 percent by weight
Cholesterin 3 GewichtsprozentCholesterol 3 weight percent
Gelbes Bienenwachs 5 GewichtsprozentYellow beeswax 5 percent by weight
Aqua dest. 22 Gewichtsprozent Beispiel 2Aqua dest. 22 percent by weight Example 2
Vaseline 30 GewichtsprozentVaseline 30 percent by weight
Jojobaöl 40 GewichtsprozentJojoba oil 40 percent by weight
Cholesterin 4 GewichtsprozentCholesterol 4 percent by weight
Walratersatz 6 GewichtsprozentWhale substitute 6 percent by weight
Aqua dest. 20 GewichtsprozentAqua dest. 20 percent by weight
Die Salbe gemäß dem vorstehenden Beispiel 1 wurde in unter ärztlicher Leitung durchgeführten Untersuchungen an Patien¬ ten, welche unter chronischer therapieresistenter Psoriasis leiden, erprobt.The ointment according to Example 1 above was tested in tests carried out under medical supervision on patients suffering from chronic therapy-resistant psoriasis.
Bei einer ersten klinischen Untersuchung wurden insgesamt 27 Patienten therapiert. Dabei wurde jeweils die eine Kör¬ perhälfte des Patienten an den befallenen Hautstellen mit Salbe der in Beispiel 1 angegebenen Zusammensetzung behandelt, während die andere Körperhälfte mit einer salizylhaltigen Salbe behandelt wurde. Der Salbenauftrag erfolgte zweimal täglich. Der Behandlungserfolg wurde jeweils nach einer, zwei und drei Wochen vom Untersuchungsleiter kontrolliert. Von den 27 behandelten Patienten waren 24 bereits nach ein oder zwei Wochen beschwerdefrei. Bei den übrigen drei Patienten zeigte sich zwar eine Wirkung, es kam jedoch nicht zur vollständigen Abheilung der Hautveränderun¬ gen.A total of 27 patients were treated in a first clinical examination. In each case, one half of the patient's body was treated at the affected skin areas with ointment of the composition given in Example 1, while the other half of the body was treated with a salicylic ointment. The ointment was applied twice a day. The success of the treatment was checked by the investigator after one, two and three weeks. Of the 27 patients treated, 24 were free of symptoms after one or two weeks. Although the other three patients showed an effect, there was no complete healing of the skin changes.
An einer zweiten Untersuchung nahmen insgesamt 21 Patienten teil. Davon wurden 12 Patienten mit einer topischen Salbe gemäß Beispiel 1 behandelt, während die übrigen 9 Patienten mit einer topischen Salbe ohne Cholesterinzusatz, ansonsten jedoch gleicher Zusammensetzung, therapiert wurden. Die 9 behandelten Psoriasis-Patienten zeigten am Ende des 3-wöchi- gen Untersuchungszeitraumes keinerlei Änderungen ihres Haut¬ status. Bei den anderen, mit der erfindungsgemäßen Salbe be- handelten 12 Patienten verschwanden die Psoriasis-Efflores- zensen in 10 Fällen.A total of 21 patients took part in a second examination. Of these, 12 patients were treated with a topical ointment according to Example 1, while the remaining 9 patients were treated with a topical ointment without added cholesterol, but otherwise of the same composition. The 9 treated psoriasis patients showed no changes in their skin status at the end of the 3-week examination period. In the other, with the ointment according to the invention in 12 patients, psoriasis efflorescence disappeared in 10 cases.
Während es bei vielen Patienten, die über einen längeren Zeitraum mit steroidhaltigen Salben therapiert werden, zu gravierenden Nebenwirkungen wie Atrophie, Teleangiektasien, Hautverdünnung und Striae im Bereich der betroffenen Haut¬ stellen kommt, konnten derartige negative Begleiterscheinun¬ gen bei den mit der erfindungsgemäßen Salbe behandelten Patienten nicht festgestellt werden. Entsprechend positiv fielen die bei den durchgeführten Untersuchungen festgehalte¬ nen Äußerungen der Patienten über das subjektive Empfinden aus. While there are serious side effects such as atrophy, telangiectasia, skin thinning and striae in the area of the affected skin in many patients who are treated with steroid-containing ointments over a long period of time, negative side effects of this type could occur in those treated with the ointment according to the invention Patients cannot be identified. The statements made by the patients about the subjective feeling in the investigations carried out were correspondingly positive.

Claims

Patentansprüche Claims
1. Topische Salbe zur Behandlung von Dermatosen, insbesondere Psoriasis, auf der Basis von Vaseline, Jojobaöl und Bienen¬ wachs als Salbengrundlage, dadurch g e k e n n z e i c h ¬ e t , daß sie Cholesterin als pharmazeutischen Wirkstoff enthält und sich zusammensetzt aus:1. Topical ointment for the treatment of dermatoses, in particular psoriasis, based on petroleum jelly, jojoba oil and beeswax as an ointment base, due to the fact that it contains cholesterol as a pharmaceutical active ingredient and is composed of:
a) 10 bis 50 Gewichtsprozent Vaseline; b) 10 bis 50 Gewichtsprozent Jojobaöl; c) 1 bis 10 Gewichtsprozent Cholesterin; d) 1 bis 10 Gewichtsprozent Bienenwachs, Walrat oder Walratersatz; e) 10 bis 40 Gewichtsprozent Wasser. a) 10 to 50 percent by weight petroleum jelly; b) 10 to 50 weight percent jojoba oil; c) 1 to 10 weight percent cholesterol; d) 1 to 10 percent by weight beeswax, whale or substitute; e) 10 to 40 weight percent water.
2. Topische Salbe nach Anspruch 1 , dadurch g e k e n n ¬ z e i c h n e t , daß sie zusammengesetzt ist aus:2. Topical ointment according to claim 1, characterized in that it is composed of:
a) 20 bis 40 Gewichtsprozent Vaseline; b) 25 bis 45 Gewichtsprozent Jojobaöl; c) 2 bis 6 Gewichtsprozent Cholesterin; d) 2 bis 8 Gewichtsprozent Bienenwachs, Walrat oder Walratersatz; e) 15 bis 30 Gewichtsprozent Wasser.a) 20 to 40 percent by weight petroleum jelly; b) 25 to 45 weight percent jojoba oil; c) 2 to 6 weight percent cholesterol; d) 2 to 8 percent by weight beeswax, whale or substitute; e) 15 to 30 weight percent water.
3. Topische Salbe nach Anspruch 2, dadurch g e k e n n ¬ z e i c h n e t , daß sie zusammengesetzt ist aus:3. Topical ointment according to claim 2, characterized in that it is composed of:
a) 25 bis 35 Gewichtsprozent Vaseline; b) 35 bis 42 Gewichtsprozent Jojobaöl; c) 3 bis 5 Gewichtsprozent Cholesterin; d) 4 bis 7 Gewichtsprozent Bienenwachs, Walrat oder Walratersatz; e) 20 bis 25 Gewichtsprozent Wasser. a) 25 to 35 percent by weight petroleum jelly; b) 35 to 42 weight percent jojoba oil; c) 3 to 5 weight percent cholesterol; d) 4 to 7 percent by weight beeswax, whale or substitute; e) 20 to 25 weight percent water.
EP89912240A 1988-10-31 1989-10-26 Topical ointment Pending EP0440715A1 (en)

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PT92148B (en) 1995-06-30
ATE84216T1 (en) 1993-01-15
GR3007370T3 (en) 1993-07-30
EP0367103A1 (en) 1990-05-09
DK7191D0 (en) 1991-01-15
WO1990004967A2 (en) 1990-05-17
DE58903222D1 (en) 1993-02-18
DK7191A (en) 1991-06-04
WO1990004967A3 (en) 1990-06-28
JPH0647544B2 (en) 1994-06-22
US5179086A (en) 1993-01-12
EP0367103B1 (en) 1993-01-07
DE3836971C1 (en) 1990-05-17
PT92148A (en) 1990-05-31
ES2053907T3 (en) 1994-08-01
JPH04501415A (en) 1992-03-12
CA2001797A1 (en) 1990-04-30

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