DE4006564C2 - Use of hexadecylphosphocholine in the treatment of psoriasis - Google Patents
Use of hexadecylphosphocholine in the treatment of psoriasisInfo
- Publication number
- DE4006564C2 DE4006564C2 DE19904006564 DE4006564A DE4006564C2 DE 4006564 C2 DE4006564 C2 DE 4006564C2 DE 19904006564 DE19904006564 DE 19904006564 DE 4006564 A DE4006564 A DE 4006564A DE 4006564 C2 DE4006564 C2 DE 4006564C2
- Authority
- DE
- Germany
- Prior art keywords
- treatment
- psoriasis
- hexadecylphosphocholine
- active ingredient
- composition
- 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.)
- Revoked
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
- A61K31/66—Phosphorus compounds
- A61K31/683—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
- A61K31/685—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
-
- 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
- A61K31/66—Phosphorus compounds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
- C07H15/02—Acyclic radicals, not substituted by cyclic structures
- C07H15/04—Acyclic radicals, not substituted by cyclic structures attached to an oxygen atom of the saccharide radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
- C07H15/02—Acyclic radicals, not substituted by cyclic structures
- C07H15/04—Acyclic radicals, not substituted by cyclic structures attached to an oxygen atom of the saccharide radical
- C07H15/06—Acyclic radicals, not substituted by cyclic structures attached to an oxygen atom of the saccharide radical being a hydroxyalkyl group esterified by a fatty acid
Description
Die Erfindung betrifft die Verwendung von Hexadecylphosphocho lin bei der Behandlung von Psoriasis; sie betrifft insbeson dere die Verwendung von Hexadecylphosphocholin als Wirkstoff in einer pharmazeutischen Zusammensetzung in einer Menge von 0,01 bis 5 Gew.-%, vorzugsweise von 0,1 bis 1,0 Gew.-%, bezo gen auf die fertige pharmazeutische Zusammensetzung, bei der Behandlung von Psoriasis.The invention relates to the use of hexadecylphosphocho lin in the treatment of psoriasis; it affects in particular the use of hexadecylphosphocholine as an active ingredient in a pharmaceutical composition in an amount of 0.01 to 5 wt .-%, preferably from 0.1 to 1.0 wt .-%, bezo gene to the finished pharmaceutical composition in which Treatment of psoriasis.
In "Angewandte Chemie", 1984, 96(4), S. 247-262, und in "Pharmazie", 1985, 40 (1), S. 702-704, ist die Chemie und Biologie von Phospholipiden mit der allgemeinen Struktur abgehandeltIn "Angewandte Chemie", 1984, 96 (4), pp. 247-262, and in "Pharmazie", 1985, 40 (1), pp 702-704, is the chemistry and Biology of phospholipids with the general structure resolved
die als funktionelle Bausteine biologischer Membranen zur ge zielten Beeinflussung der Blut-Hirn-Schranke und von Tumorge weben bzw. zur Beeinflussung der PAF-induzierten Blutplätt chenaggregation verwendet werden.which act as functional building blocks of biological membranes aimed at influencing the blood-brain barrier and tumor weave or to influence the PAF-induced blood platelets Chen aggregation can be used.
Aus GB-A-2 186 877 sind Phospholipide mit einer ähnlichen Grundstruktur bekannt, die eine Anti-Phospholipase-Aktivität und eine anti-inflammatorische Wirkung gezeigt haben.From GB-A-2 186 877 are phospholipids with a similar Basic structure known to have anti-phospholipase activity and have shown an anti-inflammatory effect.
Aus "Cancer Letters", 33, S. 199-204 (1986), ist es bekannt, daß durch Verabreichung von Alkyl-lysophospholipid-Analoga das Wachstum von Human-Lungenkrebszellen gehemmt werden kann.From "Cancer Letters", 33, pp. 199-204 (1986), it is known that by administering alkyl lysophospholipid analogs Growth of human lung cancer cells can be inhibited.
Aus "Onkologie", 11 (1988), S. 295-296, ist die Verwendung von Hexadecylphosphocholin mit der nachstehend angegebenen Formel, bei dem es sich um ein Phosphorsäureesterderivat handelt, zur Behandlung von Hautmetastasen, die als Folge einer systemi schen Krebserkrankung auftreten, bekannt.From "Onkologie", 11 (1988), pp. 295-296, the use of Hexadecylphosphocholine with the formula given below, which is a phosphoric acid ester derivative for Treatment of skin metastases that result from systemic cancer occur.
Aufgabe der Erfindung war es, einen Wirkstoff zu finden, der bei der Behandlung der Psoriasis erfolgreich eingesetzt werden kann, die bisher als praktisch nicht medikamentös erfolgreich behandelbar angesehen wurde.The object of the invention was to find an active ingredient which successfully used in the treatment of psoriasis can, so far as practically not successful with medication was considered treatable.
Es wurde nun überraschend gefunden, daß diese Aufgabe gelöst werden kann durch Verwendung von Hexadecylphosphocholin der FormelIt has now surprisingly been found that this problem has been solved can be by using hexadecylphosphocholine formula
bei der Behandlung von Psoriasis, insbesondere bei der Behand lung von Psoriasis vulgaris vom chronisch-stationären Typ.in the treatment of psoriasis, especially in the treatment development of chronic stationary psoriasis vulgaris.
Durch die erfindungsgemäße Verwendung von Hexadecylphosphocho lin ist es möglich, die bisher als medizinisch nicht heilbar angesehene Psoriasis innerhalb einer kurzen Zeitspanne von 7 Wochen vollständig zur Abheilung zu bringen, wobei nach weite ren 3 Wochen auch die für die abgeheilte Psoriasis so typi schen Hypopigmentierung vollständig verschwand und nicht wie derkehrte. Nebenwirkungen, insbesondere lokale Rötung, Juck reiz oder Brennen im behandelten Bereich, ließen sich nicht nachweisen.By using hexadecylphosphocho according to the invention lin it is possible to treat those previously considered medically incurable respected psoriasis within a short period of 7 Weeks to heal completely, taking further 3 weeks so typical for the healed psoriasis hypopigmentation completely disappeared and not how returned. Side effects, especially local redness, itching irritation or burning in the treated area, could not be to prove.
Gemäß einer bevorzugten Ausgestaltung der Erfindung wird Hexa decylphosphocholin als Wirkstoff in einer pharmazeutischen Zusammensetzung in einer Menge von 0,01 bis 5 Gew.-%, vorzugs weise von 0,1 bis 1,0 Gew.-%, bezogen auf die fertige pharma zeutische Zusammensetzung, bei der Behandlung von Psoriasis verwendet. Hexadecylphosphocholin ist eine bereits bekannte Verbindung und läßt sich beispielsweise nach bekannten Verfah ren zur Synthese von Phosphorsäureestern leicht herstellen.According to a preferred embodiment of the invention, hexa decylphosphocholine as an active ingredient in a pharmaceutical Composition in an amount of 0.01 to 5 wt .-%, preferably as from 0.1 to 1.0 wt .-%, based on the finished pharmaceutical Zeutische composition, in the treatment of psoriasis used. Hexadecylphosphocholine is one already known Connection and can, for example, according to known procedures Easily produce ren for the synthesis of phosphoric acid esters.
Der erfindungsgemäß verwendete Wirkstoff Hexadecylphosphocho lin ist besonders geeignet zur topischen Anwendung in den üb lichen Dosierungsformen, beispielsweise in Form von Lösungen, Lotionen, Salben, Cremes, Gelen, Sprays und Aerosolen, wobei die Konzentration des Wirkstoffes in dem Bereich von 0,01 bis 5 Gew.-%, vorzugsweise von 0,1 bis 1,0 Gew.-%, bezogen auf die Endformulierung, liegt.The active ingredient hexadecylphosphocho used according to the invention lin is particularly suitable for topical application in practice dosage forms, for example in the form of solutions, Lotions, ointments, creams, gels, sprays and aerosols, being the concentration of the active ingredient in the range from 0.01 to 5 wt .-%, preferably from 0.1 to 1.0 wt .-%, based on the Final formulation, lies.
Es ist möglich, den erfindungsgemäß verwendeten Wirkstoff He xadecylphosphocholin beispielsweise auch in Kombination mit anderen für den gleichen Behandlungszweck bekannten Wirkstof fen anzuwenden, wobei vielfach synergistische Effekte beobach tet werden.It is possible to use the active ingredient He xadecylphosphocholine, for example, also in combination with other active ingredient known for the same treatment purpose fen to use, often observing synergistic effects be tested.
Zum Nachweis der Wirksamkeit des erfindungsgemäß verwendeten
Wirkstoffes Hexadecylphosphocholin bei der Behandlung von Pso
riasis wurde der folgende klinische Test durchgeführt:
Bei einem Patienten wurde eine bestehende Psoriasis vulgaris
vom chronisch-stationären Typ am rechten Unterschenkel in Form
einer typischen erythematosquamösen rundlichen Psoriasisläsion
von 4 cm Durchmesser festgestellt. Diese wurde über 4 Wochen
zweimal täglich dünn mit einer Creme behandelt, welche die
folgende Zusammensetzung hatte:
5 g Hexadecylphosphocholin,
10 g Octyldodecanol,
Basiscreme DAC ad 100 g.The following clinical test was carried out to demonstrate the effectiveness of the active substance hexadecylphosphocholine used in the treatment of psoriasis:
In one patient, an existing chronic stationary psoriasis vulgaris was found on the right lower leg in the form of a typical erythematosquamous round psoriasis lesion with a diameter of 4 cm. This was treated thinly with a cream twice a day for 4 weeks, which had the following composition:
5 g hexadecylphosphocholine,
10 g octyldodecanol,
Base cream DAC ad 100 g.
Die jeweils aufgetragene Dosis betrug 5 bis 10 mg/10 cm². Die Behandlung wurde als Halbseitenbehandlung durchgeführt, die in der Dermatologie als Doppelblindversuch angesehen wird.The dose applied was 5 to 10 mg / 10 cm². The Treatment was carried out as a half-side treatment, which in dermatology is viewed as a double blind test.
Während der Behandlungsphase sowie danach wurde keine weitere topische oder systemische Behandlung durchgeführt.During the treatment phase and afterwards there was no further topical or systemic treatment performed.
Während der Behandlung kam es zu einer deutlichen Rückbildung der Schuppung, der Rötung und der Hautinfiltration der behan delten Läsion, die bereits nach 2 Wochen sichtbar wurde. 3 Wo chen nach Behandlungsende war die Läsion vollkommen abgeheilt, wobei eine für abgehielte Psoriasisläsionen typische Hypopig mentierung der Haut im behandelten Areal noch sichtbar war. Nach weiteren 3 Wochen hatte sich diese Hypopigmentierung zu rückgebildet, so daß sich nun vollkommen normale Haut zeigte. Nebenwirkungen, insbesondere lokale Rötung, Juckreiz oder Brennen im Bereich des behandelten Areals ließen sich nicht nachweisen.Significant regression occurred during treatment scaling, reddening and skin infiltration of the behan delten lesion that became visible after 2 weeks. 3 weeks After the end of treatment, the lesion had healed completely, being a typical hypopig for healed psoriasis lesions mentation of the skin in the treated area was still visible. After another 3 weeks, this hypopigmentation had gotten worse regressed so that now completely normal skin appeared. Side effects, especially local redness, itching or Burning in the area of the treated area was not possible to prove.
Claims (3)
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19883829899 DE3829899C2 (en) | 1988-09-02 | 1988-09-02 | Glycerine glycophosphatides and pharmaceutical compositions containing them for combating skin diseases |
| DE19904006564 DE4006564C2 (en) | 1988-09-02 | 1990-03-02 | Use of hexadecylphosphocholine in the treatment of psoriasis |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19883829899 DE3829899C2 (en) | 1988-09-02 | 1988-09-02 | Glycerine glycophosphatides and pharmaceutical compositions containing them for combating skin diseases |
| DE19904006564 DE4006564C2 (en) | 1988-09-02 | 1990-03-02 | Use of hexadecylphosphocholine in the treatment of psoriasis |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| DE4006564A1 DE4006564A1 (en) | 1991-09-05 |
| DE4006564C2 true DE4006564C2 (en) | 1996-02-01 |
Family
ID=25871813
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE19883829899 Expired - Fee Related DE3829899C2 (en) | 1988-09-02 | 1988-09-02 | Glycerine glycophosphatides and pharmaceutical compositions containing them for combating skin diseases |
| DE19904006564 Revoked DE4006564C2 (en) | 1988-09-02 | 1990-03-02 | Use of hexadecylphosphocholine in the treatment of psoriasis |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE19883829899 Expired - Fee Related DE3829899C2 (en) | 1988-09-02 | 1988-09-02 | Glycerine glycophosphatides and pharmaceutical compositions containing them for combating skin diseases |
Country Status (1)
| Country | Link |
|---|---|
| DE (2) | DE3829899C2 (en) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0419998A3 (en) * | 1989-09-27 | 1991-10-23 | Asta Pharma Aktiengesellschaft | Use of alkylphosphonic acid derivatives for the treatment of psoriasis |
| DE4323174C2 (en) * | 1993-07-10 | 1995-09-14 | Rhone Poulenc Rorer Gmbh | Pharmaceutical and / or cosmetic preparation |
| US5811568A (en) * | 1992-10-08 | 1998-09-22 | Shaman Pharmaceuticals, Inc. | Process for the preparation of mono- and bis(phosphocholine) derivatives which have antifungal activity |
| EP0663816A4 (en) * | 1992-10-08 | 1996-04-03 | Shaman Pharmaceuricals Inc | Novel class of phosphocholine derivatives having antifungal activity. |
| US5681829A (en) * | 1992-10-08 | 1997-10-28 | Shaman Pharmaceuticals, Inc. | Class of phosphocholine derivatives having antifungal activity |
| DE19524515A1 (en) * | 1995-07-05 | 1997-01-09 | Deutsches Krebsforsch | Saccharide conjugates |
| DE19547827A1 (en) * | 1995-12-10 | 1998-07-02 | Reutter Werner | Glycosidic phospholipid(s), especially glucosidic lecithin(s), |
| DE10133202A1 (en) * | 2001-07-07 | 2003-01-16 | Beiersdorf Ag | Topical compositions containing osmolytes, useful e.g. for treating or preventing dry skin or inflammatory conditions of the skin, e.g. eczema, polymorphic light dermatosis or psoriasis |
| WO2005002591A1 (en) * | 2003-07-02 | 2005-01-13 | Fouad Abdelaziz Ahmed Hassanin | Treatment psoriasis, impetigo, tinea by lipositol, cephalin and lecithin |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8604000D0 (en) * | 1986-02-18 | 1986-03-26 | Roussel Lab Ltd | Chemical compounds |
-
1988
- 1988-09-02 DE DE19883829899 patent/DE3829899C2/en not_active Expired - Fee Related
-
1990
- 1990-03-02 DE DE19904006564 patent/DE4006564C2/en not_active Revoked
Also Published As
| Publication number | Publication date |
|---|---|
| DE3829899A1 (en) | 1990-03-08 |
| DE4006564A1 (en) | 1991-09-05 |
| DE3829899C2 (en) | 1994-12-15 |
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