NZ623817B2

NZ623817B2 - Composition to be applied to the skin, and use thereof

Info

Publication number: NZ623817B2
Application number: NZ623817A
Authority: NZ
Inventors: Ali Nahavandi
Original assignee: Alnapharm Gmbh & Co Kg
Priority date: 2011-09-30
Filing date: 2012-09-10
Publication date: 2015-11-03

Abstract

Disclosed herein is a composition to be applied to the skin, which comprises a dermatologically compatible vehicle, coconut oil, hazelnut oil and/or avellana oil, and stinging nettle oil. Also disclosed is the use of composition for the treatment of skin diseases such as psoriasis, dermatitis, uriticaria, erythema, lichen planus as well as wounds, burns and corns. caria, erythema, lichen planus as well as wounds, burns and corns.

Description

Composition to be applied to the skin, and use thereof The present invention relates to a composition to be applied to the skin, as well as the use thereof in the treatment of skin diseases.

Psoriasis and neurodermatitis (atopic eczema) are very , chronic, non-contagious, inﬂammatory skin diseases.

Thus for example around 2 to 3% of the population suffer from the most frequently occurring psoriasis vulgaris, with psoriasis pustolosa being likewise well-known. Women and men are affected equally. Psoriasis is a chronic skin disease, which causes lifelong symptoms. Around one in ﬁve psoriasis patients suffer additional arthritic symptoms (psoriasis arthritis) and other chronic inﬂammatory diseases. Because of the interaction of various al pictures and symptoms, life expectancy can be reduced. For both these diseases, the causes and triggers have not yet been conclusively established. s theories are discussed in the literature. Genetic factors, logical changes and/or environmental inﬂuences are said to play a signiﬁcant role.

External inﬂuences can be very diverse. Mechanical, infectious, medication-related, psychological and chronic inﬂammations are seen as r factors.

For psoriasis, one possible explanation for the disease is that the body’s own e system is disrupted because of immune responses. Here, the production of the s that are responsible for the body’s defence responses proceeds unchecked, whilst T-cell production is however a uncontrolled decisive factor in the regulation of the defence system of the skin. In psoriasis, an antibody defence response develops, and not only are exogenous agents attacked, but also those of the body itself. There is a ction in the reproduction of skin cells. Affected skin areas can show severe irritation, ing, silvery-scaly ts, and are thickened in . Some patients have d skin and open wounds.

In healthy skin, the upper layer of the skin (the epidermis) is renewed at regular intervals. Here, new skin cells are formed, which then age and become hardened. The ed skin cells (keratinocytes) are cast off by the body. In the case of a healthy body, this process proceeds almost unnoticed and unseen. In healthy skin, the keratinocytes form a natural tive shield against external environmental inﬂuences. The repair mechanism for healthy skin acts via targeted direction of the keratinocyte ion and activation of the s. By contrast, in the case of psoriasis cell growth is disrupted. The formation of skin cells is heavily accelerated, and a disproportionately large number of cells is formed, The increased keratinocyte ion is ted without any outside action, and continues in an uncontrolled manner. A shiny, silvery- white scaly layer forms on the skin. The lower levels of the skin have enhanced blood circulation on account of the uncontrolled cell growth, and thus appear severely reddened.

The pathological skin changes es) are frequently distributed individually, in an r manner. The skin areas most frequently affected are those which are stretched and are subjected to continual mechanical stress. The skin are as become thickened and form scales. Through the scale formation, the skin becomes hardened and has a tendency towards dryness and wounds.

It is not possible to cure psoriasis. There are many different treatment approaches aimed at soothing the symptoms. The treatments depend on the ty, location and spread of the lesions. Local and systemic treatments are used, and these can be in the form of preparations or they can be physical. Fundamentally, for initial ms and for general care, moisturising skin care products in the form of lotions, creams, oils and ointments are used. If the condition is more advanced, external (topical), internal (systemic) treatments and light are used as forms of treatment. What all these measures have in cornmon is the intention to suppress the scale formation and pment of inﬂammation. The aim is to restore a normal balance of immune response.

However, particularly in the case of systemic therapeutic treatment, it is le for this to have far-reaching effects on the body, and this requires extremely thorough observation and monitoring, since serious complications and side effects can occur.

One task of the present invention is to provide a ition that is to be applied to the skin, which overcomes the disadvantages of the prior art, and which in ular enables an extremely gentle way of restoring the natural protective function of the skin. The intention here is, in particular, to regenerate the natural barrier function of the skin, and to maintain the processes present in healthy skin. Here, the composition according to the invention should preferably be capable of being used to support the therapeutic treatment of psoriasis and neurodermatitis.

This problem is solved by a composition to be applied to the skin, which comprises a dermatologically compatible vehicle, coconut oil, ut oil and/or avellana oil, and stinging nettle oil.

It is preferably envisaged here that the weight ratio of dermatologically compatible vehiclezcoconut oil : hazelnut oil and/or avellana oil : ng nettle oil lies within a range of 1» 50:]-30:i-50:1-10.

Furthermore, it is preferably envisaged that the composition comprises almond oil.

It is preferably envisaged here that the weight ratio of derrnatologically compatible vehicle : coconut oil : hazelnut oil and/or avellana oil : ng nettle oil : almond oil lies within a range of1—50:15021-10zl—20.

Furthermore, it is preferably envisaged that the composition comprises TRF extract (tocotrienol- rich on).

It is particularly preferred here that the weight ratio of vehiclezcoconut zelnut oil and/or avellana oil : ng nettle oil :almond oil : TRF extract lies within a range of 1-50:1-30:1-SO:1- 1020-20: l-ZO.

It can also be envisaged that the composition comprises oil of bitter almonds.

It is preferably envisaged here that the weight ratio of vehiclezcoconut oilzhazelnut oil and/or avellana oil: ng nettle oil: almond oil: TRF extract: oil of bitter almonds lies within a range of 1-50: [-30:1-50:1-10:O-20:0-20:1-10.

It is rmore proposed that the composition comprises natural aromatics, preferably lavender aroma.

For preference, it is envisaged here that the weight ratio of vehicle:coconut oil:hazelnut oil and/or avellana oil: stinging nettle oil: almond oil: TRF extract: oil of bitter almondsznatural ics lies within a range of 1-50:1-30:1-50:l-10:0-20:0—20:0-10:0.1-1.

For ular preference, it is envisaged that the composition comprises: Dermatologically compatible vehicle 1-50% by weight, preferably 30-50% by weight, even more preferably 40.00% by weight, Coconut oil 1-30% by weight, preferably 10-30% by weight, even more preferably 15-25% by weight, even more preferably 17.50% by Weight, Hazelnut oil and/o ravellana oil 1-50% by weight, preferably 10-40% by weight, even more preferably 15-35% by weight, even more preferably 20-30% by weight, even more preferably 25.00% by weight, Stinging nettle oil 1—10% by , preferably 1-7% by weight, even more preferably 3.00% by weight, Almond oil 0-20% by weight, ably 5-15% by weight, even more ably 10.00% by weight, TRF extract (tocotrienol-rich fraction) 0-20% by , preferably 1-10% by weight, even more preferably 2-7% by weight, even more preferably 3.00% by weight, Oil ofbitter almonds 0—10% by weight, preferably 0.5-3% by weight, even more preferably 1.00% by weight, Aromatics 0-1% by weight, preferably 03-07% by weight, even more preferably 0.50% by weight, n all the percentages by weight relate to the total quantity of the composition.

If the composition according to the invention contains dermatologically compatible vehicles, coconut oil, hazelnut oil and/or avellana oil, stinging nettle oil and oil of bitter s, the weight ratios preferably lie within a range of l-50:1-30:1-50:1—1021-10.

It can furthermore be envisaged that it is presented in the form of an ointment, cream, lotion, tincture, oil or gel.

In principle, any dermatologically compatible vehicle that is suitable for the tion of ointments, creams, lotions, tinctures, oils or gel scan be used. Experts in the ﬁeld know of corresponding dermatologically compatibl evehicles.

Here, it can preferably be envisaged that the dermatologically compatible vehicles ed from the : a. Hydrophobic nts for example sing: white Vaseline Ph. Eur, yellow Vaseline Ph. Eur, simple ophthalmic ointment DAC b. Lipophilic gels for example comprising: hydrophobic base gel DAC 0. lipogels for e comprising: lard DAB, white almond oil ointment Fl-I A.4, excipial almond oil ointment . water-absorbing ointments W/O absorption ointments for example comprising: wool wax alcohol ointment DAB (Ungt. Alcohol.

Lanae), Eucerinurn Abhydricum, Ungt. Sorbitansesquioleati, Ungt.

Sorbitanmonostearinic, wool wax-free W/O-absorption ointment, Pionier KWH pharma, emulsifying hydrophobic base gel DAC, emulsifying eye ointment (NRF .20) O/W absorption ointments for example comprising: hydrophilic ointment DAB, Unguentum Cordes Lipophiiic creams for example comprising: n DAB, oily cream (Ungt. Alcoholum Lanae aquosum), Eucerin cum aqua, ent ointment (Ungt. Molle) DAC, hobic base cream DAC (NRF 11.104), hydrophobic tretinoin cream 0.025/0.05 or 0.1% (NRF 11.123), hydrophobic triclosan cream 2% (NRF 11.122), hydrophobic canol cream 5% (NRF 11.119), hydrophobic polidocanol cream 5% with urea 5% (NRF 11.120), Cremor vaselini MB 59, Cremor sorbitansequioleati, Cremor sorbitanmonostearati, W/O lotions . Quasi-W/O creams for example comprising: cold cream (Ungt. s) DAB, cold cream nature] RP Hydrophilic creams for example comprising: nic hydrophilic cream DAB, non—ionic hydrophilic cream SR DAC (NRF 8.27), non-ionic aqueous liniment DAC (NRF 11.92) Hydrophilic lotions for e comprising: hydrophilic base emulsion (NRF 8.25) . Hydrophilic gels for example comprising: hydroxyethyl cellulose gel DAB A second problem is solved by the use of the composition for the treatment of skin es, particular psoriasis, neuroderrnatitis (atopic dermatitis), seborrhoeic dermatitis, urticaria, and corns. erythema and lichen planus, as well as for the treatment of wounds / skin burns Surprisingly, it was found that the composition according to the invention soothes symptoms associated with skin diseases, such as in particular psoriasis and neurodermatitis. er, well as composition ing to the invention accelerates the healing of wounds / skin bums as coms. In the opinion of the inventors, this takes place on account of physical effects. The of the composition is based on natural oils as well as a tional vehicle for the manufacture composition, in order to make this suitable for topical application. In combination, the ingredients have a positive effect on the regeneration of natural skin functions. The soothing the skin, the effect is rather ed through moisturising and caring effects. When applied to composition es protective ﬁlm that protects the affected skin areas from external environmental inﬂuences and supports the body’s own regeneration of skin functions. Through the ion of a protective film, the increased drying of the lesions is stopped, and the water t in the skin layers can be regenerated. In particular, the water content in the corneum skin has natural (Stratum comeum) is a decisive factor for healthy skin. The epidermis of y barrier functions which regulate the water brium, and protect the skin from environmental inﬂuences and harmful substances. However, if the skin is affected by psoriasis or neuroderrnatitis, the natural barrier function is impaired. The composition according to the ion accelerates the restoration of the normal barrier function of the skin. The composition according to the invention ts the skin from harmful environmental inﬂuences and substances that r allergies. The lipid components contained in the composition according the invention also produce a cooling effect, resulting in onal soothing.

The effects of the composition according to the invention mean that the skin can regenerate, formation of the skin’s natural barrier function is supported, and the natural protective barrier function of healthy skin is ed. from the Further features and advantages of the composition according to the invention follow following detailed description of preferred embodiments.

Example production ofa composition as a cream: Into a dermatologically compatible vehicle, in this case for example Eucerin icum, the components, the oils listed in the composition, are added one after another, whilst stirring, and these are worked into the vehicle. The quantitative ratios of the components result from the number of ingredients and the size of the batch. The quantitative tions result from the desired batch size. The weight quantities are calculated from the percentages by weight in relation to the batch size.

Depending on the dermatological vehicle used and the number and quantity ratio of the oils used, the result is an oily or creamy structure of the composition. itions used in percentages by weight, for testing efﬁcacy: anhydricum oil almonds Oil oil nettle Hazelnut exuaCt bitter No. Eucerin coconu}: Stinging TRF Oil _| 40.0 17.5 25.0 DJ '0 O O U1 ._.i O ._n w LI) 0 NO NO O A0 L» O ._. ._. O 4;O IIIIIII 10 HM 00 l0 NO 4:.O N \l b.) O U] 0 NLn ._. EEIEIII N U] O U1 The cream compositions listed in the table were used to test efﬁcacy in 49 ts with psoriasis, 33 patients with neurodermatitis as well as 28 patients for the treatment of wounds / skin burns and corns. The creams with the example itions (see above) were applied 1 — 3 times a day.

The effect of the compositions on the diseased skin was assessed in 49 patients with psoriasis, at intervals of l, 5, 10, 20, 30, 45, 60, 75 and 90 days after the beginning of application.

The results of the effect observed are shown in the following table.

Efﬁcacy in the case ofpsoriasis ment of efficacy: Poor ++++ - -/+ + ++ +++ The effect of the compositions on the diseased skin was assessed, for 33 patients with neurodermatitis, at intervals of 5, 10, 14, 22, 30, 45, 60, 75 and 90 days after the beginning of ation.

The results of the observed effect are shown in the following table.

Efficacy in the case of neurodermatitis Composition II) a e m days 'U V‘) 10 .— 20days --"* -/+ + ---- I -\+ I I Assessment of efﬁcacy: Poor «#131good - -/+ + ++ +-H- ++++ The effect of the compositions on the diseased skin was assessed in 28 patients with wounds / skin burns as well as coms, at intervals of l, 2, 5, 7, 9, 10 and 14 days after the beginning of application.

The s of the effect observed are shown in the following table.

Wounds / skin burns / corns Assessment of efﬁcacy: Poor +4++ - -/+ + ++ +++ From the results for the compositions which are shown above, it can be seen that all the compositions listed bring about soothing in psoriasis, neurodermatitis and in the treatment of wounds / skin burns as well as corns. The composition that is ably envisaged has the most sal and most comprehensive efﬁcacy in all the envisaged areas of greatest, application.

Furthermore, comparison compositions were produced which comprised a dermatologically oil or compatible vehicle (Eucerin anhydricum) and, on the one hand, respectively only hazelnut in the coconut oil, and on the other hand a mixture of hazelnut oil/coconut oil, and their y case of psoriasis patients was observed.

In addition, correSponding trials were carried out based on “vehicle + stinging nettle oil”, “vehicle + stinging nettle oil 3% + t oil” and “vehicle + stinging nettle oil 3% + hazelnut oil”, and the compositions that were produced were ed in respect of their efﬁcacy in the case of sis patients.

Finally, a composition according to the invention, of a dermatologically compatible vehicle, coconut oil, hazelnut oil and stinging nettle oil, was ed and likewise investigated.

Dermatologically compatible vehicle + hazelnut oil A dermatologically compatible e, n anhydricum, was mixed with hazelnut oil in the proportions shown in the table below, with the percentages being percentages by weight. The mode of action of the composition produced in this way in the treatment of psoriasis was tested.

For this, 30 people with mild to moderate psoriasis were treated with this composition over a period of 30 days. In order to enable the treatment to be observed, different vehicle/oil proportions were applied to different areas of skin, and the effect was observed. The results are shown in the following table: Assessment of efﬁcacy: Poor -/+ + ++ +++ ++++ Dermatologically compatible e + coconut oil Analogously to the investigations of a composition of vehicle + hazelnut oil as bed above, corresponding investigations were also carried out for a composition of just the vehicle and coconut oil. The results are shown in the following table: Trial ofvehiclc + coconut oil: Efﬁcacy in the case ofpsoriasis Assessment of efﬁcacy: Poor ry good _ -/+ + ++ +++ ++-H- Vehicle + hazelnut oil + coc0nut oil A composition of vehicle, hazelnut oil and t oil was produced, with the two oils being added to the vehicle in equal proportions by weight. The oil proportions given in the table below are ated from the sum of the individual oil components.

The results are as follows: Trial of vehicle + hazelnut oil + coconut oii: Efﬁcacy in the case ofpsoriasis Assessment of efﬁcacy: Poor#Wgood H—H- - -/+ + ++ +++ Of the compositions tested in this connection, the composition with an oil content of 40% (with the same proportions by weight of ut oil and coconut oil) proved to be the most effective.

Trial of vehicle + stinging nettle oil: Efﬁcacy in the case ofpsoriasis ment of efﬁcacy: Poor _ -/+ + ++ +++ ++++ Trial of vehicle + stinging nettle oi13% + t oil: Efficacy in the case of psoriasis Assessment of efﬁcacy: Poor _ -/+ + ++ +++ Trial of vehicle + stinging nettle oil 3% + hazelnut oil: Efﬁcacy in the case of sis Assessment of efﬁcacy: Poor - -/+ + H +++ ++++ Vehicle + hazelnut oil + t oil + stin in nettle oil accordin to the invention Starting out from the composition, described above, with a 40% oil content (equal proportions of hazelnut oil and coconut oil), stinging nettle oil was added to this composition, so that a composition according to the ion was produced.

The following table shows the results for the treatment of psoriasis with the composition according to the invention: Trial of vehicle + hazelnut oil + coconut oil + stinging nettle oil: cy in the case of psoriasis a) 8 33 8‘ 3 .2 go 0—! V) V) L’) '" 5 E” >\ a % @ é‘ E a: at 'o '0 -o "7-1 '0 '0 o O o o V) U —‘ W v—‘ (\I m 1 + + ++ +++ +++ 2 + ++ +++ +++ ++++ ‘ 3 ++ +++ ++++ ++++ ++++ ‘ ++ +++ ++++ ++++ ++++ ++ +++ +++ ++++ ++++ Assessment of efﬁcacy: Poor Very good - -/+ + ++ +++ ++++ Overall, it is clearly apparent that the composition according to the invention demonstrates clearly improved results in the treatment of psoriasis compared with comparison compositions, after just 30 days. Similar results were also found when the compositions described here were used in the treatment of neurodermatitis or wounds/skin burns/corns.

The features of the invention which are disclosed in the above description and in the claims can be of signiﬁcance both individually and in any combination for the realisation of the invention in its individual embodiments. ses/comprising and grammatical variations thereof when used in this speciﬁcation are to be taken to y the ce of stated features, integers, steps or components or groups thereof, but do not preclude the presence or addition of one or more other es, rs, steps, components or groups thereof.

THE

Claims

CLAIMS NG THE INVENTION ARE AS FOLLOWS:

1. Composition to be applied to the skin, comprising a dermatologically compatible vehicle, coconut oil, hazelnut oil and/or avellana oil, and stinging nettle oil.

2. Composition according to claim 1, further comprising TRF extract (tocotrienol- rich fraction).

3. Composition according to claim 1 or 2, wherein the percentage ratio of dermatologically compatible e to coconut oil to hazelnut oil and/or avellana oil to stinging nettle oil lies within a range of 1-5021—302110.

4. Composition according to any one of the preceding claims, further comprising 10 almond oil.

5. Composition according to claim 4, n the percentage ratio of vehicle to coconut oil to hazelnut oil and/or avellana oil to stinging nettle oil to almond oil lies within a range of1-50zl5021-10: 1—20.

6. Composition according to any one of the preceding claims, further comprising oil 15 of bitter almonds.

7. Composition according to claim 6, wherein the weight ratio of vehicle to coconut oil to hazelnut oil and/or avellana oil to stinging nettle oil to almond oil to oil of bitter s lies within a range of ~3021-50:1—lO:0—20:l-10.

8. Composition according to any one of the preceding claims, r comprising 20 natural aromatics, preferably lavender aroma.

9. Composition according to any one of the ing claims, which comprises: Dennatologically compatible vehicle 1-50% by weight, preferably 30—50% by weight, even more preferably 40.00% by weight, Coconut oil 1-30% by weight, preferably 10-30% by weight, even more preferably 15- 25% by weight, even more preferablyl 7.50% by , 5 ut oil and/or avellana oil 1-50% by weight, preferably 10—40% by , even more preferably 15— 35% by weight, even more preferably 20-30% by weight, even more preferably 25.00% by weight, ‘10 Stinging nettle oil 1—10% by weight, ably 1-7% by weight, even more preferably 3.00% by weight, Almond oil 0-20% by weight, preferably 5-15% by weight, even more preferably 15 10.00% by weight, TRF extract (tocotrienol-iich fraction) 0-20% by weight, preferably 1-10% by weight, even more preferably 2-7% by weight, even more preferably 3.00% by , 20 Oil of bitter almonds 0-10% by weight, preferably 0.5—3% by weight, even more preferably 1.00% by weight, Aromatic substance 0-1% by weight, preferably 03—07% by weight, even more preferably 25 0.50% by weight, wherein all the details of percentages by weight relate to the total quantity of the composition.

10. Composition according to any one of the preceding claims, further comprising ted in the form of an ointment, cream, lotion, tincture, oil or gel. 30

ll. Composition according to any one of the preceding claims, wherein the ologically compatible vehicle is selected from the groups of: a) Hydrophobic ointments b) Lipophilic gels c) lipogels d) water—absorbing ointments W/O absorption ointments e) O/W absorption ointments t) Lipophilic creams g) W/O lotions h) quasi-W/O creams i) hydrophilic creams 10 j) hydrophilic lotions k) hydrophilic gels

12. Use of the composition according to any one of the preceding claims 1 to 11 in the cture of a medicament for the treatment of skin diseases, in particular psoriasis, 15 neuroderrnatitis, atopic dermatitis, hoeic dermatitis, urticaria, erythema and lichen planus, as well as for the ent of wounds / skin burns and corns.

13. The composition according to any one of claims 1 to 11, or the use ing to claim 12, substantially as hereinbefore described. ALNAPHARM GMBH & CO. KG WATERMARK PATENT AND TRADE MARKS ATTORNEYS P38739AU00