WO2017137887A1

WO2017137887A1 - Composition of asphodelus root extracts

Info

Publication number: WO2017137887A1
Application number: PCT/IB2017/050646
Authority: WO
Inventors: Pietro CECCOBELLI; Claudio MIRABELLA
Original assignee: Ceccobelli Pietro; Mirabella Claudio
Priority date: 2016-02-11
Filing date: 2017-02-07
Publication date: 2017-08-17
Also published as: ITUB20160655A1

Abstract

Process for obtaining an alkalized composition with Asphodelus root extract base, said process providing for the treatment of the finely-divided root of the plant of the Asphodelus genus with a strong mineral base and deliquescent or with a solution having a pH comprised between 10 and 14, said plant root of the Asphodelus genus comprising substances such as: water, levulose, insulin, aloe emodin, chlorogenic acid, isochlorogenic acid, luteolin, luteoside, isoorientin, vitexin, anthraquinone c-glycosides, anthrone c-glycosides, bianthrones, c-glycosides.

Description

"Composition of Asphodelus root extracts"

Description

Field of the art

The present invention refers to the medical field. More in detail the invention refers to a process for obtaining a composition comprising components of plant origin for use in specific therapeutic treatments. In particular, for use in the treatment of pathologies of skin tissues, of skin adnexa such as hair, nails and mucous membranes.

State of the art

The use of remedies of natural origin, in particular of plant origin, for the treatment of pathologies of various nature represents a curative approach in the medical science field that has been known since antiquity. For example, and consistent with the field of application of the present invention, the use of plant remedies for the treatment of dermatological pathologies such as dermatitis undoubtedly represents one of the most well-known and effective in the field.

Dermatitises are a group of many different pathologies which affect the skin, involving skin manifestations that range from simple redness to scaling, depending on the gravity. The cause of dermatitises is not always well known, even if the pathology is often attributable to an immune response with inflammatory reaction of the skin. Generally, the causes of dermatitis can be of chemical nature, e.g. it can be caused by contact with substances such as detergents or diluents or perfumes, etc.; or of physical nature, e.g. it can be caused by burns or abrasions; or of microbial nature, e.g. of viral, bacterial, protozoic or mycotic nature; or of parasitic nature due for example to skin parasites. Alternatively, it can be a consequence of a skin disease, with allergic causes such as non-topical dermatitis or neurodermatitis, or autoimmune causes such as psoriasis.

The natural remedies for the treatment of these pathologies are generally grouped together in three large categories: those of the tampon remedies such as, by way of a non-limiting example, chamomile, to be applied on a sterile gauze previously moistened with chamomile before then tamponing the irritated skin zone, or blueberry which, due to its properties for the epidermal microcirculation, can help reduce redness and wounds without the risk of scars. Another category is that of the spreadable remedies such as coconut oil which, due to its antibacterial and antimycotic properties, can help reduce dermatitis of infectious nature. Another category is that of the food remedies, such as foods rich with vitamin E which is naturally contained in wheat, corn, peanut butter, sunflower seeds and in many other foods. Other substances of plant origin that are known for the curative effects for dermatitises, for example against non-topical dermatitis and in particular against eczema are the following: Liquorice (glicyrrhiza glabra), known for its anti-inflammatory properties. It acts in a manner analogous to corticosteroids and also inhibits the breakage of Cortisol, which is a corticosteroid produced by the human body. Burdock (arctium lappa), a plant used for different skin disturbances. It is rich with minerals and contains inulin which is a fiber that facilitates the destruction of many types of skin bacteria, whose presence would aggravate the eczema. Dandelion (taraxacum officinale), a plant which contains inulin and is also rich with vitamins and minerals, some of which very healthy for the skin. Gotu kola (centella asiatica), a plant that is indicated in the treatment of skin wounds and also used for inflammations. Echinacea (echinacea purpurea, e. angustigolia, e. purpurea), a wild flower that contains active principles curative for skin infections and inflammations as well as substances which stimulate the reformation of the connective tissue. Comfrey (symphitum officinale), a plant that contains allantoin which is a known lenitive for the skin. More specifically, allantoin is capable of increasing the elasticity of the skin, facilitating the rebirth of cells and decreasing the wound healing times. Coleus (coleus foskohli) is a plant that reduces the production of histamine and of all the other chemical inflammatory substances. Those listed above are only some of the plant species whose utility is known in the treatment of dermatological pathologies.

Studies conducted in the course of the conception of the present invention have revealed that there are many different plant species whose properties can be effective in the treatment of dermatological pathologies. A plant species known as Asphodelus was found to be of particular interest. This is a genus of plants of the Liliaceae family which comprises various herbaceous species, generically known with the trivial name of Asphodelus. They are distributed in Europe, above all in Mediterranean regions and are found up to a height of 1000 m above the sea. They are herbaceous plants with perennial, fasciculated and enlarged tuberous roots, joined together in the apical part, from which leaves and flowers depart. The latter develop in racemose inflorescence, more or less branched, corresponding with the different species varieties. Asphodelus is a plant known since antiquity. It was in fact well- known to the Greeks, as a species for food use. The therapeutic use instead stems from more recent times, and substantially arose for the treatment of ulcers and scabies.

At any rate, Asphodelus has never been used on large scale for therapeutic purposes, but rather it is a plant well-known in cosmetics. Its use for therapeutic purposes substantially provides for its external administration. Its lenitive, emollient, refreshing and decongestant properties therefore render it useful for the treatment of skin rashes, for reducing the inflammation thereof, and for the treatment of solar erythema. Such properties have been known for some time and have been exploited for the implementation of methods for preparing compositions for their use in the medical field and in particular, but not exclusively, in the dermatological field.

For example, the document GR2008100079 describes a process for preparing an ointment substantially derived from the peeled roots of Asphodelus. The method more specifically regards an Asphodelus root extract with the addition of a quantity of olive oil and pure wax for obtaining a cream for treating wounds.

Otherwise, the document US005091181 describes a pharmaceutical composition comprising a quantity of an edible part of Asphodelus for the treatment of human and animal subjects having white blood cell deficiency.

Additionally, the document US005667783 describes a method for the treatment of HIV- positive subjects with a composition comprising extracts of plants of the Asphodelus genus in addition to other components.

The document CH671336 instead describes a phytopharmacological topical composition for the treatment of burns and erythemas of the skin. More specifically, such topical composition is obtained by means of boiling and filtration of the aqueous solution of active principles and of essences of officinal herbs such as: fresh root of Asphodelus Verus Albus, leaves of Rosmarinus Officinalis, leaves of Salvia Officinalis, leaves of Chelidonium Maius L. Such composition has application in the treatment of skin for treating burns and erythemas.

Additionally, the document CA2377118 describes a composition for use in the treatment of psoriasis. Such composition is a derivative of Asphodelus Microcarpus and includes 3- methylanthralin, chrysophanol, aloe-emodin, aloe-emodin monoacetate, and/or derivates of these substances. Said composition is prepared by extracting a liquid from the roots of Asphodelus Microcarpus and mixing the liquid with acetic acid. Such document also describes the method for treating psoriasis by applying said composition on the affected skin area with a frequency of one application per day for a period comprised between 14-56 days. Finally, the document EP 0995443 describes a preparation comprising fluids of the roots of Asphodelus albus for the treatment of burns, abrasions and herpes (both Herpes zoster and Herpes simplex).

In light of the abovementioned prior art documents, it is therefore evident that the capacity of derivatives of Asphodelus to treat skin lesions of various nature, increasing the immune defenses of the organism as well as the cellular regeneration of the zone affected by the lesion, is known.

Nevertheless, up to now, all the formulations prepared by suitably working various parts of plants of the Asphodelus genus have not had high commercial interest, probably due to the cost associated with the preparation of the formulation as well as due to the effectiveness of their use.

For such purpose, the object of the present industrial invention patent application, described in detail hereinbelow, is to propose a new process for obtaining a particular composition with Asphodelus root extract base for use in the treatment of skin lesions and/or rashes of various nature. Such composition, resulting from the present process, due to the combination of the substances present therein and in particular due to the quantities thereof present in active form for the provided treatment, is particularly effective in the process of healing said skin lesions and/or rashes.

Surprisingly, the present composition has proven useful in the treatment of other problems in the medical field, so that the object of the present industrial invention patent application is also that of describing and claiming the present composition for further medical uses.

Description of the invention

The present industrial invention patent application refers to a process for obtaining an alkalized composition comprising active principles of natural origin for its use in the medical field and in particular in the dermatological field. More in detail, the composition obtainable with the present process comprises the active principles extractable from the roots of the Mediterranean Asphodelus plant, independent of the specific herbaceous species to which it belongs. More in detail, the composition is obtainable and hence results from the treatment of starting substances comprised in the plant root of the Asphodelus genus, which include: water, levulose, insulin, aloe emodin, chlorogenic acid, isochlorogenic acid, luteolin, luteoside, isoorientin, vitexin, anthraquinone c-glycosides, anthrone c-glycosides, bianthrone c-glycosides. With respect to the known compositions which use the derivatives of Asphodelus for medical uses, the composition resulting from the present process comprises a greater quantity of active principles coming from Asphodelus, i.e. it lacks other additional active principles of natural and/or synthetic origin. The composition was prepared in various formulations defined specifically for the provided medical use. More in detail, the present process, in all variants thereof relative to the obtainment of a composition specific for a certain medical use, provides for treating the root of the plant of the Asphodelus genus with an alkaline agent. In particular, the fresh root of Asphodelus was treated with agents with different acid/base behavior and which have a pH value comprised between 8 and 14, preferably between 9 and 14 and still more preferably between 10 and 14, unlike the known compositions resulting from processes that provide for the use of agents with acidic behavior, such as acetic acid. More in detail, in the course of the tests executed for obtaining various preparations of the composition with Asphodelus root base, the procedure was conducted by treating the fresh and dry root of Asphodelus, in one case with an alkaline substance such as a strong mineral base and deliquescent in order to obtain an alkaline preparation of Asphodelus root, in another case with an alcoholic solution, slightly basic, in order to obtain a mother tincture and an officinal tincture and, in still another case, with an aqueous solution with slightly alkaline pH in order to obtain a decoction. Surprisingly, it was found that the preparation obtained from the treatment of the root of the plant with a strong mineral base and deliquescent was particularly effective in the treatment of various pathologies, such as in the treatment of lesions and/or pathologies of the skin tissues, in particular in the treatment of mycosis and onychomycosis. At any rate, all the compositions deriving from the present process, which uses agents with basic behavior, are more effective than the known compositions resulting from the treatment with acidic agents for the same medical uses. It should be indicated that, conventionally, the tinctures, whether mother or officinal, are prepared by treating the root of the herbaceous species of interest with an alcoholic solvent. Depending on whether the fresh root of the plant or the dry root of the plant is used, one obtains respectively a mother tincture or an officinal tincture. In the course of the tests conducts for obtaining the aforesaid preparations, it was thought to use an alkalizing agent for treating the root and for verifying if the effectiveness of the treatment depended on the pH of the product. As anticipated, the alkaline preparation, obtained with the present process by treating the fresh root of Asphodelus with an alkaline agent such as a strong mineral base and deliquescent, was particularly effective not only with respect to the other preparations known in the literature - which in addition to the substances naturally present in Asphodelus comprise further substances and/or additional active principles coming from other sources - but also with respect to the other preparations that are the object of the present application, thus showing an effective dependence of treatment effectiveness on the pH of the agents used in the steps of the present process! Probably, such behavior derives from the fact that in a basic environment, the functional groups and/or active sites of the active principles, and of the molecules in general 0150 present in the root of the Asphodelus plant - have a distribution of the charges such to facilitate their mutual interaction in terms of orbital overlaps, hence to facilitate the formation of bonds, and the consequent formation of the species actually responsible for therapeutic action in the treatment of many different problems, such as the aforesaid that are verifiable at the skin.

Description of the preferred embodiments

In the various embodiments, the process according to the present invention provides for the treatment of the plant root of the Asphodelus genus with different alkaline agents for obtaining the same number of different preparations:

A first alkaline preparation was obtained by treating the fresh root of Asphodelus with NaOH in pellets. In any case, also other strong mineral bases and deliquescents can be employed. In one experiment, 1kg of fresh root of Asphodelus was treated with lOOg of NaOH in pellets and subjected to pressing. The pulp thus obtained was left to rest for seven days.

A second preparation is in the form of an alkalized alcoholic solution of fresh root and in particular in the form of mother tincture: for example, in a further experiment 300g of fresh root were treated with ½ liter of ethanol admixed with a negligible volume of an aqueous alkaline solution, the treated root was then left to rest per 5 days and, subsequently, was subjected to pressing;

A third preparation of the composition is in the form of an alkalized alcoholic solution of dry root, hence in the form of an officinal tincture: for example, in a further experiment, 20g of dry root were treated with ½ liter of pure ethanol and 35g of a slightly alkaline aqueous solution. The root thus treated was therefore left to rest for a period of time of three weeks. Subsequently, the alkalized alcoholic extract was then recovered in order to be administered for internal use with the addition of water; A fourth preparation of the composition is in decoction form: for example, in a further experiment, 5g of fresh root or of dry root - in accordance with the uses - were treated with a liter of an aqueous alkaline solution and all was brought to boiling. (The administration is provided upon dilution of the alkaline decoction with water)

A fifth preparation of the composition is in oily form: 300g of dry root were previously treated with NaOH in pellets and subjected to pressing. Subsequently, the resulting pulp was mixed with 1 liter of olive oil. At any rate, other non- allergenic vegetable oils or non- allergenic synthetic oils can be employed.

Finally, a further preparation provides for the existence of the composition in the form of admixed activated carbon. Such preparation is obtained by subjecting to pressing the plant root of the Asphodelus genus with an aqueous alkaline solution and activated carbon.

The main indications of the present alkalized composition provide for its use in the treatment of pathologies and problems such as: dermatosis, eczema, mycosis, burns, onychomycosis, ephelides, warts, verrucae, alopecia, vitiligo, gingivitis, verrucous nevus, papillitis, acne, herpes labialis, insect bites, condyloma, herpes zoster, wounds and as anti-pruriginous agent. The present composition, for the above-listed indications, is preferably used in the form of alkalized alcoholic extract, both of fresh root and dry root, hence both in the form of a mother tincture and in the form of an officinal tincture, both alkalized and in the form of an oily preparation comprising the dry root of the plant previously subjected to pressing with NaOH in pellets.

Other secondary indications of the composition provide for its use in the therapeutic treatment of nerves and articulations, otitis, scabies, as antiseptic and anthelmintic agent, as reconstituent and for eliminating toxins.

The present composition, for these further and above-listed indications, is preferably used in the form of alkaline pulp seeds, of alkalized decoction, of activated carbon admixed with aqueous alkaline solution and in the form of alkalized alcoholic extract. More specifically, said composition is used in pulp form for the therapeutic treatment of nerves and articulations, in decoction form when assumed as reconstituent, in the form of admixed activated carbon when indicated as toxin purifying agent and in the form of alkaline alcoholic extract also when indicated for scabies, as antiseptic and anthelmintic agent as well as for the abovementioned uses.

Typically, the preparations in pulp seeds and alkaline alcoholic extracts are employed for external use, while the preparations of activated carbon and of decoctions are for internal use.

In addition, in some cases, the alkalized alcoholic solution of fresh root, hence the officinal tincture, is also adapted to be used for internal use upon dilution with water.

As mentioned above, the plant root - based composition of the Asphodelus genus has proven particularly effective in particular treatments. Specifically, the composition in the form of alkalized alcoholic extract has proven particularly effective in the treatment of alopecia in the treatment of mycosis, condyloma, herpes, abscesses, onychomycosis and aphta. The effectiveness of the treatment for the relative above-listed uses has also proven particularly high when the present composition is in oil form, and more precisely oil comprising the composition obtained from the pressing of the root of the plant with a strong mineral base and deliquescent like NaOH. In particular the composition in oily form has proven particularly effective in the treatment of mycosis and onychomycosis, herpes, condyloma, verrucae and abscesses, perionychia (felon) and rhinosinusitis by means of aerosol. For the treatment of rhinosinusitis, the composition with Asphodelus root base, resulting from the present process, can also be administered in powder form.

As repeated several times above, in all embodiments thereof the composition resulting from the present process has proven to be particularly effective due to the fact that it arises from the treatment of the root of the plant with an alkaline agent, it too having an alkaline pH, comprised between 8 and 14, and preferably between 10 and 14. It is assumed that the greater effectiveness of the treatment of the aforesaid pathologies and problems, verifiable following the addition of NaOH on the finely-divided fresh root of Asphodelus, is probably due to the fact that NaOH catalyzes the formation of the species that are actually active in the aforesaid treatments and which up to now were obtained in neutral setting or with acidic catalysis. In any case, even when the treatment is with a solvent with neutral pH such as water or which is slightly acidic, the present composition with respect to those known still has greater effectiveness since the active species present therein are administered as is - hence resulting more concentrated with respect to analogous substances present in compositions in which other natural substances are also added that are curative for the pathologies mentioned in the present description. In all embodiments thereof corresponding to the variants of the present process, the resulting composition can comprise pharmaceutically-acceptable excipients and can also be present in the following formulations: solution, ointment, oil/cream, powder and spray/foam.

Claims

1. Process for obtaining a composition with Asphodelus root extract base, said process providing for the treatment of the finely-divided root of the plant of the Asphodelus genus with a strong mineral base and deliquescent or with a solution having a pH comprised between 10 and 14, said plant root of the Asphodelus genus comprising substances such as: water, levulose, insulin, aloe emodin, chlorogenic acid, isochlorogenic acid, luteolin, luteoside, isoorientin, vitexin, anthraquinone c-glycosides, anthrone c-glycosides, bianthrones, c-glycosides.

2. Process according to the preceding claim wherein IKg of finely-divided fresh root of the plant of the Asphodelus genus is subjected to pressing with lOOg of NaOH in pellets.

3. Process according to claim 1 wherein the fresh root of the plant of the Asphodelus genus is treated with a volume of ethanol previously admixed with a negligible volume of an aqueous alkaline solution, said Asphodelus root being subsequently left to rest and subsequently subjected to pressing.

4. Process according to the preceding claim wherein 300g of fresh root of the plant of the Asphodelus genus are treated with ½ liter of ethanol with a negligible volume of an aqueous alkaline solution, subsequently left to rest for five days and subsequently subjected to pressing.

5. Process according to claim 1 wherein the dry root of the plant is treated with an alcoholic solution of alkalized ethanol in order to obtain an alcoholic extract that is a precursor of a decoction, said alcoholic extract being subsequently diluted with water.

6. Process according to the preceding claim wherein 20g of dry root of Asphodelus are treated with ½ liter of pure ethanol and 35g of an aqueous alkaline solution, and subsequently left to rest for a period of time of three weeks, said process providing for the recovery of the alcoholic extract of the Asphodelus root thus treated and the dilution of said alcoholic extract with water.

7. Process according to claim 1 wherein the fresh or dry root of the Asphodelus plant is treated with an aqueous alkaline solution, said process subsequently providing for the heating of the aqueous alkaline solution comprising the fresh or dry root of the plant up to boiling in order to obtain a decoction.

8. Process according to the preceding claim wherein 5g of fresh or dry root of the Asphodelus plant are treated with 1 liter of an aqueous alkaline solution, said process providing for the heating of the aqueous alkaline solution containing the fresh or dry root of the Asphodelus plant up to boiling in order to obtain a decoction.

9. Process according to claim 1 wherein the dry or fresh root of the plant of the Asphodelus genus is subjected to pressing with NaOH in pellets and subsequently mixed with a non- allergenic oil, said oil being a natural vegetable or synthetic non- allergenic oil.

10. Process according to the preceding claim wherein the non-allergenic oil is olive oil.

11. Process according to claim 1 wherein the fresh or dry root of the plant of the Asphodelus genus is treated with an aqueous alkaline solution and subsequently subjected to pressing with activated carbon in order to obtain activated carbon admixed with Asphodelus root.

12. Root extract - based composition of the plant of the Asphodelus genus comprising water, levulose, insulin, aloe emodin, chlorogenic acid, isochlorogenic acid, luteolin, luteoside, isoorientin, vitexin, anthraquinone c-glycosides, anthrone c-glycosides, bianthrones, c- glycosides characterized in that it has a pH comprised between 10 and 14, said composition being obtainable with the process according to any one of the preceding claims.

13. Alkalized composition of plant root extracts of Asphodelus according to the preceding claim characterized in that it appears in the form of pulp seeds, said composition being obtainable with the process according to claim 2.

14. Alkalized composition of plant root extracts of Asphodelus according to claim 12 characterized in that it appears in the form of mother tincture, said composition being obtainable with the process according to claims 3 and 4.

15. Alkalized composition of plant root extracts of Asphodelus according to claim 12 characterized in that it appears in the form of officinal tincture, said composition being obtainable with the process according to claims 5 and 6.

16. Alkalized composition of plant root extracts of Asphodelus according to claim 12 characterized in that it appears in decoction form, said composition being obtainable from the process according to claim 7, 8.

17. Alkalized composition of plant root extracts of Asphodelus according to claim 12 characterized in that it appears in oily form, said composition comprising a vegetable or synthetic non- allergenic oil, said composition being obtainable with the process according to claims 9 and 10.

18. Alkalized composition of plant root extracts of Asphodelus according to claim 12 characterized in that it appears in the form of activated carbon admixed with substances present in the Asphodelus root, said composition being obtainable with the process according to claim 11.

19. Composition according to claim 12 characterized in that it comprises pharmaceutically- acceptable excipients and in that it appears in the following formulations: solution, ointment, oil/cream, powder, spray/foam.

20. Alkalized composition of plant root extracts of the Asphodelus genus according to claims 13, 14, 15, 17 and 19 for use in a method for treating pathologies and problems such as: dermatosis, eczema, scabies, mycosis, burns, onychomycosis, ephelides, abscesses, warts, verrucae, perionychia, alopecia, vitiligo, gingivitis, verrucous nevus, papillitis, acne, herpes labialis, aphta, insect bites, condyloma, herpes zoster, wounds, rhinosinusitis, as antiseptic, anthelmintic and as anti-pruriginous agent.

21. Alkalized composition of plant root extracts of the Asphodelus genus according to claim 13 for use in a method for the therapeutic treatment of nerves and articulations.

22. Alkalized composition of plant root extracts of the Asphodelus genus according to claim 16 for use as reconstituent.

23. Alkalized composition of plant root extracts of the Asphodelus genus according to claim 18 for use in a method for eliminating toxins from the body.