WO2016188919A1

WO2016188919A1 - Healing composition based on sedum telephium and allantoin

Info

Publication number: WO2016188919A1
Application number: PCT/EP2016/061473
Authority: WO
Inventors: Elena CONTU
Original assignee: Mag S.R.L. Societa' A Responsabilita' Limitata Semplificata
Priority date: 2015-05-22
Filing date: 2016-05-20
Publication date: 2016-12-01
Also published as: ITUB20150763A1; EP3297627A1

Abstract

A composition with healing action that comprises from 85% to 95% by weight on the total weight of the composition of 23% Sedum Telephium hydrophilic gel and from 5% to 15% by weight on the total weight of the composition of 0.5% allantoin. A method for preparing the composition according to the invention and its use for treating skin or mucosal lesions.

Description

HEALING COMPOSITION BASED ON SEDUM TELEPHIUM AND ALLANTOIN

The present invention relates to a healing composition, comprising extract of Sedum Telephium and allantoin.

The cosmetic and pharmaceutical fields nowadays offer many products with healing and re-epithelializing action. Among these, products based on fibrin, collagen or collagenase, iodine, hyaluronate, extract of common wheat, hydrocolloids, calendula extract, aloe gel can for example be mentioned. Besides traditional pharmaceutical products, substances of natural origin which have a soothing action and are capable of favoring tissue regeneration are also known.

Sedum Telephium (hereinafter also referred to as Sedum T.) is the scientific name of a succulent plant, belonging to the Crassulaceae family, which is commonly known in Italy as "erba della Madonna", literally "Madonna's grass", and is known in the English-speaking world by many other names including "livelong" and "live-forever". This plant is known in traditional medicine for its anti-inflammatory, pain-relieving, healing and emollient properties: the leaves of Sedum Telephium, applied to the area to be treated, have the above-listed effects. The aforementioned properties are due to the abundance of polysaccharides and polyphenols in the leaves of the plant. Preparations based on Sedum Telephium have therefore been used in traditional medicine since ancient times to promote healing and re- epithelialization of injuries, burns, sores and ulcers and to promote suppuration of abscesses and mastitis; Sedum T. is in fact even suitable for application on infected areas. Further the emollient properties of Sedum T. make the extract suitable for application on calluses and plantar corns and in general on hyperkeratotic skin regions.

Currently, Sedum Telephium extract is known and marketed as a herbal preparation in the form of an alcoholic gel (for example by KOS S.r.l. Laboratorio di Erboristeria (herbalist laboratory)). Even in the form of an alcohol-based gel Sedum T. maintains its healing, re-epithelializing and anti-inflammatory properties, as shown by the studies carried out by Dr. Sergio Balatri (see for example: S. Balatri, "Impiego del Sedum Telephium L. nella pratica chirurgica minore" [Use of Sedum Telephium L. in minor surgery]. Boll, e Mem. della Societa Tosco-Umbra di Chirurgia, XLII, (1), 337-341, 1981-1982). It is clear however that the form of an alcohol-based gel limits the use of Sedum Telephium extract to application on intact skin only; alcohol-based gel cannot instead be applied to injured skin, for example skin affected by sores, burns, ulceration and wounds, which has an even greater need for a treatment favoring tissue healing and regeneration. The topical application of Sedum Telephium has no contraindications, apart from a possible hypersensitivity thereto. Furthermore, no particular side effects have been found, except for a possible cutaneous sensitization after some days of use, which can be treated with topical preparations for irritated skin, such as for example ointments based on zinc oxide.

Allantoin is an intermediate of the metabolism of many animals, plants and bacteria. In particular, it is the final product of the oxidation of uric acid in the metabolic pathway of purines catabolism and it is produced by the action of the urate oxidase and 5-hydroxyisourate hydrolase enzymes. Allantoin is present in the botanic extract of Symphytum officinale, a plant of the Boraginaceae family, and in the urine of many animals. Snail slime, known for its healing, soothing and emollient properties, is also particularly rich in allantoin, which is the component that carries out the above actions. Actually, allantoin has a twofold function, depending on the concentration at which it is present in the formulation. In fact, at concentrations comprised between 0.1% and 0.5% by weight, the action of allantoin is moisturizing, anti-reddening, and soothing. At concentrations comprised between 0.5% and 3% by weight, the action of allantoin is healing.

Allantoin is therefore used both in the cosmetic field and in the pharmaceutical field, especially in dermatological formulations for topical application, and it is present in several preparations that favor the healing of small injuries and moisturizing of the skin. The topical application of allantoin has no contraindications, apart from a possible hypersensitivity thereto.

A limit of many medicines and cosmetic products that are currently available on the market is the fact that they include preservatives in their formulation, in order to make them last longer over time, while at the same time keeping their chemical-physical properties and their efficacy as unaltered as possible. Among the most widespread and commonly used preservatives are parabens (esters of parahydroxybenzoic acid), which are known for their antibacterial and fungicidal action. Parabens and their salts are widely used in formulations of cosmetics and medicines, both for topical use and for parenteral use. However, the safety of parabens in terms of human health is disputed by some in the scientific community. First of all, nowadays many people have developed an allergy to these substances, which causes skin reactions at the sites of contact with parabens containing products; furthermore, it appears that parabens are capable of interfering with the human endocrine system, in particular by mimicking the action of estrogen hormones. As a precautionary measure, therefore, the scientific community is leaning toward a progressive reduction of the use of parabens and their salts in cosmetic and pharmaceutical products, in favor of preservatives with less impact on human health or, where possible, in favor of the reduction or elimination of preservatives.

In light of the foregoing, the aim of the present invention is to provide a healing composition that overcomes the limits and drawbacks of the conventional formulations. Within this aim, an object of the invention is to provide a composition that is capable of ensuring a higher healing effect than that of the currently known formulations. Another object of the invention is to provide a healing composition that can also be applied to open lesions of skin and mucous membranes. Another object of the present invention is to provide a composition based on substances of natural origin and without parabens.

Another object of the present invention is to further provide a method for preparing a composition that has a healing action that exceeds that of known compositions.

Another object of the invention is to provide a healing composition that is highly effective, has no toxicity and is easy and low cost to provide.

This aim and these and other objects which will become better apparent hereinafter are achieved by a healing composition, comprising:

(a) 85% to 95% by weight on the total weight of the composition of

23% Sedum Telephium hydrophilic gel; and

(b) 5% to 15% by weight on the total weight of the composition of 0.5% allantoin.

Further characteristics and advantages of the invention will become better apparent from the description of some preferred, but not exclusive, embodiments of the composition according to the invention, and of the corresponding method for its preparation.

As it is known to the person skilled in the art, in the context of the present invention the term "hydrophilic gel" indicates a gel that comprises one or more hydrophilic polymers. The term "23% Sedum Telephium hydrophilic gel" means that the Sedum T. extract represents 23% by weight on the total weight of the gel.

A first aspect of the invention, as stated, relates to a healing composition that comprises from 85% to 95% by weight on the total weight of the composition of 23% Sedum Telephium hydrophilic gel and from 5% to 15% by weight on the total weight of the composition of 0.5% allantoin.

In a preferred embodiment, the composition can comprise from 88% to 92% by weight on the total weight of the composition of 23% Sedum Telephium hydrophilic gel. More preferably, the composition can comprise 90% by weight on the total weight of the composition of 23% Sedum Telephium hydrophilic gel.

In another preferred embodiment, the composition can comprise from 8% to 12% by weight on the total weight of the composition of 0.5% allantoin. More preferably, the composition can comprise 10% by weight on the total weight of the composition of 0.5% allantoin.

In an even more preferred embodiment, the composition can comprise 90% by weight on the total weight of the composition of 23% Sedum Telephium hydrophilic gel and 10% by weight on the total weight of the composition of 0.5% allantoin.

As stated above, the hydrophilic gel is a gel that comprises one or more hydrophilic polymers. In an embodiment of the invention, the hydrophilic gel can be a gel of cellulose, a gel of cellulose derivatives, or a gel of mixtures thereof, in water. Preferably, such gel can be a gel of hydroxyethylcellulose in water. Even more preferably, such gel can consist of 3% by weight of hydroxyethylcellulose and 97% by weight of water.

Preferably, the allantoin present in the composition according to the present invention can be extracted from snail slime and purified using methods known to the person skilled in the art.

The composition of the invention can further comprise one or more pharmaceutically acceptable excipients. Considering the chemical nature of the formulation, the excipients are preferably hydrophilic. By way of example, some excipients that can be present in the composition of the invention can be xanthan gum, ascorbic acid, and disodium ethylenediaminotetraacetic acid (EDTA).

The composition of the invention takes the physical form of a gel.

Therefore, it can be administered topically, by direct application onto the areas of the skin or mucous membranes to be treated. By virtue of the water- based (instead of alcohol-based) composition of the gel, the composition can also be applied to areas affected by open lesions.

In another aspect, the present invention relates to a method for preparing the healing composition described herein, which comprises the following steps:

(a) preparing a gel by dispersing in water one or more hydrophilic polymers;

(b) adding to the hydrophilic gel obtained in step (a) the Sedum

Telephium extract;

(c) adding to the Sedum Telephium gel obtained in step (b) the 0.5% allantoin.

All the steps of the method are carried out at ambient temperature. Typically, the ambient temperature can be comprised between 18°C and 28°C. However, as it is clear to a person skilled in the art, temperatures outside the range indicated can also be considered acceptable, as long as the method is carried out with no heating or cooling of the components.

Another aspect of the invention regards the use of the composition described herein for treating skin or mucosal lesions. In particular, the composition of the invention can be used to treat lesions that require healing, and/or re-epithelialization, and/or regeneration, and/or moisturizing of the skin or of the mucous membranes. Among the lesions that can be treated with the composition of the invention are, by way of non-limiting example, injuries, sores, ulcers, burns, abrasions, grazes.

The use of the composition according to the invention is topical, by way of direct application on the skin or on the mucous membranes, even if injured.

In light of the foregoing, it has been observed that the composition according to the invention fully achieves the intended aim. First of all, the composition described herein is effective in favoring the healing, re- epithelialization and regeneration of skin and mucosal tissue, and also for improving irritation, hyperkeratosis, and dehydration of skin and of mucous membranes. Furthermore, the specific content of allantoin enables this substance to have both a moisturizing, anti-reddening and soothing action, and also a healing action. In particular, it has been observed that the healing action of allantoin is synergistic with the action of the Sedum Telephium gel. Therefore, the combination of allantoin and of Sedum T. extract in the same composition allows to have a synergistic effect in terms of healing and re-epithelialization.

In addition, the formulation of the composition of the invention, based on a hydrophilic gel, makes it possible to use it for treating a broad category of skin or mucosal conditions, including open lesions.

Also, the composition described herein contains substances of natural origin, makes it possible to avoid the use of parabens, and is safe, in that its use has no contraindications.

Finally, the method for preparing the composition of the invention is easy to provide and does not require particular or expensive conditions or equipment for its implementation.

The healing composition according to the invention has been developed in particular for treating lesions of various types, of the skin and of the mucous membranes, in human beings; however, it can also be used in veterinary medicine.

The healing composition, conceived as described, is susceptible of numerous modifications and variations, all of which are within the scope of the appended claims. Moreover, all the details may be substituted by other equivalent elements, the correspondence of which is known to the person skilled in the art.

It should be understood that the characteristics of embodiments described with reference to an aspect of the present invention are to be considered valid also with reference to the other aspects of the invention described herein, even if they are not explicitly repeated.

EXAMPLE:

Below is a detailed example of preparation of the healing composition according to the invention. A hydrophilic gel of hydroxyethylcellulose (3% by weight) in water (97% by weight) was prepared. To prepare the gel, hydroxyethylcellulose was dispersed slowly in water, adding it by "sprinkling" and mixing for about two minutes, until the components were completely amalgamated.

Four hours after the preparation of the hydrophilic gel, the Sedum

Telephium extract was added to the gel; the resulting Sedum T. gel comprises 23% by weight of Sedum T. extract with respect to the total weight of the Sedum T. gel. Subsequently, allantoin (in powder form) was added to the Sedum T. gel, stirring until the components were completely amalgamated.

All the steps described here were carried out by working at ambient temperature.

The disclosures in Italian Patent Application No. 102015000016929 (UB2015A000763) from which this application claims priority are incorporated herein by reference.

Claims

1. A healing composition, comprising:

(a) 85% to 95% by weight on the total weight of the composition of 23% Sedum Telephium hydrophilic gel; and

(b) 5% to 15% by weight on the total weight of the composition of

0.5% allantoin.

2. The composition according to claim 1, comprising 88% to 92% by weight on the total weight of the composition of 23% Sedum Telephium hydrophilic gel.

3. The composition according to claim 2, comprising 90% by weight on the total weight of the composition of 23% Sedum Telephium hydrophilic gel.

4. The composition according to any one of claims from 1 to 3, comprising 8% to 12% by weight on the total weight of the composition of 0.5% allantoin.

5. The composition according to claim 4, comprising 10% by weight on the total weight of the composition of 0.5% allantoin.

6. The composition according to any one of claims 1 to 5, comprising 90% by weight on the total weight of the composition of 23% Sedum Telephium hydrophilic gel and 10% by weight on the total weight of the composition of 0.5% allantoin.

7. The composition according to any one of claims 1 to 6, wherein the hydrophilic gel comprises one or more polymers selected from the group consisting of cellulose, cellulose derivatives and mixtures thereof.

8. The composition according to claim 7, wherein the hydrophilic polymer is hydroxyethylcellulose.

9. The composition according to any one of claims 1 to 8, further comprising one or more pharmaceutically acceptable excipients.

10. The composition according to claim 9, wherein said one or more pharmaceutically acceptable excipients are independently selected from the group consisting of xanthan gum, ascorbic acid and disodium ethylenediaminotetraacetic acid (EDTA).

11. A method for preparing the composition according to any one of claims 1 to 10, comprising the steps of:

(a) preparing a gel by dispersing in water one or more hydrophilic polymers;

(b) adding to the hydrophilic gel obtained in step (a) the Sedum Telephium extract;

(c) adding to the Sedum Telephium gel obtained in step (b) the 0.5% allantoin;

wherein steps (a), (b) and (c) are carried out at ambient temperature.

12. The composition according to any one of claims 1 to 10, for use in treating skin or mucosal lesions.

13. The composition for use according to claim 12, wherein the lesions are selected from the group consisting of wounds, sores, ulcers, burns, abrasions, grazes.