• 专利附录
  • 专利说明
  • 权利要求
  • 类似技术
  • 同族专利
  • 引用文献
  • 法律状态
  • 优先权
    • 专利摘要:
    Combination with regenerative function of the skin barrier function. The present invention relates to a combination of active agents comprising one or more betaines; one or more polyalcohols; hyaluronic acid or a pharmaceutically or cosmetically acceptable salt; Leaf extract of Opuntia Ficus Indica; and Olea Europea olive leaf extract and topical pharmaceutical or cosmetic compositions containing it. The invention also relates to its pharmaceutical use for the treatment and/or prevention of cutaneous affections that occur with a disruption of the barrier function of the skin; and its cosmetic use as agents for skin care. (Machine-translation by Google Translate, not legally binding)
    公开号:ES2663574A1
    申请号:ES201631320
    申请日:2016-10-13
    公开日:2018-04-13
    发明作者:Aurora Del Carmen GARRE CONTRERAS；Susana MEZQUITA REGUEIRO；Maialen ELIZARI GALAR
    申请人:Laboratorios Cinfa SA；
    IPC主号:
    专利说明:

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    INCI, CAS number 90082-216) refers to an extract of Opuntia Ficus Indica leaf that is mainly formed by polysaccharides with mucoadesive effect. Specifically, the polysaccharide content in the Opuntia Ficus Indica extract ranges from 1% to 70% by weight. This extract is obtainable by means of a procedure that includes washing and cutting the clamps of Opuntia Ficus Indica into pieces of about 10cm, then they are compressed using a hydraulic forging press and the juice obtained is centrifuged for 15 min at 5,000 g and the supernatant It ultrafilters. In this way, an aqueous solution enriched in the high molecular weight polysaccharide fraction (greater than 104 Da) is obtained. This aqueous solution is then concentrated at low pressure and at a temperature between 35 ° C and 40 ° C, and subsequently dried by spray-drying.
    or lyophilization as described in patent application WO2011026606. As described above, the combination of the invention comprises from 0.1% to 1.0% by weight of Opuntia Ficus Indica leaf extract. In a particular embodiment, the combination of the invention comprises 0.17% of Opuntia Ficus Indica leaf extract.
    Finally, the combination of the invention also comprises an extract of European Olea leaf (INCI name, CAS number 8001-25-0). European Olea leaf extract refers to an extract obtained from the European Olea leaves that is mainly formed by biophenols with wound healing effect and with a lenitive effect. Specifically, the content of biophenols in the extract is from 3.7% to 4.3% by weight. Specifically, said extract contains: from 2 to 40% by weight of flavonoids (apigenin, luteolin and its derivatives), from 0.5% to 10% by weight of oleuropein and from 1% to 30% by weight of hydroxytyrosol and derivatives thereof. This extract is obtained by a procedure comprising drying and cutting the leaves of European Olea and its subsequent extraction with a 50:50 (v / v) ethanol / water mixture at room temperature for 12 hours. The extraction process is carried out with a 1: 5 (g / ml) plant: solvent ratio. When the extraction is complete, the extract is removed and the leaf is subjected to a second hydroalcoholic extraction process under the same conditions. The extracts are mixed and the solvent is removed by concentration in vacuo at 40 ° C. Finally, to increase the concentration of biophenols, the extract is adsorbed in styrenic resins and subsequently the biophenols are eluted with an ethanol / water solution.
    50:50 (v / v) as described in patent application WO2011026606. As described above, the combination of the invention comprises from 0.1% to 1.0% in
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    from 0.1% to 1.0% by weight of Olea European olive leaf extract.
    In a particular embodiment, optionally in combination with one or more features of the various embodiments described above or below, the combination of the invention comprises: 1% by weight of trimethylglycine; 6% by weight of xylitol; 0.1% by weight of the sodium or potassium salt of hyaluronic acid; preferably high molecular weight hyaluronic acid; 0.17% by weight of aqueous extract of Opuntia Ficus Indica leaf; and 0.12% by weight of Olea European olive leaf extract.
    A second aspect of the invention relates to a topical pharmaceutical composition comprising a therapeutically effective amount of the combination of active ingredients defined in the first aspect of the invention together with one or more pharmaceutically acceptable excipients and / or topical carriers.
    For the purposes of the invention, the term "topical" refers to the local application on the skin or mucosal surfaces of the body, the mucosal surfaces include the nasal cavity, oral cavity and vaginal mucosa.
    The term "therapeutically effective amount" refers to the amount of the combination of active ingredients of the invention that, when administered, is sufficient to prevent the development of, or relieve to some extent, one or more of the symptoms of the disease. That is headed. The particular dose of the combination administered according to this invention will be determined by the particular circumstances surrounding the case, including the compound administered, the route of administration, the particular condition to be treated, and similar considerations.
    The term "pharmaceutically acceptable excipients and / or topical carriers" refers to excipients or carriers suitable for use in contact with human skin in pharmaceutical technology for the preparation of compositions for medical use.
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    foaming, including polysorbate 20 or 40, coconut glycoside, lauryl glycoside, decyl glycoside, lauryl sulfates such as, for example, ammonium, sodium, magnesium, MEA, trimethylamine (TEA), or mipa lauryl sulfate, cocamidopropyl betaine, or alkylsulfosuccinates of sodium.
    The term "wetting agent" refers to a hygroscopic material that attracts water molecules from the surrounding environment both by absorption or adsorption, preventing the skin from losing moisture. Examples of suitable topical humectants include, but are not limited to, glycerin, diglycerin, ethylhexyl glycerin, glucose, honey, lactic acid, polyethylene glycol, propylene glycol, sorbitol, sucrose, or trehalose. Preferably, the humectant is selected from the group consisting of glycerin, diglycerin, ethylhexylglycerin, and mixtures thereof.
    The term "pH regulating agent" refers to acids or bases that can be used to adjust the pH of the finished product to the desired level without affecting the stability of the solution. Examples of topical pH regulating agents include, but are not limited to, acetic acid, lactic acid, citric acid, ethanolamine, formic acid, oxalic acid, potassium hydroxide, sodium hydroxide, triethanolamine, or mixtures thereof. Preferably, the pH regulating agent is selected from the group consisting of triethanolamine, sodium hydroxide, lactic acid, and citric acid.
    The term "antioxidant" refers to a material that slows or prevents the oxidation of other molecules. Antioxidants include free radical sequestrants and reducing agents. Examples of suitable antioxidants include, without limitation, free radical scavengers or reducing agents such as acetylcysteine, ascorbic acid, ascorbyl palmitate, butylated hydroxytoluene, green tea extract, caffeic acid, cysteine, tocopherol, ubiquinone, gallato propyl, butylated hydroxytoluene (BHT), and mixtures thereof. Preferably, the antioxidant agent is selected from the group consisting of ascorbyl palmitate and tocopherol.
    The term "preservative" refers to a material that prevents or reduces or slows microbial growth without affecting the stability of the solution. Examples of appropriate preservative agents include, but are not limited to, benzoic acid, butylparaben, ethylparaben, propylparaben, methylparaben, sorbic acid, potassium sorbate, sodium benzoate, phenoxyethanol, triclosan, or mixtures thereof. Preferably, the agent
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    up to 1.5% by weight of perfume; and enough water for 100%.
    The third aspect of the invention relates to the use of the combination of the first aspect of the invention for the preparation of a medicament or medical device for the treatment and / or prevention of skin conditions that present with a disruption of the skin's barrier function. . This aspect can also be formulated as the combination of the first aspect of the invention for use in the treatment and / or prevention of skin conditions that present with a disruption of the skin's barrier function. It also refers to a method for the prophylaxis and / or treatment of a skin condition that involves a disruption of the skin's barrier function, wherein said method comprises administering an effective amount of the combination of the first aspect of the invention in combination. with vehicles
    or pharmaceutically acceptable excipients to a subject in need, including a human being. Thus, the regenerative effect of the combination skin barrier and the composition of the present invention is shown in the results of the examples (cf. Section 2.4. Of the examples).
    In one embodiment, optionally in combination with one or more features of the various embodiments described above or below, the skin condition is selected from the group consisting of burns, skin ulcers, atopic dermatitis, seborrheic dermatitis, acne, skin hypersensitivity, rosacea, psoriasis, xerosis, eczema, facial erythrosis and facial couperose; preferably the skin condition is selected from the group consisting of burns and skin ulcers.
    In one embodiment, optionally in combination with one or more features of the various embodiments described above or below, the skin condition is a burn that is selected from the group consisting of surface burns, first degree burns and second degree burns, where Such burns can have both a physical and chemical origin.
    In one embodiment, optionally in combination with one or more features of the various embodiments described above or below, the skin condition is a skin ulcer whose origin is both a physical and chemical origin, such as surface ulcers of thermal origin, or as a result of a treatment of
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    antioxidants 1.0
    Water 62
    Sodium hyaluronate 0.10
    Oil phase Opuntia Ficus Indica leaf extract0.17
    European Olea leaf extract 0.12
    Emollients 3.0
    Emulsion stabilizers and thickeners 2.5
    (Phase O) Chelating agents and antioxidants0.6
    solvent 0.5
    Other components: pH regulating agents, aromas, skin conditioning agents and fillers 0.5
    Another composition of the present invention is the composition 2 shown in the following table:
    Phase ComponentfunctionQuantity (%)
    Water phase (FA) XylitolActive ingredient1.0
    Glycerin Active ingredient3.6
    betaine Active ingredient3.9
    decyl isostearate emollient3.1
    butylene glycol dicaprilate / dicaprate Emollient3.0
    Cyclopentasiloxane Emollient1.1
    Soy glycerides Emollient1.1
    Moringa oleifera seed oil Emollient1.0
    isostearyl isostearate Emollient3.1
    Limnanthes alba seed oil Emollient1.7
    cetearyl alcohol Emulsion stabilizer0.8
    Niacinamide Antioxidant2.0
    Ammonium acryloyl dimethyl restaurant / vp copolymer Emulsifier / thick nte1.0
    22
    Sodium hyaluronate Active ingredient0.5
    Water Vehicle60.4
    Oil Phase (FO) Opuntia Ficus Indica leaf extractActive ingredient0.05
    European Olea leaf extract Active ingredient2.05
    Shea Butter emollient1.5
    glyceryl stearate Emulsion Stabilizer0.9
    inulin lauryl carbamate Emulsifier0.5
    1,2-hexanediol Solvent0.5
    caprilil glycol Emollient1.2
    Dimethicone Emollient0.4
    Xanthan gum Thickener1.0
    Diethyl Syringylidene Malonate Antioxidant0.2
    Maltodextrin Binding agent0.2
    Zea mays oil Emollient0.9
    stearic acid Emulsion Stabilizer0.9
    Trisodium ethylenediamine disucinate Chelating agent0.1
    Allantoin Skin conditioning agent0.2
    stearyl glycinate fragrance0.01
    pentaerythrityl tetra-di-t-butyl hydroxyhydrocinamate Antioxidant0.1
    Calendula officinalis extract antioxidant0.8
    Madecassosido (extract of centella asiatica) Antioxidant0.2
    Dimethiconol emollient0.2
    Arginine PH regulator0.05
    lactic acid PH regulator0.04
    Asiaticoside Antioxidant0.1
    caprylic / capric triglyceride Emollient0.02
    2. 3
    Antimicrobial,
    tropolone conditioner0.006
    skin 1.2. Procedure for preparing the emulsion of the invention
    A. Preparation of the Phases:
    Aqueous Phase (Phase A)
    In the main vessel, equipped with turbines, blades and heating system, the active ingredients (xylitol, hyaluronic acid and betaine) were dissolved in water with the excipients described in the previous section until a solution was obtained transparent and homogeneous (if necessary, the waste would be removed). Then, the solution obtained was heated to a temperature between 40 ° C and 45 ° C and the rest of the water-soluble ingredients were added little by little until a homogeneous mixture was obtained. Then, the obtained mixture was heated at a temperature between 70 ° C and 75 ° C while maintaining slow stirring.
    Oil Phase (Phase O)
    In a separate mixing vessel, equipped with shovels and heating system, the emollients, antioxidant agents of the oil phase were added and the resulting mixture was heated to 75 ° C while mixing until a clear phase was obtained.
    B. Emulsion preparation
    The oil phase (Phase O) was slowly added to the aqueous phase (Phase A) and thoroughly homogenized with turbine and the resulting mixture was maintained at the same conditions of stirring and temperature for 2-15 minutes.
    After this time, the resulting emulsion was cooled to 40 ° C while homogenizing, loading agents, chelating agents, Opuntia Ficus Indica leaf extract, leaf extract were added one at a time until completely dissolved. Olea
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    European, and the other components as described in the Tables of the previous section while maintaining homogenization and subsequently, cooled to 25 ° C while stirring slowly.
    EXAMPLE 2: In vivo efficacy studies 2.0. Sample
    The effectiveness studies were carried out with the composition 1 of the present invention mentioned in section 1.1. of the present invention. 2.1. Cell renewal studies
    To determine the cell renewal, transparent adhesive discs applied on the skin were used to collect the scaling cells of the cornea layer and subsequent evaluation by colorimetry using Chromameter CR 400, Minolta.
    The rate of skin rotation was evaluated both in the short term and in the long term. The short-term evaluation was carried out by decreasing the intensity of the fluorescent spot (T5 days -T0) after applying the product for 5 days compared to the area of the skin that had not been treated.
    Regarding the long-term evaluation, it was carried out by measuring the number of days required to induce the disappearance of the fluorescent spot in the treated area with respect to the area of the untreated skin.
    Finally, the amount of scaly corneocytes was evaluated by colorimetric analysis using D-Squames -L * parameter in the treated area compared to the area of the untreated skin on day 0 (T0) and on the day that ended test (TF). In this case, D-Spames was applied in the selected areas for 30 seconds and after it was removed, each disc is pressed on the black card and in order to analyze colorimetrically to quantify the corneocytes that adhere to the disc. 2.2. Study of calming efficacy and restoration of the barrier function
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    To determine the calming efficacy and restoration of the barrier function against chemical stimuli (through the application of sodium lauryl sulfate) and physical (by applying UV radiation emitted from a Multiport 601-300 which is an Xenon arc lamp with a spectrum continuous between 290 nm and 400 nm with 6 independent lights) an instrumental assessment was performed by measuring trans-epidermal water loss (TEWL) using Tewameter TM 210, Courage & Khazaka and the evaluation of redness through Chromameter CR- 400, Minolta. TEWL is the amount of water that evaporates per hour, and square centimeter of skin, and this parameter is used to identify the state of the skin barrier. An increased TEWL means that there is a certain level of damage to the barrier due to a lack of barrier substances, and, as a consequence, the skin dries due to moisture loss. 2.3. Study of the moisturizing effect
    The immediate moisturizing effect has been tested after a single application of the composition of the invention and subsequent instrumental evaluation by means of Corneometer CM 825 with hydration kinetics being performed at 30, 60, 120 and 180 minutes after said application. 2.4. Results
    The results of the studies carried out in sections 2.1-2.3 demonstrate the efficacy of the topical composition of the invention comprising the combination of one or more betaines; one or more polyols; hyaluronic acid or a pharmaceutically or cosmetically acceptable salt; Opuntia Ficus Indica leaf extract and Olea European olive leaf extract for the treatment and / or prevention of skin conditions that present with a disruption of the skin's barrier function; as well as its use as a skin repair agent.
    A. Skin recovery - CHEMICAL DAMAGE (SLS)
    As seen in Table 1, the composition of the invention induces a faster recovery of the skin and barrier function after chemical damage by exposure to sodium lauryl sulfate.
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    权利要求:
    Claims (1)
    [1]
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