Anti-allergic composition for the eyes

Abstract

An anti-allergic product comprising a plant extract in an amount of at least 0.01% w / w, wherein the plant extract is selected from the group consisting of Camellia sinensis leaf extract, Melaleuca alternifolia leaf oil, and mixtures thereof, an amphiphilic preservative, and a glycolipid. The eyelid cleansing composition is configured to reduce redness, discomfort, and irritation in and around the eyelids.

Description

Technical Field

[0001] The present invention broadly relates to anti-allergy products for alleviating symptoms associated with eyelid allergies.

Background Art

[0002] Eye health relates not only to the eyes but also to structures associated with the eyes, such as the eyelids. The eyelids are important in overall eye health because they protect the eyes from dangers such as approaching objects or air pollutants such as pollen, dust particles, or other foreign substances. The eyelids have extremely important glands, the lacrimal gland and Meibomian glands, which produce the tear film layer essential for a healthy eye. When a person blinks, a new tear film is created, and the tears are distributed across the entire cornea to moisten the surface of the eye. This blinking action also "washes away" foreign objects from the eyes.

[0003] However, the eyelids are susceptible to various allergies and bacterial infections on the skin surface. Seasonal allergies can also cause redness, itching, and irritation of the eyes and eyelids. Allergy eye drops relieve various eye symptoms but do not soothe the irritated eyelids. Therefore, there is a need for products that can alleviate the symptoms associated with eyelid allergic conditions.

[0004] According to an embodiment, the anti-allergy composition contains at least 0.01% w / w of a plant extract, where the plant extract is selected from the group consisting of Camellia sinesis leaf extract, Melaleuca alternifolia leaf oil, and mixtures thereof. The composition further contains a glycolipid, an amphiphilic preservative, and water. In an embodiment, the glycolipid is a sphingolipid selected from the group consisting of sphingolipids, ceramides, glycerophospholipids, sphingolipid derivatives, and combinations thereof.

[0005] In one exemplary embodiment, the sphingolipid is selected from the group consisting of sphingosine, sphinganin, phytosphingosine, phytosphingosine salts, tetraacetyl-phytosphingosine, N-acetylphytosphingosine, and mixtures thereof. The sphingolipid is preferably in the range of 0.1% to 0.3% w / w.

[0006] In one or more embodiments, the preservative is present in an amount ranging from 0.01% to 5% w / w. In a particular embodiment, the preservative is lauramine oxide.

[0007] According to one embodiment, the anti-allergic composition further comprises at least one polyol having 2 to 12 carbon atoms. The at least one polyol may be a 1,2-diol selected from the group consisting of 1,2-hexanediol, 1,2-octanediol, 1,2-decanediol, and mixtures thereof. Embodiments of the composition contain at least one polyol in the range of 0.01% to 5% w / w.

[0008] Exemplary embodiments of the anti-allergic composition further include one or more surfactants present in the range of 0.1 to 20% w / w. Of the one or more surfactants, the first surfactant has an HLB (hydrophilic-lipophilic ratio) value between 10 and 18, and the second surfactant, if present, has an HLB value between 10 and 18 or between 5 and 10. In certain embodiments, the surfactants include decyl glucoside and polysorbate 20.

[0009] In one embodiment, the anti-allergic composition further comprises a foam stabilizer. The foam stabilizer is preferably a polyethylene glycol diester of methyl glucose and a fatty acid.

[0010] In certain embodiments of the anti-allergic composition, the pH is in the range of 3.5 to 6.5, the refractive index is approximately 1.33 to 1.35, and the specific gravity is approximately 0.99 to 1.01.

[0011] Additional embodiments of the anti-allergic composition include one or more humectants, softeners, wetting agents, and lubricants, as well as one or more skin conditioning agents, antioxidants, sedatives, cooling agents, viscosity modifiers, and nutrients.

[0012] According to one embodiment, an anti-allergic composition is combined with a substrate capable of impregnating a desired amount of the composition, wherein the composition-impregnated substrate is configured as a single-use product.

[0013] In one exemplary embodiment, the anti-allergic composition comprises 0.1–0.3% phytosphingosine HCl, 0.01–5% hexanediol, 0.01–5% octanediol, 0.1–20% polysorbate 20, 0.1–20% decyl glucoside, at least 0.01% tea tree oil, at least 0.01% green tea extract, 0.01–5% lauramine oxide, and water to 100%. The pH is in the range of 3.5–6.5, the refractive index is approximately 1.33–1.35, and the specific gravity is approximately 0.99–1.0.

[0014] In one embodiment, the anti-allergic composition may be used by gently applying it to the surface of the eyelids and the surrounding eye area, thereby relieving redness, discomfort, and irritation in the applied area. The composition may be formulated to be left on the skin or to be washed off. [Modes for carrying out the invention]

[0015] The terms and phrases "invention," "this invention," and "this invention," as well as similar terms and phrases, when used herein, are non-limiting and are not intended to limit the subject matter to any one embodiment, but rather to encompass all possible embodiments as described herein.

[0016] Where used herein, all weight percentages (wt.%) are based on the total wt.% of the antiallergic composition unless otherwise specified. In addition, all composition percentages are based on a total equal to 100 wt.% unless otherwise specified.

[0017] The products and methods described herein may “include,” “essentially consist of,” or “consist of” any of the components or steps disclosed throughout this specification. Where used herein and in the claims, the words “comprising” (and any form of comprising, such as comprise and comprises), “having” (and any form of having, such as have and has), “including” (and any form of including, such as includes and include), or “containing” (and any form of containing, such as contains and contain) are comprehensive or open-ended and may include, but do not exclude, other components or steps described herein. The use of the words “a” or “an,” where used in the claims and / or herein with the term “comprising,” may mean “one,” but is not inconsistent with the meanings of “one or more,” “at least one,” and “one or more.” As used herein, "essentially consisting of" means that the present invention may include additional components / steps in addition to the components / steps described in the claims, but only if such additional components do not substantially alter the basic and novel features of the claimed invention. Generally, additives should not be present at all, or may be present only in trace amounts. However, it may be possible to include up to about 10% by weight of substances that substantially alter the basic and novel features of the invention, provided that the usefulness (not the degree of usefulness) of the composition is maintained.

[0018] All ranges described herein include both endpoints, including those describing a range "between" two values. Terms such as "about," "generally," and "substantially" should be interpreted as modifying a term or value so that it is not absolute. Such terms are defined by context, and the terms they modify as such will be understood by those skilled in the art. In one non-limiting embodiment, such terms are defined as within 1%, more preferably within 0.1%, and most preferably within 0.01%. The term "substantially" and its variations are defined as being mostly, but not necessarily completely, as understood by those skilled in the art.

[0019] As used herein, the term “effective amount” of a composition refers to an amount sufficient to elicit a desired biological response. As will be understood by those skilled in the art, and as will be understood by those skilled in the art, the effective amount of a substance may vary depending on factors such as the desired biological endpoint, the patient, and so on. In some embodiments, a therapeutically effective amount of a composition is an amount sufficient to treat, inhibit, suppress, prevent, and / or delay the onset of one or more eyelid allergic symptoms when administered to a subject suffering from or susceptible to a disease, disorder, and / or condition. The terms “treat” or “suppress,” or any variation thereof, include a quantitative or qualitative reduction of allergic symptoms. For example, an effective / therapeutically effective amount of a composition to treat eyelid allergy is an amount that alleviates, soothes, reduces, inhibits, prevents, delays the onset of, suppresses the severity of, and / or reduces the frequency of one or more symptoms or features associated with an allergic eyelid condition.

[0020] The anti-allergic composition may contain anti-inflammatory agents, antibacterial agents, antifungal agents, and anti-irritant agents. In one embodiment, the composition is an eyelid cleanser for removing pollen, contaminants, and allergens from the eyelids and the eyelid margins / parts surrounding the eyes / eyelids. The composition may be configured to prevent or suppress eyelid allergy-like symptoms, i.e., redness, itching, irritation, or inflammation of the eyelids or surrounding areas. The composition has effective amounts of one or more plant extracts, lipophilic or amphiphilic agents, antibacterial preservatives, and a suitable solvent or carrier.

[0021] The plant extract may be selected from the group consisting of Camellia Sinensis (green tea) leaf extract, Melaleuca alternifolia (tea tree) leaf oil, Citrus sinensis, chamomile flower, and combinations thereof. In a particular embodiment, the plant extract may include a mixture of green tea leaf extract and tea tree leaf oil. The selected plant extract contains an effective amount (i.e., at least 0.01% w / w of the composition) of polyphenol compounds and terpene compounds. Such plant extracts typically have antibacterial, antifungal, and / or anti-inflammatory activity.

[0022] For example, certain Camellia Sinensis leaf extracts, or green tea leaf extracts, have been shown to contain polyphenols. These polyphenols may include flavanol derivatives, such as catechins, epigallocatechin, and epigallocatechin gallate. Green tea leaf extracts generally possess antioxidant effects that can protect the skin from the damaging effects of free radicals. In addition, certain green tea extracts contain anti-inflammatory agents that suppress inflammation in the skin. Some green tea extracts have also been shown to have moisturizing properties and act as inhibitors of epidermal collagenase (a collagen-inhibiting enzyme that breaks down collagen), helping to maintain firm and elastic skin.

[0023] Tea tree leaf oil, or tea tree oil, is generally obtained by steam distillation from Melaleuca alternifolia, a plant native to Australia, and contains around 100 components, including terpinenes, terpenes, and related derivatives and combinations. More specifically, tea tree oil often contains monoterpenes, sesquiterpenes, and related alcohols.

[0024] One important aspect of a composition is its antimicrobial activity, typically provided by one or more antimicrobial agents. In some embodiments, the composition comprises glycolipids. Glycolipids may be selected from the group consisting of sphingolipids, ceramides, glycerophospholipids, sphingolipid derivatives, and combinations thereof. In some embodiments, a sphingoid base is selected from the group consisting of sphingosine, sphinganine, phytosphingosine, phytosphingosine salts, tetraacetyl-phytosphingosine, N-acetylphytosphingosine, and mixtures thereof. In a particular embodiment, the sphingoid base comprises about 0.1% to about 0.3% phytosphingosine and / or phytosphingosine hydrochloride (HCl) as the active ingredient. In one embodiment, the composition contains about 0.2% phytosphingosine HCl. Phytosphingosine and phytosphingosine HCl can inhibit the growth of microorganisms on the skin, suppress skin redness and inflammation, and are active at very low concentrations. PSG (phytosphingosine) HCl may contribute to preventing water loss from the skin, enhancing collagen synthesis while inhibiting its breakdown, and soothing inflamed skin. PSG HCl can also exhibit skin protective and anti-inflammatory properties at low concentrations of as little as 0.1%.

[0025] Preferred embodiments of the composition include a preservative having effective antimicrobial activity. One such preservative with significant antimicrobial properties is lauramine oxide. Lauramine oxide is an ideal amphiphilic preservative for the eye area because it is compatible with a wide range of surfactant systems, including anionic, cationic, amphoteric, nonionic, and various combinations thereof. In one or more embodiments, the preservative is selected from the group consisting of lauramine oxide, myristamine oxide, combinations of lauramine oxide and myristamine oxide, N,N-dialkylamine oxides having long alkyl chains between C10 and C18, and mixtures thereof. In some embodiments, the N,N-dialkyl is preferably methyl. The N,N-dialkylamine oxide having long alkyl chains between C10 and C18 is preferably oleyldimethylamine oxide.

[0026] The composition further comprises a polyol having 2 to 12 carbon atoms. Preferably, at least one 1,2-diol compound is included for the solubilization of glycolipids. 1,2-diols may be included in the composition because they have activity that enhances antibacterial properties. Preferred 1,2-diols are selected from the group consisting of: 1,2-hexanediol is a synthetic preservative with broad-spectrum antibacterial activity. Similarly, 1,2-octanediol (also known as caprylyl glycol) is another active substance that functions as a preservative and antibacterial agent.

[0027] A blend of one or more surfactants may also be included in the anti-allergy composition to promote solubilization of tea tree oil. Various surfactants may be included in the composition to obtain the desired foaming power and / or detergency. By including surfactants, the ability of the composition to dissolve and remove oils, antigens, debris, and flaky skin is increased. Preferred surfactants include nonionic or amphoteric surfactants having foaming ability and an HLB value between 10 and 18. When two or more surfactants are used, at least one surfactant should have an HLB value between 10 and 18, and the other surfactant(s) should have either an HLB value between 10 and 18 or an HLB value between 5 and 10.

[0028] Suitable surfactants may include amphoteric surfactants, anionic surfactants, and nonionic surfactants. Suitable amphoteric surfactants include, but are not limited to, alkyl dimethyl betaine, alkyl amide betaine, sulfobetaine, and imidazoline amphoteric surfactants. Suitable anionic surfactants include, but are not limited to, fatty alcohol sulfate, alpha olefin sulfonate, sulfosuccinate, sarcosinate, phosphate ester, and carboxylate. Suitable nonionic surfactants include, but are not limited to, alkanolamide, ethoxylated amide, ester, alkylated alcohol, alkyl polyglucoside, amine oxide, sorbitan ester, and ethoxylate.

[0029] Examples of the one or more surfactants include, but are not limited to, sorbitan esters (such as Span 20 or sorbitan monolaurate), polyethylene glycol (PEG)-modified surfactants (such as polysorbate 20, Brij 52, PEG-75 lanolin), modified phospholipids, modified sugars (such as alkyl polyglucosides, alkyl glucosides, fatty acid glucamides), amine oxides, and / or block copolymers such as Pluronic® (Pluronic F120) or tyloxapol. The total concentration of the surfactant ranges from 0.1 to 20% w / w of the final formulation, more preferably from 0.5 to 5%. By including a surfactant, the cleaning ability of the composition can be enhanced and the composition can be given foaming ability. The foam is considered to have an optimal cleaning ability.

[0030] A preferred surfactant system for the composition includes decyl glucoside and polysorbate 20 to promote solubilization of tea tree oil. The system is optimized to enhance the foaming characteristics of the composition and delivery of the active ingredient to the skin surface. The HLB values of decyl glucoside and polysorbate 20 are 12.8 and 16.7, respectively.

[0031] Optionally, a foam stabilizer may be added to the composition, and examples of the agent include, but are not limited to, polyethylene glycol diesters of methyl glucose and fatty acids. The fatty acid may be selected from the group consisting of oleic acid, stearic acid, lauric acid, caprylic acid, and capric acid. Preferably, examples of the one or more foam stabilizers include PEG-120 methyl glucose dioleate.

[0032] One or more humectants, softeners, wetting agents, or lubricants are also commonly added to the composition, and these are generally referred to herein as humectants. Suitable humectants include propylene glycol, glycerin, polyethylene glycol (e.g., PEG-300, 400, 600) or generally liquid polyols, nut oils and derivatives, rose water (flower extract), cucumber extract, fruit extract, sodium alginate, hyaluronic acid, diglycerides, triglycerides, PEG-75 lanolin, mineral oil, and silicone oil.

[0033] Optional additional components may be added to the composition in amounts up to 5% w / w of the composition. These optional components include compounds such as skin conditioning agents (e.g., D-panthenol), antioxidants (e.g., vitamin E and its derivatives, green tea extract, vitamin C and its derivatives), anti-irritant / sedatives (e.g., allantoin, aloe vera, tea tree oil), cooling agents (e.g., sorbitol, xylitol, menthol, thymol), viscosity modifiers (e.g., carboxymethycellulose, hypromellose, carbopol), and nutrients (e.g., minerals, vitamins, amino acids, or polypeptides).

[0034] An exemplary embodiment of the composition is shown in Table 1. This embodiment has a pH in the range of 3.5 to 6.5, a refractive index of about 1.33 to 1.35, and a specific gravity of about 0.99 to 1.01. Those skilled in the art will see that the range of properties in the composition can be adjusted while maintaining physiological adaptability with the eye area. The given ranges reflect one optimal condition for each of the components listed below and do not limit all possible embodiments of the present invention.

[0035] [Table 1]

[0036] The composition is substantially non-irritating to the eyes. Advantageously, the composition does not contain astringents such as zinc or zinc salts.

[0037] The composition may be selected from the group consisting of solutions, mists, foams, gels, sprays, lotions, suspensions, emulsifiers, ointments, and combinations thereof.

[0038] In one embodiment, the composition may be combined with a suitable substrate to form an anti-allergic product for cleansing the eyelids. The substrate can be impregnated with a clinically effective amount of the composition. The substrate may be a wipe, a cloth pad or towelette, or any suitable material capable of absorbing the desired amount of the composition. The term "pad" refers to a thick piece of cloth capable of holding or absorbing the composition. The cloth may be a lint-free cloth such as rayon or another suitable material. In certain embodiments, the cloth pad may be a cotton pad. The cloth pad may include a textured surface.

[0039] Anti-allergy products may be packaged as single-use products. Anti-allergy products may be supplied in sealed packaging. Such packages, ranging from 1 to 100 units, may be supplied in containers.

[0040] In another embodiment, a method for treating eyelid allergy involves preparing an anti-allergic product disclosed herein. The method further involves gently rubbing the product onto the surface of the eyelid and / or the area surrounding the eyelid, or the entire area, to reduce redness, discomfort, and irritation on and around the eyelid. The composition may be configured as a composition that does not form a residue. The composition can be left on the eyelid or washed off with water. The composition can wash away and remove foreign matter and debris, including microorganisms such as bacteria or allergens, from the application site on the eyelid. The composition can also induce foaming, which aids in the cleansing ability of the formulation, and can prevent allergies of the eyelid and eyelid margin, and promote anti-inflammatory and redness suppression.

[0041] The present invention may include, or may essentially consist of, other components not described (such as biological protective gloves) in addition to the components described herein.

[0042] In one or more embodiments, an anti-allergic composition for the eyes may be prepared by first preparing a glycolipid mixture. This involves adding a predetermined amount of 1,2-diol to a mixing vessel to promote the solubilization of the glycolipid mixture. The antimicrobial glycolipid is then incorporated into the same vessel. The mixture is then mixed at 500 RPM for 30 minutes, or until the glycolipid is completely dissolved and a clear solution is obtained. Heating of the mixture is not required to completely dissolve the glycolipid.

[0043] In a separate container, add purified water equivalent to approximately 90% of the final batch weight. Next, add the dissolved glycolipid mixture to the purified water. Rinse the first mixing container with purified water as needed and transfer the contents to the new container. The mixing process is started at 500 RPM.

[0044] While mixing, add the surfactant, plant extract, preservative, and any other additional ingredients described herein to the mixture. Rinse all containers and vessels with purified water and transfer to the container in which the mixing is taking place. Continue the mixing process until homogeneity is achieved. Finally, use purified water to bring the mixture to its final weight and mix for a further 30 minutes to ensure homogeneity.

[0045] The potential for eye irritation was evaluated using the non-animal EpiOcular test. The antiallergic agent had an estimated Draize eye irritation score of approximately "0" in 100% of cases, and was classified as "non-irritant." A human repeated patch test was performed on a panel of 50 subjects. Importantly, no signs of skin irritation or sensitization were observed with respect to the antiallergic agent.

[0046] The stability of the anti-allergic composition was evaluated for 18 months at room temperature and 6 months at 40°C. Under both conditions, the pH, refractive index, and specific gravity of the composition remained unchanged from their initial values. In addition, the composition maintained a clear to yellow appearance throughout the test without the formation of any visible particulate matter. An antimicrobial efficacy test was performed on a sample at room temperature for 18 months according to USP51 and passed.

[0047] Those skilled in the art will see that various modifications and variations can be made in the present invention without departing from the scope or spirit of the invention. Other embodiments of the present invention will also be evident to those skilled in the art from the discussion herein and the practice of the invention disclosed herein. This specification and the examples are intended to be illustrative only.

Claims

1. (i) A plant extract in an amount of at least 0.01% w / w, wherein the plant extract is selected from the group consisting of Camellia sinensis leaf extract, Malaleuca alternifolia leaf oil, and mixtures thereof. (ii) glycolipids; (iii) Amphiphilic preservatives, and (iv) water An anti-allergic composition containing the above.

2. The anti-allergic composition according to claim 1, wherein the glycolipid is selected from the group consisting of sphingolipids, ceramides, glycerophospholipids, sphingolipid derivatives, and combinations thereof.

3. The anti-allergic composition according to claim 2, wherein the glycolipid is a sphingolipid selected from the group consisting of sphingosine, sphinganin, phytosphingosine, phytosphingosine salts, tetraacetyl-phytosphingosine, N-acetylphytosphingosine, and mixtures thereof.

4. The anti-allergic composition according to claim 3, wherein the sphingolipid is in the range of 0.1% to 0.3% w / w.

5. The anti-allergic composition according to claim 1, wherein the amphiphilic preservative is present in an amount of 0.01% to 5% w / w.

6. The anti-allergic composition according to claim 1, wherein the amphiphilic preservative is selected from the group consisting of lauramine oxide, myristamine oxide, a combination of lauramine oxide and myristamine oxide, N,N-dialkylamine oxide having a long alkyl chain between C10 and C18, and mixtures thereof.

7. The anti-allergic composition according to claim 1, further comprising at least one polyol.

8. The anti-allergic composition according to claim 7, wherein the polyol has 2 to 12 carbon atoms.

9. The anti-allergic composition according to claim 8, wherein the polyol is a 1,2-diol selected from the group consisting of 1,2-hexanediol, 1,2-octanediol, 1,2-decanediol, and mixtures thereof.

10. The anti-allergic composition according to claim 9, wherein the polyol is present in an amount of 0.01% to 5% w / w.

11. The anti-allergic composition according to claim 1, further comprising one or more surfactants.

12. The anti-allergic composition according to claim 11, wherein the one or more surfactants are present in an amount of 0.1 to 20% w / w.

13. The anti-allergic composition according to claim 11, wherein the one or more surfactants comprises decyl glucoside and polysorbate 20.

14. The anti-allergic composition according to claim 11, wherein the first surfactant has an HLB (hydrophilic-lipophilic ratio) value between 10 and 18.

15. The anti-allergic composition according to claim 14, wherein the second surfactant has an HLB value between 10 and 18 or between 5 and 10.

16. The anti-allergic composition according to claim 1, further comprising a foam stabilizer.

17. The anti-allergic composition according to claim 16, wherein the foam stabilizer is a polyethylene glycol diester of methyl glucose and a fatty acid.

18. The anti-allergic composition according to claim 1, wherein the pH is in the range of 3.5 to 6.

5.

19. The anti-allergic composition according to claim 1, wherein the refractive index is approximately 1.33 to 1.

35.

20. The anti-allergic composition according to claim 1, wherein the specific gravity is approximately 0.99 to 1.

01.

21. The anti-allergic composition according to claim 1, further comprising one or more humectants, softeners, wetting agents, and lubricants.

22. The anti-allergic composition according to claim 1, further comprising one or more skin conditioning agents, antioxidants, sedatives, cooling agents, viscosity modifiers, and nutrients.

23. The anti-allergic composition according to claim 1, wherein the composition is combined with a substrate capable of impregnating a desired amount of the composition.

24. The anti-allergic composition and substrate according to claim 23, wherein the composition-impregnated substrate is configured as a single-use product.

25. 0.1-0.3% phytosphingosine HCl, 0.01-5% hexanediol, 0.01-5% octanediol, 0.1-20% polysorbate 20, 0.1-20% decyl glucoside, At least 0.01% tea tree oil, At least 0.01% green tea extract, 0.01-5% lauramine oxide, and Water until it reaches 100% An anti-allergic composition consisting of the following.

26. The use of the anti-allergic composition according to claim 1 in the manufacture of a pharmaceutical product for treating eyelid allergies, To prepare the anti-allergic composition described in claim 1, and Gently apply the composition to the surface of the eyelid and the surrounding eye area. Includes, Here, the composition is configured to alleviate redness, discomfort, and irritation in the applied area. use.

27. The use according to claim 26, wherein the anti-allergic composition is configured as a composition that is left on the skin or washed off.

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