Abstract: An anti-wrinkle under eye composition comprising peptides, a flavonoid, a chelating agent, a skin lightening agent, an exfoliating agent, a skin protectant and one or more dermatologically acceptable excipients.
CLIAMS:We Claim:
1. An anti-wrinkle under eye composition comprising:
a) peptides
b) a flavonoid,
c) a chelating agent,
d) a skin lightening agent,
e) an exfoliating agent and
f) a skin protectant
2. The composition according to claim 1, wherein the peptides are mixture of tripeptide N-palmitoyl-Gly-His-Lys and a tetrapeptide N-palmitoyl-Gly-Gln-Pro-Arg
3. The composition according to claim 1, wherein the flavonoid is chrysine.
4. The composition according to claim 1, wherein the chelating agent is N-hydroxysuccinimide.
5. The composition according to claim 1, wherein the components a) to c) are in the form of a ready-to-use solution.
6. The composition according to claim 1, wherein the skin lightening agent is in the form of a ready-to-use solution comprising diacetyl boldine.
7. The composition according to claim 1, wherein the exfoliating agent is in the form of a ready- to-use solution comprising grapefruit extract, lemon fruit extract, tomato extract, bilberry extract, citric acid and lactic acid.
8. The composition according to claim 1, wherein the skin protectant is in the form of powder comprising a blend of allantoin and glycyrrhetinic acid.
9. The composition according to claim 1 may further comprise at least one dermatologically acceptable excipients selected from the group consisting of solvents, emulsifying agents, gelling agents/ thickening agents, neutralizers, buffering agents, humectants/ moisturizers, film-forming agents, antioxidants, chelating agents, preservatives, emollients.
10. The composition substantially as herein as described with reference to the fore going example.
,TagSPECI:The following specification particularly describes the invention and the manner in which it should be performed.
Aspects of the present invention relate to anti-wrinkle under eye compositions. Further aspects of the present invention relate to methods for preparing and using such compositions.
The first visible signs of aging usually found on the skin are dryness, fine lines and wrinkles, rings or circles under the eyes, loss of elasticity, wasting and sagging of the skin, loss of firmness, thinning of the skin, hyperpigmentation, age spots. One of the major factors responsible for these skin conditions is stress caused by atmospheric pollution, lack of sleep, lifestyle etc. Skin is perpetually exposed to these stresses and as the skin ages, there is a reduction in protein synthesis, an increase in proteolysis and a general disruption of the skin barrier, connective tissue and cohesion.
Periorbital hyperpigmentation or wrinkles under the eye is a common condition that presents as a bilateral semicircle of hyperchromatic discoloration of the skin. The dark discoloration may be seen both superior and inferior to the eyelids in a semicircle shape following the orbital rim. The discoloration may extend beyond the orbital rim on both the medial and lateral sides of the eyelid opening. The factors that may contribute to the darkening appearance include congestion within the microvascular and subcutaneous blood vessel plexus, post-inflammatory hyperpigmentation, dermal melanin deposition, allergic dermatitis, and shadowing due to edema or wrinkles.
International Application Publication No. WO2005048968 discloses cosmetic compositions containing a tripeptide such as N-palmitoyl-Gly-His-Lys and a tetrapeptide such as N-palmitoyl-Gly-Gln-Pro-Arg are useful for treating visible signs of aging including wrinkles, stretch marks and dark circles.
International Application Publication No. WO2006031555 discloses diacetyl boldine for slimming, reducing cellulite, firming and decreasing pigmentation of the skin.
International Application Publication No. WO2005102266 discloses cosmetic composition Haloxyl® for treating rings under the eyes and/or hematoma. It further discloses anti-wrinkle cream containing Lumiskin® with skin whitening property.
Several skin care products are available for treatment of periorbital hyperpigmentation or wrinkles under the eye. However these products are incapable of providing the much needed effect to the affected areas.
We have now surprisingly found that an anti-wrinkle under eye composition comprising a combination of peptides, a flavonoid, a chelating agent, a skin lightening agent, an exfoliating agent and a skin protectant is beneficial for treatment of periorbital hyperpigmentation or wrinkles under the eye.
EMBODIMENTS
In an aspect, the invention relates to an anti-wrinkle under eye composition comprising:
a) peptides
b) a flavonoid,
c) a chelating agent,
d) a skin lightening agent,
e) an exfoliating agent and
f) a skin protectant
In one of the embodiments, the peptides are a mixture of tripeptide and a tetrapeptide.
In a preferred embodiment the tripeptide is N-Acyl-Gly-His-Lys and more preferably N-Palmitoyl-Gly-His-Lys.
In a preferred embodiment the tetrapeptide is N-Acyl- Gly-Gln-Pro-Arg and more preferably N-palmitoyl-Gly-Gln-Pro-Arg.
In one of the embodiments, the flavonoid is chrysine.
In one of the embodiments, the chelating agent is N-hydroxysuccinimide.
In another embodiment the components a) to c) are in the form of a ready-to-use solution.
In a preferred embodiment the ready-to-use solution comprising components a) to c) comprises water, glycerin and steareth-20.
In one of the embodiments, the skin lightening agent is diacetyl boldine.
In a preferred embodiment, the skin lightening agent is in the form of a ready-to-use solution comprising diacetyl boldine and caprylic/capric triglyceride
In one of the embodiments, the exfoliating agent is in the form of a ready-to-use solution comprising grapefruit extract, lemon fruit extract, tomato extract, bilberry extract, citric acid and lactic acid.
In one of the embodiments, the skin protectant is in the form of powder comprising a blend of allantoin and glycyrrhetinic acid.
In an aspect, the anti-wrinkle under eye composition of the invention may further comprise at least one dermatologically acceptable excipients selected from the group consisting of solvents, emulsifying agents, gelling agents/ thickening agents, neutralizers, buffering agents, humectants/ moisturizers, film-forming agents, antioxidants, chelating agents, preservatives, emollients and the like.
In an aspect, the anti-wrinkle under eye composition of the invention is used for the treatment of periorbital hyperpigmentation or wrinkles under the eye.
In an aspect, the process for preparing an anti-wrinkle under eye composition of the invention comprises:
a) Preparing an oil phase
b) Preparing an aqueous phase comprising exfoliating agent.
c) Adding the oil phase to the aqueous phase with stirring and homogenization
d) Adding the Haloxyl®, and Lumiskin® during cooling
e) Adjusting pH and volume
f) Cooling the bulk to room temperature.
DETAILED DESCRIPTION OF INVENTION
All publications cited herein are hereby incorporated by reference in their entirety.
The anti-wrinkle under eye compositions of the present invention comprise combination of tri and tetra peptides and derivatives thereof, in amounts that are safe and effective to improve the visible sign of aging in human skin including fine lines, wrinkles, enlarged pores, roughness, dryness, and other skin texture defects such as stretch marks (as caused by pregnancy, trauma or other influences, bags under the eyes, also called "puffy eyes" and dark (under eye) circles, both caused by thinning of the skin, insufficient blood circulation and slack tissue. These peptides can stimulate the production of certain advantageous biomolecules, such as, without limitation, collagen I, fibronectin, collagen IV and hyaluronic acid, in skin cells. As used herein, "peptides" refers to both the naturally occurring peptides and synthesized peptides. Also useful herein are naturally occurring and commercially available compositions that contain peptides.
Chrysin (5,7-dihydroxyflavone) is a fairly common flavonoid in the plant kingdom such as Pinus aristata, Prunus domestica, Pelargonium species, Pinaceae species including Pinus, Passiflora species (Passiflora coerulea L., Passiflora incarnata) including tropical Passion fruit, propolis, Daucus carota, Eriodictyon californicum, Eucalyptus globulus, Populus nigra, Populus tacamahacca, Prunus cerasus, Scutellaria baicalensis, Scutellaria galericulata, Spartium junceum, Ulmus sieboldiana, Flourensia resinosa, Oroxylum indicum. Its antioxidant properties and anti-inflammatory activity have been widely reported in the literature. Chrysin is basically an UGT enzyme inducing agent acting as detoxification-inducing agent. In particular, chrysin is used as an agent against rings under the eyes. Chrysin may be used to eliminate the hemoglobin degradation products which result in the formation of bilirubin (orange-colored pigment) which accumulates in the skin. The term "UGT enzyme inducing agents” used herein, mean any substance, simple or complex compound, of natural or synthetic origin, able to induce, stimulate or increase the activity of the UGT enzymes and/or able to induce, increase or accelerate the reaction catalyzed by that enzyme.
N-hydroxysuccinimide is a chelator or chelating agent. As used herein, "chelator" or "chelating agent" means an active agent capable of removing a metal ion from a system by forming a complex so that the metal ion cannot readily participate in or catalyze chemical reactions. The inclusion of a chelating agent is especially useful for providing protection against UV radiation which can contribute to excessive scaling or skin texture changes and against other environmental agents which can cause skin damage, in order to decrease the local iron load, which generates, as indicated above, a pro-oxidant situation and pigmentation.
Preferred commercially available ready-to-use solution of four active ingredients: tripeptide N-Palmitoyl-Gly-His-Lys (Pal-GHK), tetrapeptide N-Palmitoyl-Gly-Gln-Pro-Arg (Pal-GQPR), chrysin and N-hydroxysuccinimide in water, glycerin and steareth-20 is Haloxyl® manufactured by SEDERMA.
In a preferred embodiment, the amount of Haloxyl® is from about 0.5% to about 5% w/w, more preferably about 2.0% w/w of the anti-wrinkle under eye composition.
The anti-wrinkle under eye composition of present invention may further comprise additional chelating agents selected from disodium EDTA, NTA, deferoxamine, hydroxamic acids and their salts, phytic acid, phytate, gluconic acid and its salts, transferrine, lactoferrin.
In a preferred embodiment, the amount of chelating agent is form about 0.001% to about 5% w/w, preferably form about 0.01 to about 2% w/w, more preferably form about 0.05 to about 0.5% w/w of the anti-wrinkle under eye composition.
The compositions of the present invention may contain a skin lightening agent. Preferred skin lightening agent useful in compositions of the present invention is diacetyl boldine and derivatives thereof. In particular, diacetyl boldine reduces melanin production in an effective and non-toxic matter, block lipogenesis and present antioxidant activity. Preferred commercially available diacetyl boldine compositions include Lumiskin® manufactured by SEDERMA. Lumiskin® is a ready-to-use 0.1% by weight oily solution of diacetyl boldine in Caprylic/Capric triglyceride.
In a preferred embodiment, the amount of Lumiskin® is from about 0.5% to about 10% w/w, more preferably about 4.0% w/w of the anti-wrinkle under eye composition.
The compositions of the present invention may contain an exfoliating agent. Preferred commercially available exfoliating agent compositions include Acifructol® complex P63 Manufactured by GATTEFOSSE. Acifructol® complex P63 is a ready-to-use solution of grapefruit extract, lemon fruit extract, tomato extract, bilberry extract, citric acid and lactic acid.
In a preferred embodiment the proportion of Acifructol® complex P63 is from about 0.01% to about 5% w/w, preferably from about 0.1 to about 2.0% w/w, more preferably about 0.5% w/w of the anti-wrinkle under eye composition.
The compositions of the present invention may contain a skin protectant. Preferred commercially available skin protectant composition includes Alglycera® manufactured by Akema Fine Chemicals. Alglycera® is a blend of allantoin and glycyrrhetinic acid.
In a preferred embodiment the proportion of Alglycera® is from about 0.01% to about 2% w/w, preferably from about 0.05 to about 0.5% w/w, more preferably about 0.1% w/w of the anti-wrinkle under eye composition.
In one of the embodiment, anti-wrinkle under eye compositions of the present invention is in the form of an emulsion comprising an aqueous phase and an oil phase.
The anti-wrinkle under eye composition of the invention may further comprise at least one dermatologically acceptable excipients selected from the group consisting of solvents, emulsifying agents, gelling agents/ thickening agents, neutralizers, buffering agents, humectants/ moisturizers, film-forming agents, antioxidants, chelating agents, preservatives, emollients and the like.
Examples of solvents useful in the present invention include, but are not limited to, alcohols, esters, isopropyl palmitate, isopropyl myristate, mineral oils, dicaprylyl carbonate (Cetiol® CC), purified water, petrolatum and mixtures thereof.
In preferred embodiment the amount of the solvent is from about 0.5% to about 99% w/w, more preferably from about 50% to about 80%w/w of the anti-wrinkle under eye compositions.
Examples of emulsifying agents/emulsifiers useful in this invention include, but are not limited to, silicone emulsifiers, non-silicon-containing emulsifiers, and mixtures thereof, known by those skilled in the art for use in topical personal care products. A wide variety of silicone emulsifiers are useful herein as antifoaming agents. These silicone emulsifiers are typically organically modified organopolysiloxanes, also known to those skilled in the art as silicone surfactants. Useful silicone emulsifiers include dimethicone copolyols and dimethicone and cyclomethicone copolyol (DC® 3225 C) and mixtures thereof.
Nonlimiting examples of non-silicon-containing emulsifiers include polyethylene glycol 20 sorbitan monolaurate (Polysorbate 20), polyethylene glycol 5 soya sterol, Steareth-20, Ceteareth-20, PPG-2 methyl glucose ether distearate, Ceteth-10, Polysorbate 80, cetyl phosphate, potassium cetyl phosphate, diethanolamine cetyl phosphate, Polysorbate 60, glyceryl monostearate, blend of glyceryl monostearate and PEG-100 stearate (Arlacel™ 165), polyoxyethylene 20 sorbitan trioleate (Polysorbate 85), sorbitan monolaurate, sorbitan monostearate (Arlacel™ 60), polyoxyethylene 4 lauryl ether sodium stearate, polyglyceryl-4 isostearate, hexyl laurate, steareth-20, ceteareth-20, PPG-2 methyl glucose ether distearate, ceteth-10, diethanolamine cetyl phosphate, cetyl alcohol, liquid paraffins, lanolin alcohols, sorbitan monooleate (Tween™ 80), lecithin, sorbitan monoesters, such as sorbitan monoleate, sorbitan monolaurate, sorbitan monopalmitate, and sorbitan monostearate, polysorbates, such as those prepared from lauric, palmitic, stearic and oleic acids, cetomacrogol 1000, mononylphenyl ethers of polyethylene glycols, such as the monoxynols, polyoxyethylene monoesters, such as polyoxythylene monostearate, polyoxyethylene monolaurate, and polyoxyethylene monoleate, polyoxyethylene castor oil derivatives, polyoxyl 40 hydrogenated castor oil, dioctyl sodium sulfosuccinate, sodium lauryl sulfate, poloxamers having a molecular weight between 2,000 and 8,000, triethanolamine, and ureas such as diazolidinyl urea and mixtures thereof.
In a preferred embodiment the amount of the emulsifier is from about 0.1% to about 15% w/w of the anti-wrinkle under eye composition.
Examples of gelling agents/ thickening agents useful in this invention include, but are not limited to, carbomers (Carbopol® products) such as Carbopol® ETD 2020, Carbopol® 980, Carbopol® 974P, Carbopol® Ultrez, polyethylene oxides, ammonium methacrylates, carrageenan, cellulose acetate phthalate aqueous products such as CAPNF from Eastman, carboxymethyl cellulose sodium, carboxy polymethylene, cellulose, cellulose acetates (microcrystalline), cellulose polymers, divinylbenzene styrene copolymers, ethyl celluloses, ethylene vinyl acetate, silicone, polyisobutylene, shellac, guar gum, guar rosin, cellulose derivatives such as hydroxyethyl celluloses, hydroxymethyl celluloses, hydroxypropyl celluloses, hydroxypropyl methylcelluloses, carboxymethyl celluloses, and methyl celluloses, hypromellose phthalates (hydroxypropyl methylcellulose phthalate), methyl acrylate, microcrystalline wax, polyvinyl alcohols, polyvinyl acetates, polyvinyl acetate phthalates such as Suretic from Colorcon, polyvinylpyrrolidones (PVP), PVP ethyl celluloses, acrylates, PEG/PVP, xanthan gum, trimethyl siloxysilicate, maleic acid/anhydride copolymers, polacrilin, poloxamers, polyethylene oxides, polyglactic acid/poly-l-lactic acid, terpene resin, locust bean gum, prolamines (e.g., zein), acrylic copolymers, polyurethane dispersions, gelatin (both type A and type B from various sources such as pigs, cattle, and fish), dextrin, starch, polyvinyl alcohol-polyethylene glycol copolymers, methyacrylic acid-ethyl acrylate copolymers such as Kollicoat polymers from BASF, methacrylic acid and methacrylate based polymers, e.g., poly(methacrylic acid) copolymers and methylmethacrylate copolymers, including Eudragit polymers from Evonik Industries (Eudragit E, L, NE, RL, RS, S100), esters of polyvinylmethylether/maleic anhydride copolymers such as Gantrez™ ES-425, Gantrez™ ES-225 available from ISP, Pemulen™ TR1, Sepineo™ P600, Tinovis® ADE and any mixtures thereof. Other polymers are also suitable for use as gel-forming agents, depending on the solvent vehicle components, the drug, and the specific functional requirements of the given formulation and mixtures thereof.
In a preferred embodiment the proportion of gelling agents is from about 0.01% to about 5%w/w, more preferably from about 0.1% to about 3% w/w of the anti-wrinkle under eye composition.
Examples of neutralizers useful in this invention include, but are not limited to sodium hydroxide, potassium hydroxide, triethylamine, diethanolamine, triethanolamine and other dermatologically acceptable neutralizing agents and mixtures thereof.
In a preferred embodiment the amount of neutralizers is from about 0.01% to about 1% w/w of the anti-wrinkle under eye composition.
Examples of buffering agent useful in this invention include, but are not limited to phosphates such as monobasic sodium phosphate, and dibasic sodium phosphate, glycine, citric acid, ascorbic acid, citrate, acetate and other dermatologically acceptable buffering agents any mixtures thereof.
In a preferred embodiment the amount of buffering agent is from about 0.001% to about 1%w/w, more preferably from about 0.01% to about 0.05% w/w of the anti-wrinkle under eye composition.
Examples of humectants/moisturizers useful in this invention include, but are not limited to: polyhydroxy alcohols such as sorbitol, glycerin, hexanetriol, propylene glycol, hexylene glycol, and the like; jojoba oil; ceramides; polyethylene glycols; sugars and starches; sugar and starch derivatives (e.g., alkoxylated glucose); D-panthenol; hyaluronic acid; lactamide monoethanolamine; acetamide monoethanolamine; 2-pyrrolidone-5-carboxylic acid; urea; and any mixtures thereof.
In a preferred embodiment the amount of humectants/moisturizers is from about 1% to about 20% w/w of the anti-wrinkle under eye composition.
Examples of film forming agents useful in this invention include, but are not limited to vinyl polymers, copolymers of vinylpyrrolidone and long-chain a-olefins such as vinylpyrrolidone/eicosene co-polymer (Antaron® V-220F), butylated polyvinyl pyrrolidones, vinylpyrrolidone-dimethylaminoethylmethacrylate copolymers, triacontanyl PVP, polyquaternium-55, diethyl phthalate, dibutyl adipate, dibutyl phthalate and any mixtures thereof.
In a preferred embodiment the amount of film forming agents is from about 0.01% to about 1%w/w, more preferably from about 0.1% to about 0.5% w/w of the anti-wrinkle under eye composition.
Examples of antioxidants useful in this invention include, but are not limited to butylated hydroxytoluene (BHT), ascorbyl palmitate, butylated hydroxyanisole (BHA), ascorbic acid (Vitamin C), propyl gallate, and alpha-tocopherol (Vitamin E), vitamin E acetate, and any mixtures thereof.
In a preferred embodiment the amount of antioxidant is from about 0.01% to about 1% w/w of the anti-wrinkle under eye composition.
Examples of preservatives useful in this invention include, but are not limited to, alkyl esters of parahydroxybenzoic acid like methylparaben, ethylparaben, butylparaben, propylparaben and isobutylparaben, benzoates, hydantoin derivatives, propionate salts, sorbic acid, benzyl alcohol, imidazolidinyl urea, sodium dehydroacetate, pentylene glycol, o-phenylphenol, sodium o-phenylphenol, chlorocresol, salicylic acid, sodium salicylate, magnesium salicylate, resorcin, chloroxylenol, thymol, triclosan, cresols, benzalkonium chloride, benzethonium chloride, cetylpyridium chloride, benzoic acid, sodium benzoate, sorbic acid, dehydroacetic acid, sodium dehydroacetate, chlorhexidine, chlorhexidine gluconate, chloramine T, triclocarban, iodopropynyl butylcarbanate, chlorobutanol, chlorphenesin, hinokitol, silver chloride, zinc pyrithione, alkyldiaminothylglycine hydrochloride, glycerol caprylate, and any mixtures thereof. Appropriate preservatives can be chosen to satisfy a preservative challenge test and to provide product stability.
In a preferred embodiment the amount of preservatives is from about 0.01% to about 1% w/w of the anti-wrinkle under eye composition.
The compositions of the present invention may also contain at least one emollient. Useful emollients include, but are not limited to, white petrolatum, light mineral oil, cetyl alcohol, stearyl alcohol, cetostearyl alcohol, volatile silicone oils, non-volatile emollients, and mixtures thereof. Examples of volatile silicone oils useful herein include: Dow Corning 344, Dow Corning 345, and Dow Corning 200 (manufactured by Dow Corning Corp.), Silicone 7207 and Silicone 7158 (manufactured by the Union Carbide Corp.), SF 1202 (manufactured by General Electric), and SWS-03314 (manufactured by SWS Silicones, Inc.). Examples of non-volatile emollients include hydrocarbons (e.g., the Permethyl products), propoxylated alcohols, non-volatile silicone oils, and mixtures thereof. Non-volatile silicone oils useful as emollient materials include polyalkylsiloxanes, polyalklyarylsiloxanes, and polyethersiloxane copolymers.
In a preferred embodiment the amount of emollient is from about 0.1% to about 10% w/w of the anti-wrinkle under eye composition.
Anti-wrinkle under eye compositions of the present invention can be part of a kit or device and be filled into tubes, jars, bottles, aerosol containers, and any other forms of packaging that will allow ease of application topically around the eye area. The formulations are meant to be applied topically, either manually or by using a convenient applicator preferably a long nozzle coex LDPE tube, for patient compliance and ease of application. The dose, and number and frequency of applications can be decided by a person skilled in the art of treating conditions, such as a physician, a dermatologist, and the like.
In embodiments, the invention includes forms of packaging for the anti-wrinkle under eye composition, such that skin protection characteristics of the formulations are maintained during transportation, storage, and use for commercially relevant times (e.g., 6 months, 12 months, 24 months, or intermediate or longer periods).
The anti-wrinkle under eye composition of the present invention is stable over 12 months at 40°C / 75% RH.
Certain specific aspects and embodiments of the invention will be explained in more detail with reference to the following examples, being provided only for purposes of illustration, and it is to be understood that the present invention is not deemed to be limited thereto.
Example 1
Sr. No. Ingredients Amount (%w/w)
1. Haloxyl® 2.00
2. Lumiskin® 4.00
3. Jojoba oil 3.75
4. Light mineral oil 1.50
5. Dicaprylyl carbonate (Cetiol® CC) 1.50
6. Vinyl pyrrolidone/eicosene co-polymer (Antaron® V-220 F) 0.20
7. Cetyl alcohol 2.50
8. Glyceryl stearate and PEG 100 stearate (ArlacelTM 165) 0.65
9. Alglycera® 0.10
10. Cetomacrogol 1000 2.30
11. Sorbitan monostearate (ArlacelTM 60) 1.35
12. Cyclomethicone and dimethicone copolyol (DC® 3225 C) 2.00
13. Methyl paraben 0.10
14. Propyl paraben 0.20
15. Butylated hydroxytoluene 0.10
16. Butylated hydroxyanisole 0.10
17. Ascorbyl palmitate 0.02
18. Carbopol® ETD 2020 0.20
19. Acifructol® complex P63 0.50
20. Disodium EDTA 0.10
21. Glycerin 7.00
22. Sodium dihydrogen phosphate monohydrate 0.02
23. Sodium hydroxide 0.20
24. Purified water 69.61
Manufacturing process:
Oil Phase
a) Preparing an oil phase by combining jojoba oil, light mineral oil, cetyl alcohol, glyceryl stearate, PEG 100 stearate, sorbitan monostearate, dicaprylyl carbonate, cetomacrogol 1000 and vinyl pyrrolidone/eicosene co-polymer while maintaining the temperature at 70±5°C.
b) Adding methyl paraben, propyl paraben, butylated hydroxyanisole, butylated hydroxytoluene, ascorbyl palmitate and cyclomethicone and dimethicone copolyol to oil phase while maintaining the temperature at 70±5°.
Aqueous Phase
c) Preparing an aqueous phase by heating purified water to about 70±5°C and sequentially adding sodium dihydrogen phosphate, disodium EDTA, acifructol® complex P63 and carbopol, then stirring to achieve homogeneity while maintaining 70±5°C.
Mixing
d) Adding the oil phase to the aqueous phase with stirring, with homogenizing at high speed.
e) Dispersing Alglycera® in glycerin by heating up to 65±5°C, then mixing to the bulk of step d) under homogenization.
f) Cooling the bulk to 42±2°C under stirring and adding Lumiskin® to the bulk of step e).
g) Cooling the bulk to 37±2°C under stirring and adding Haloxyl® to the bulk of step f).
h) Dissolving sodium hydroxide in purified water and adding to the bulk of step g) with stirring for neutralization and to get desired pH.
i) Allowing the bulk to cool to room temperature under stirring.
Example 2
S.No. Ingredients Amount (%w/w)
1 Haloxyl® 2.0
2 Lumiskin® 4.0
3 Jojoba oil 5.0
4 Light mineral oil 2.0
5 Cetyl alcohol 1.5
6 Polyoxyl 40 hydrogenated castor oil 0.2
7 Alglycera® 0.1
8 Cyclomethicone and dimethicone copolyol (DC® 3225 C) 2.0
9 Sorbitan monostearate (ArlacelTM 60) 3.0
10 Cetomacrogol 1000 2.0
11 Vinyl pyrrolidone/eicosene co-polymer (Antaron® V-220 F) 1.0
12 Dicaprylyl carbonate (Cetiol® CC) 2.0
13 Acifructol® complex P63 1.0
14 Glycerine 7.0
15 Carbopol® ETD 2020 0.07
16 Vitamin E acetate 0.02
17 Methylparaben 0.1
18 Propylparaben 0.2
19 Ascorbyl palmitate 0.1
20 Disodium EDTA 0.05
21 Butylated hydroxyanisole 0.1
22 Trolamine 0.56
24 Purified water 65.9
Manufacturing process:
OIL PHASE
a) Preparing an oil phase by combining jojoba oil, light mineral oil, cetyl alcohol, sorbitan monostearate, dicaprylyl carbonate, polyoxyl 40 hydrogenated castor oil, cetomacrogol 1000 and vinyl pyrrolidone/eicosene co-polymer while maintaining the temperature at 70±5°C.
b) Adding methyl paraben and propyl paraben, butylated hydroxyanisole, vitamin E acetate, ascorbyl palmitate and dimethicone and cyclomethicone copolyol to oil phase while maintaining the temperature at 70±5°C.
AQUEOUS PHASE
c) Preparing an aqueous phase by heating purified water to about 70±5°C and sequentially adding disodium EDTA, and carbopol, then stirring to achieve homogeneity while maintaining 70±5°C.
MIXING
d) Adding the oil phase to the aqueous phase with stirring, with homogenizing at high speed.
e) Adding glycerin and Alglycera® dispersion to bulk of step d) and homogenizing.
f) Cooling the bulk to 45+2 °C under stirring.
g) Adding Lumiskin®, Acifructol® complex P63 and Haloxyl® to the bulk of step f).
h) Adding trolamine solution to the bulk of step g) with stirring for neutralization and to get desired pH.
i) Allowing the bulk to cool to room temperature under stirring.
Example 3
S.No. Ingredients Amount (%w/w)
1 Haloxyl® 2.0
2 Lumiskin® 4.0
3 Jojoba oil 5.0
4 Light mineral oil 2.0
5 Cetyl alcohol 1.5
6 Polyoxyl 40 hydrogenated castor oil 0.2
7 Alglycera® 0.1
8 Dicaprylyl carbonate (Cetiol® CC) 2.0
9 Cetomacrogol 1000 2.0
10 Cyclomethicone and dimethicone copolyol (DC® 3225 C) 2.0
11 Glycerine 7.0
12 Sorbitan monostearate (ArlacelTM 60) 3.0
13 Vinyl pyrrolidone/eicosene co-polymer (Antaron® V-220 F) 1.0
14 Acifructol® complex P63 0.5
15 Carbopol® ETD 2020 0.07
16 Methylparaben 0.1
17 Propylparaben 0.2
18 Ascorbyl palmitate 0.02
19 Vitamin E acetate 0.002
20 Citric acid 0.1
21 Ascorbic acid 0.2
22 Disodium EDTA 0.05
23 Butylated hydroxyanisole 0.1
24 Butylated hydroxytoluene 0.1
25 Trolamine q.s.
26 Purified water 66.758
OIL PHASE
a) Preparing an oil phase by combining jojoba oil, light mineral oil, cetyl alcohol, sorbitan monostearate, dicaprylyl carbonate, polyoxyl 40 hydrogenated castor oil, cetomacrogol 1000 and vinyl pyrrolidone/eicosene co-polymer while maintaining the temperature at 70±5°C.
b) Add methyl paraben and propyl paraben, butylated hydroxyanisole, butylated hydroxytoluene, vitamin E acetate, ascorbyl palmitate and dimethicone and cyclomethicone copolyol to oil phase while maintaining the temperature at 70±5°C.
AQUEOUS PHASE
c) Preparing an aqueous phase by heating purified water to about 70±5°C and sequentially adding disodium EDTA, citric acid, ascorbic acid and carbopol under homogenization while maintaining the temperature at 70±5°C.
MIXING
d) Adding the oil phase to the aqueous phase with stirring, and homogenizing at high speed.
e) Dispersing Alglycera® in glycerin and heating up to 65±5°C, then mixing to the bulk of step d).
f) Cooling the bulk and to 45+2 °C and adding Lumiskin® to the homogenized bulk of step e)
g) Cooling the bulk and to 40+2 °C and adding Haloxyl® and Acifructol® complex P63.
h) Adding trolamine solution to the bulk of step g) with stirring for neutralization and to get desired pH.
i) Allowing the bulk to cool to room temperature under stirring.
We Claim:
1. An anti-wrinkle under eye composition comprising:
a) peptides
b) a flavonoid,
c) a chelating agent,
d) a skin lightening agent,
e) an exfoliating agent and
f) a skin protectant
2. The composition according to claim 1, wherein the peptides are mixture of tripeptide N-palmitoyl-Gly-His-Lys and a tetrapeptide N-palmitoyl-Gly-Gln-Pro-Arg
3. The composition according to claim 1, wherein the flavonoid is chrysine.
4. The composition according to claim 1, wherein the chelating agent is N-hydroxysuccinimide.
5. The composition according to claim 1, wherein the components a) to c) are in the form of a ready-to-use solution.
6. The composition according to claim 1, wherein the skin lightening agent is in the form of a ready-to-use solution comprising diacetyl boldine.
7. The composition according to claim 1, wherein the exfoliating agent is in the form of a ready- to-use solution comprising grapefruit extract, lemon fruit extract, tomato extract, bilberry extract, citric acid and lactic acid.
8. The composition according to claim 1, wherein the skin protectant is in the form of powder comprising a blend of allantoin and glycyrrhetinic acid.
9. The composition according to claim 1 may further comprise at least one dermatologically acceptable excipients selected from the group consisting of solvents, emulsifying agents, gelling agents/ thickening agents, neutralizers, buffering agents, humectants/ moisturizers, film-forming agents, antioxidants, chelating agents, preservatives, emollients.
10. The composition substantially as herein as described with reference to the fore going example.
| # | Name | Date |
|---|---|---|
| 1 | Complete Form 3.pdf | 2013-06-15 |
| 1 | Form-2.pdf | 2013-06-15 |
| 2 | Complete Form 5.pdf | 2013-06-15 |
| 3 | Complete Form 3.pdf | 2013-06-15 |
| 3 | Form-2.pdf | 2013-06-15 |