WO2012099899A2

WO2012099899A2 - Topical dermatological compositions for the treatment of acne

Info

Publication number: WO2012099899A2
Application number: PCT/US2012/021593
Authority: WO
Inventors: Gil DUBNIKOV
Original assignee: Innovative Cosmetics Ltd.; Feigelson, Daniel
Priority date: 2011-01-17
Filing date: 2012-01-17
Publication date: 2012-07-26
Also published as: WO2012099899A3

Abstract

There are disclosed dermatological topical pharmaceutical compositions for the treatment of acne, comprising an efficacious amount of quince seed jelly and a pharmaceutically acceptable carrier or excipient therefor. Methods of using the compositions, and other embodiments, are also disclosed.

Description

Topical Dermatological Compositions For the Treatment of Acne

[0001] This application claims priority from and the benefit of U.S. provisional patent application USSN 61/433302, filed January 17, 2011 and entitled "Topical Dermatological Compositions For the Treatment of Acne". The contents of this application are incorporated herein by reference.

BACKGROUND

[0002] Human skin contains many sebaceous glands just below the skin's surface. These glands produce sebum, a natural oil, that keeps the skin smooth and supple. Tiny pores in the skin allow the sebum to come to the skin's surface; hairs also project through these pores. In individuals with acne, the sebaceous glands produce excess sebum, and the dead skin cells lining the openings of the hair follicles (the tubes that hold the hair) are not shed properly and clog up the follicles. The combination of these two effects results in a build-up of oil in the hair follicles. This in turn causes blackheads and whiteheads to form. Although in some people, acne does goes no farther than this, in others the build-up of oil in the hair follicles creates an ideal environment for growth of the usually-present-and-generally-harmless bacterium

Propionibacterium acne. These bacteria feed off the sebum, and their growth produces substances that may elicit an immune response. When this occurs, the skin becomes inflamed, resulting in the redness associated with spots and blotches. In more severe inflammatory acne, cysts develop beneath the skin's surface. If these cysts rupture, the infection can spread. This can result in scars.

[0003] There is currently no absolute cure for acne, but various treatments can help to control the symptoms. Among the treatments currently used are:

Gently washing the affected area(s) with warm water and a mild soap twice a day to remove dead skin cells and excess oil;

Applying medication to the affected skin, such as a topical over-the-counter acne treatment containing benzoyl peroxide or salicylic acid, or prescription medications such as antimicrobials or retinoid;

administering oral antibiotics or oral contraceptives; and

Physical methods, such as comedo extraction or light therapy.

[0004] Published Patent Application US 7008647 suggests a cosmetic and dermatological composition for treating acne that uses one or more antimicrobial metals selected from silver, gold, platinum, and palladium but most preferably silver, preferably formed with atomic disorder, and preferably in a nanocrystalline form.

BRIEF STATEMENT OF EMBODIMENTS OF THE INVENTION

[0005] There is thus provided, in accordance with an embodiment of the invention, a deraiatological topical pharmaceutical composition for the treatment of acne, comprising an efficacious amount of quince seed jelly and a pharmaceutically acceptable carrier or excipient therefor.

[0006] In some embodiments, the composition is in the form of a lotion. In some embodiments, the composition is in the form of a gel. In some embodiments, the composition is in the form of a cream. In some embodiments, the composition is in the form of an ointment. In some embodiments, the composition is in the form of a paste. In some embodiments, the composition is in the form of a salve. In some embodiments, the composition is in the form of a foam. In some embodiments, the composition is in the form of a liquid. In some embodiments, the composition is in the form of an aerosol spray.

[0007] In some embodiments, the composition further comprises an emulsifier. In some embodiments, the composition further comprises a thickener. In some embodiments, the composition further comprises a penetration-enhancing or absorption aid agent. In some embodiments, the composition further comprises a buffering agent. In some embodiments, the composition further comprises an antioxidant. In some embodiments, the composition further comprises an emollient. In some embodiments, the composition further comprises a stabilizer. In some embodiments, the composition further comprises a fragrance. In some embodiments, the composition further comprises a skin softening agent. In some embodiments, the composition further comprises a tissue regenerating and/or protecting agent. In some embodiments, the composition further comprises a preservative. In some embodiments, the composition further comprises an additional active ingredient. In some embodiments, the additional active ingredient is selected from the group consisting of salicylic acid or a pharmaceutically acceptable salt thereof, sulfur, resorcinol or a pharmaceutically acceptable salt thereof, and combinations thereof.

[0008] In some embodiments, the composition is as follows:

Ingredient amount (wt. )

Water q.s.

Quince seed jelly 5.00-10.00

Propylene glycol 1.00-3.00

Glycerin 1.00-3.00

Polysorbate 20 1.00-2.00 SD alcohol 40 1.00-2.00

Triethanolamine 0.50-1.00

Carbomer (Carbopol) 1.00-2.00

Panthenol 0.50-1.00

Imidazolidinyl urea 0.10-0.30

Methylparaben 0.10-0.30

Allantoin 0.10-0.30

Propylparaben 0.10-0.20

Sea Salt (Dead Sea Minerals) 0.10-0.20

Tea Tree Oil 0.10-0.30

Aloe barbadensis leaf extract 0.10-0.30

Tocopheryl acetate 0.10-0.30

Hyaluronic Acid 0.10-0.20

Triclosan 0.10-0.30

Fragrance 0.10-0.30

[0009] In some embodiments, the composition is as follows:

[0010] In some embodiments, the composition is as follows:

Ingredient amount (wt.%)

Water q.s.

Quince seed jelly 5.00-10.00

Propylene glycol 1.00-3.00

Glycerin 1.00-3.00

Polysorbate 20 1.00-2.00

SD alcohol 40 1.00-2.00

Panthenol 0.50-1.00

Imidazolidinyl urea 0.10-0.30

Allantoin 0.10-0.30

Sea Salt (Dead Sea Minerals) 0.10-0.20

Tea Tree Oil 0.10-0.30 Aloe barbadensis leaf extract 0.10-0.30

Hyaluronic Acid 0.10-0.20

Triclosan 0.01-0.10

Hydroxethylcellulose 0.50-1.50

Salicylic acid 1.50-2.50

Sodium dehydroacetic acid, 0.20-0.50

Sodium benzoate 0.10-0.30

DMDM hydantoin 0.10-0.30

Fragrance 0.05-0.10

[0011] In some embodiments, the composition is as follov

Ingredient amount (wt. )

Water q.s.

Quince seed jelly 5.00-10.00

Cetyl alcohol 2.00-5.00

Caprylic/capric triglyceride 2.00-5.00

Propylene glycol 2.00-4.00

Glycerin 2.00-4.00

Lactic acid 0.10-0.30

Glyceryl stearate 2.00-5.00

PEG-40 stearate 2.00-5.00

Panthenol 0.50-1.00

Salicylic acid 1.50-2.50

Demethicone 0.50-2.50

Sea salt (Dead Sea Minerals) 0.10-0.30

Imidazolidinyl urea 0.10-0.30

Sorbitan tristearate 0.10-0.30

Allantoin 0.10-0.20

Tocopheryl acetate 0.10-0.20

Aloe barbadensis leaf extract 0.10-0.20

Fragrance 0.05-0.10

Phenoxyethanol 0.30-0.90

Propylparaben Up to 100

Ethylparaben 5.00-10.00

Methylparaben 2.00-5.00

Butylparaben 2.00-5.00

[0012] In some embodiments, the composition is a cream that comprises at least one of the following: cetyl alcohol, caprylic/capric triglyceride, propylene glycol, glycerin, lactic acid, glyceryl stearate, PEG-40 stearate, panthenol, salicylic acid, demethicone, sea salt (Dead Sea Minerals), imidazolidinyl urea, sorbitan tristearate, allantoin, tocopheryl acetate, Aloe barbadensis leaf extract, fragrance, phenoxyethanol, propylparaben, ethylparaben, methylparaben, butylparaben.

[0013] In some embodiments the composition is a gel that comprises at least one of the following: propylene glycol, glycerin, polysorbate 20, SD alcohol 40, panthenol, imidazolidinyl urea, allantoin, sea salt (Dead Sea Minerals), tea tree oil, Aloe barbadensis leaf extract, hyaluronic acid, triclosan, hydroxethylcellulose, salicylic acid, sodium dehydroacetic acid, sodium benzoate, DMDM hydantoin, fragrance, triethanolamine, carbomer, methylparaben, allantoin, tocopheryl acetate, triclosan.

[0014] There is also provided, in accordance with an embodiment of the invention, a method for treating or preventing acne, comprising applying to the skin of a patient in need of such treatment an efficacious amount of a dermatological topical pharmaceutical composition comprising quince seed jelly and a pharmaceutically acceptable carrier or excipient therefor. In some embodiments, the composition is a composition in accordance with an embodiment of the invention. In some embodiments, the composition is applied once daily. In some embodiments, the composition is applied at least twice daily. In some embodiments, the treatment is conducted for a period of at least one week. In some embodiments, the treatment is conducted for a period of at least two weeks.

DETAILED DESCRIPTION

[0015] In the context of this patent application, the term "quince seed jelly" refers to a jelly-like substance which is prepared by soaking seeds of the quince plant, viz. Cydonia oblonga, in water. Usually, soaking the seeds in water at room temperature for one to three hours is sufficient to prepare the jelly, although the seeds may also be soaked in water which is boiling or brought to a boil. The soaking process releases the mucilage from the seed coat, producing a mucilaginous mass having a jelly-like consistency. This substance, the "quince seed jelly", then serves as the basis for the preparation of formulations in accordance with some embodiments of the invention. It will be appreciated that while in some embodiments of the present invention, quince seeds may be used to prepare the "quince seed jelly", in other embodiments seeds of the flax (linseed) plant may be soaked in an analogous manner to yield "quince seed jelly".

[0016] It will be appreciated by those skilled in the art that in accordance with embodiments of the invention, the dermatological topical compositions may take various forms, such as lotions, gels, creams, ointments, pastes, salves, foams, liquid (e.g. aerosol) sprays and the like. Thus, skilled artisans will appreciate that in accordance with various embodiments, the compositions may contain one or more additional ingredients selected from, inter alia, emulsifiers; thickeners; penetration-enhancing agents/absorption aid agents; buffering agents; antioxidants; emollients; stabilizers, fragrances; skin softening agents; tissue regenerating and/or protecting agents; and preservatives. It will also be appreciated that additional active ingredients, such as antibiotic compounds suitable for topical dermal administration, may also be included in the compositions. In some embodiments, one or more of the additional ingredients are derived from natural sources. [0017] Skilled artisans will understand how to formulate compositions in accordance with embodiments of the invention; methods of formulating topical formulations for dermal administration are also described, for example, in Gennaro, ed., Remington: The Science and Practice of Pharmacy, 21st edition, Lippincott Williams & Wilkins, Philadelphia, 2005; Ansel et al., Pharmaceutical Dosage Forms and Drug Delivery Systems, 7th ed., Lippincott Williams & Wilkins Publishers (1999) (ISBN: 0683305727); and Kibbe (ed.), Handbook of Pharmaceutical Excipients American Pharmaceutical Association, 3rd ed. (2000) (ISBN: 091733096X), the contents of which are incorporated herein by reference.

[0018] Emulsifiers: As is appreciated by those skilled in the art, emulsifiers may be selected from nonionic, anionic, cationic, or amphoteric emulsifying agents, and may generally be selected to provide an oil-in- water or a water-in-oil emulsion. In embodiments of the present invention, emulsifiers may be present in an amount from about 0 to about 5.5% by weight.

[0019] Illustrative nonionic emulsifiers are alkoxylated compounds based on C₁₀-22 fatty alcohols and acids and sorbitan. These materials are available, for instance, from the Shell Chemical Company under the Neodol trademark. Copolymers of

polyoxypropylenepolyoxyethylene sold by the BASE Corporation under the Pluronic trademark are sometimes also useful. Alkyl polyglycosides available from the Henkel Corporation may also be utilized for purposes of this invention.

[0020] Anionic type emulsifiers include fatty acid soaps, sodium lauryl sulfate, sodium lauryl ether sulfate, alkyl benzene sulphonate, mono- and dialkyl acid phosphates, sarcosinates, taurates and sodium fatty acyl isethionate.

[0021] Amphoteric emulsifiers useful in the compositions in accordance with some

embodiments of the present invention include such materials such as dialkylamine oxide and various types of betaines (such as cocamidopropyl betaine).

[0022] Examples of emulsifiers include, for oil-in-water emulsions, phospholipids; surfactants such as free fatty acids, esters of fatty acids with polyoxyalkylene compounds like

polyoxypropylene glycol and polyoxyethylene glycol; ethers of fatty alcohols with

polyoxyalkylene glycols; esters of fatty acids with polyoxyalkylated sorbitan; soaps; glycerol- polyalkylene stearate; glycerol-polyoxyethylene ricinoleate; homo- and copolymers of polyalkylene glycols; polyethoxylated soya-oil and castor oil as well as hydrogenated derivatives; ethers and esters of sucrose or other carbohydrates with fatty acids, fatty alcohols, these being optionally polyoxyalkylated; mono-, di- and triglycerides of saturated or unsaturated fatty acids; glycerides or soya-oil and sucrose. Some suitable oil in water emulsifiers are Pemulen TR-1 (Acrylates/Cio-30 Alkyl Acrylate Crosspolymer-Noveon), Pemulen TR-2 (Acrylates/Cio-30 Alkyl Acrylate Crosspolymer-Noveon), ETD 2020 (Acrylates/Cio-30 Alkyl Acrylate Crosspolymer-Noveon), Carbopol 1382 (Acrylates/Cio-30 Alkyl Acrylate

Crosspolymer-Noveon), Natrosol CS Plus 330, 430, Polysurf 67 (Cetyl Hydroxyethyl Cellulose- Hercules), Aculyn 22 (Acrylates/Steareth-20 Methacrylate Copolymer-Rohm&Haas) Aculyn 25 (Acrylates/Laureth-25 Methacrylate copolymer-Rohm&Haas), Aculyn 28 (Acrylates/Beheneth- 25 Methacrylate copolymer-Rohm&Haas), Aculyn 46 (Peg-150/Stearyl Alcohol/SMDI copolymer-Rohm&Haas) Stabylen 30 (Acrylates/Vinyl Isodecanoate-3V), Structure 2001 (Acrylates/Steareth-20 Itaconate copolymer-National Starch), Structure 3001 (Acrylates/Ceteth- 20 Itaconate copolymer-National Starch), Structure Plus (Acrylates/Aminoacrylates/C 10-30 Alkyl Peg 20 Itaconate copolymer-National Starch, Quatrisoft LM-200 (Polyquaternium-24), polycarbonates, polyethers, polyethylenes, polypropylenes, polyvinyl chloride, polystyrene, polyamides, polyacrylates, cyclodextrins and mixtures thereof. Other suitable emulsifiers include sub-micron organic or inorganic particles absorbed at the interface. Examples of suitable particles include micronized zeolite, fumed silica, titanium dioxide, zinc oxide, and aluminum oxide. Suitable water-in-oil emulsifiers include stearic acid, palmitic acid, stearyl alcohol, behenyl alcohol, stearic acid, palmitic acid, the polyethylene glycol ether of stearyl alcohol having an average of about 1 to about 5 ethylene oxide units, the polyethylene glycol ether of cetyl alcohol having an average of about 1 to about 5 ethylene oxide units, and mixtures thereof; stearyl alcohol, cetyl alcohol, behenyl alcohol, the polyethylene glycol ether of stearyl alcohol having an average of about 2 ethylene oxide units (steareth-2), the polyethylene glycol ether of cetyl alcohol having an average of about 2 ethylene oxide units, and mixtures thereof; PEG-30 Dipolyhydroxystearate, Sorbitan Oleate and mixtures thereof. Furthermore, mixtures of anionic/amphoteric and nonionic surfactants may in some instances be used to make water-in-oil emulsions. These surfactants include ammonium lauryl sulfate, ammonium laureth sulfate, sodium lauryl sulfate, sodium laureth sulfate, sodium tridecyl sulfate, sodium trideceth sulfate, sodium C₁₂-i3 alkyl sulfate, sodium C_12-15 alkyl sulfate, sodium Cn-i5 alkyl sulfate, sodium C_12-18 alkyl sulfate, sodium C₁₀-i6 alkyl sulfate, sodium C_12-13 pareth sulfate, sodium C_12-13 pareth-n sulfate, and sodium C_12-14 pareth-n sulfate, sodium 3-dodecyl-aminopropionate, sodium 3- dodecylaminopropane sulfonate, sodium lauryl sarcosinate, N-alkyltaurines, cocoamidopropyl betaine, glyceryl monohydroxystearate, isosteareth-2, trideceth-3, hydroxystearic acid, propylene glycol stearate, PEG-2 stearate, sorbitan monostearate, glyceryl laurate, laureth-2, cocamide monoethanolamine, lauramide monoethanolamine, and mixtures thereof.

[0023] Thickening Agents: Thickening agents include dermatologically acceptable thickening agents as known in the art. Examples of thickening agents from natural sources are alovera, beeswax, coconut oil, guar gum, palm oil, and borax. Additional examples of thickeners include polyethylene glycol; glycerol; hydrophobic silicon oxides of the AEROSIL type, which are available from Degussa AG, such as AEROSIL^® OX50, AEROSIL^® 130, AEROSIL^® 150, AEROSIL^® 200, AEROSIL^® 300, AEROSIL^® 380, AEROSIL^® MOX 80, AEROSIL^® MOX 170, AEROSIL^® COK 84, AEROSIL^® R 202, AEROSIL^® R 805, AEROSIL^® R 812,

AEROSIL^® R 972, AEROSIL^® R 974 and AEROSIL^® R976; Cms monocarboxylic acid salts, such as calcium and magnesium salts of lauric acid, myristic acid, palmitic acid, oleic acid and stearic acid; crosslinked acrylates (e.g. Carbopol 982), hydrophobically-modified acrylates (e.g. Carbopol 1382), cellulosic derivatives and natural gums. Among useful cellulosic derivatives which may function as thickeners are sodium carboxymethylcellulose, hydroxypropyl methylcellulose, hydroxypropyl cellulose, hydroxyethyl cellulose, ethyl cellulose and hydroxymethyl cellulose. Suitable natural gums that may be used as thickeners include guar gum, xanthan gum, sclerotium, carrageenan, pectin, guar-guar, agar-agar, alginates, and combinations of these gums. Suitable thickeners also include polysaccharides, relatively high molecular weight polyethylene glycol mono- and diesters of fatty acids, polyacrylates, polyvinyl alcohol and polyvinylpyrrolidone. Amounts of the thickener may range from about 0 to about 5 wt.%.

[0024] Emollients: Emollients can be selected from polyols, esters and hydrocarbons. Suitable polyols may include propylene glycol, dipropylene glycol, polypropylene glycol, polyethylene glycol, sorbitol, hydroxypropyl sorbitol, hexylene glycol, 1,3-butylene glycol, 1,2,6-hexanetriol, glycerin, ethoxylated glycerin, propoxylated glycerin, xylitol and mixtures thereof.

[0025] Esters useful as emollients include alkyl esters of fatty acids having 10 to 20 carbon atoms, such as methyl, isopropyl, and butyl esters of fatty acids. Other examples include hexyl laurate, isohexyl laurate, isohexyl palmitate, isopropyl palmitate, decyl oleate, isodecyl oleate, hexadecyl stearate, decyl stearate, isopropyl isostearate, diisopropyl adipate, diisohexyl adipate, dihexyldecyl adipate, diisopropyl sebacate, lauryl lactate, myristyl lactate, and cetyl lactate, and C_12-15 alcohol benzoate esters.

[0026] Esters useful as emollients also include alkenyl esters of fatty acids having 10 to 20 carbon atoms. Examples thereof include oleyl myristate, oleyl stearate and oleyl oleate.

[0027] Esters useful as emollients also include ether-esters such as fatty acids esters of ethoxylated fatty alcohols.

[0028] Esters useful as emollients also include polyhydric alcohol esters. Ethylene glycol mono- and di-fatty acid esters, diethylene glycol mono- and di-fatty acid esters, polyethylene glycol (200 6000) mono- and di-fatty acid esters, polyglycerol poly-fatty esters, ethoxylated glyceryl monostearate, 1,3-butylene glycol monostearate, 1,3-butylene glycol distearate, polyoxyethylene polyol fatty acid ester, sorbitan fatty acid esters, and polyoxyethylene sorbitan fatty acid esters are satisfactory polyhydric alcohol esters.

[0029] Esters useful as emollients additionally include wax esters such as beeswax, spermaceti, myristyl myristate, stearyl stearate.

[0030] Esters useful as emollients still further include sterol esters, of which cholesterol fatty acid esters are examples thereof.

[0031] Emollients may be present in an amount from 0 to about 7.5 weight percent, preferably from about 1 to about 6 weight percent of the composition.

[0032] Penetration Enhancers/Absorption Aid Agents: Compositions in accordance with embodiments of the invention may include agents to aid in the absorption of the composition into the skin, in particular that facilitate penetration through the upper stratum corneum barrier to the deeper skin layers, for example by helping the quince seed jelly to penetrate into the skin, and/or by improving the solubility of the jelly in the composition. Absorption aids include dermatologically acceptable absorption aids as known in the art; examples from natural sources are jojoba oil and vegetable squalene. As is appreciated by those skilled in the art, some of the emulsifiers mentioned above may also function as penetration enhancers. Other examples of suitable penetration enhancers in clued a mixture of N-lauroyl sarcosine and oleic acid;

polyoxyethylene-9-lauryl ether, polyoxyethylene-20-cetyl ether; propylene glycol;

ethoxydiglycol; dimethyl isosorbide; urea; various alcohols such as ethanol, oleyl, and tetrahydrofuryl; alkyl sulfoxides such as dimethyl sulfoxide; dimethyl acetamide; dimethyl formamide; polyethylene glycol; pyrrolidones such as polyvinylpyrrolidone; urea; and various water-soluble or insoluble sugar esters such as Tween 80 (polysorbate 80) and Span 60 (sorbitan monostearate). The penetration enhancer/absorption aid agent may be present in an amount from 0 to about 4.5 weight percent, preferably from about 0.15 to about 2.75 weight percent of the composition.

[0033] Anti-Oxidants: Anti-oxidants include dermatologically acceptable anti-oxidants as known in the art. Examples of suitable anti-oxidants from natural sources are vitamin E, wheat germ oil, and safflower oil, carotenoids, Echinacoside and caffeoyl derivatives, grape seed extract, milk thistle extract, Silybum marianum, ginkgo biloba, green tea polyphenols, and the like, and mixtures thereof. Additional representative antioxidants include ascorbic acid, vitamin E, tocopheryl acetate, betaglucan, coenzyme Q10, butylated hydroxytoluene (BHT), superoxide dismutase, catalase, glutathione peroxidase, ascorbyl palmitate, dilauryl ascorbate, butylated hydroxyanisole, sodium meta bisulfite, ί-β-carotene, a-tocopherol, oligomeric proanthocyanidins or proanthanols, silymarin, carotenoids such as beta-carotene, canthaxanthin, zeaxanthin, lycopen, lutein, crocetin, capsanthin, and the like. Chelators of heavy metals, such as ethylenediamine tetraacetic acid (EDTA) can also be used. The anti-oxidant component may be present in an amount from about 0 to about 1 weight percent, preferably from about 0.01 to about 0.75 weight percent of the composition.

[0034] Skin Softening Agents: Skin softening agents include dermatologically acceptable skin softening agents as known in the art; examples of suitable skin softening agents from natural sources are sweet almond oil and sesame oil. Additional examples of suitable skin softening agents are glycerin, propylene glycol, caprylic/capric triglyceride, pantothenol and its derivatives and related moieties, and hyaluronic acid and related moieties. Skin softening agents may be present in an amount from about 0 to about 7.5 weight percent, preferably from about 0.15 to about 1.25 weight percent of the composition.

[0035] Tissue regenerating and/or protecting agents: Tissue regenerating and/or protecting agents include dermatologically acceptable tissue regenerating and/or protecting agents as known in the art. Examples of suitable tissue regenerating and/or protecting agents from natural sources are grape seed oil and sunflower oil. Tissue regenerating and/or protecting agents may be present in an amount from about 0 to about 5 weight percent, preferably from about 0.5 to about 2 weight percent of the composition.

[0036] Preservatives: Preservatives include dermatologically acceptable preservatives as known in the art, which are useful to prevent microbial contamination; examples of suitable

preservatives from natural sources are paraben, tea tree oil (oil obtained from the leaf of Melaleuca alterniolia), thyme oil, grapefruit seed extract, and D-Alpha Tocopherol Acetate (Vitamin E). Additional examples include methyl paraben, propyl paraben, phenylethyl alcohol, benzyl alcohol, benzalkonium chloride, benzoic acid, or benzoates such as sodium benzoate, ethylenediaminetetraacetic acid (EDTA), and thimerosal. Preservatives may be present in an amount from about 0 to about 4 weight percent, preferably from about 0.15 to about 1 weight percent of the composition.

[0037] Further additional ingredients: In some embodiments, the composition further comprises dead sea minerals. These may be obtained commercially as dry salt or as a mud, see e.g.

www.deadseacosmetics.com or h ttp ://deadseami rs eral .com/, and contain, inter alia, chloride, bromide, sulfate, bicarbonate, calcium, sodium, potassium, zinc and magnesium ions. Dead Sea Minerals may be present in an amount from about 0 to about 1 weight percent, preferably from about 0.01 to about 0.25 weight percent of the composition. [0038] Compositions in accordance with embodiments of the invention may also contain humectants such as glycerol, propylene glycol (E 1520), glyceryl triacetate (E1518), sugar polyols like sorbitol (E420), xylitol and maltitol (E965), polymeric polyols like polydextrose (E1200), or natural extracts like quillaia (E999), lactic acid or urea. Humectants may be present in an amount from about 0 to about 8.5 weight percent, preferably from about 3 to about 6.5 weight percent of the composition.

[0039] In some embodiments, about 75-82 wt.% of the composition consists of a mixture of water (about 85-90 wt.%) and quince seed jelly (about 10-15 wt.%), with the remainder consisting of excipient(s) and/or other ingredient(s), such as anti-oxidants, skin softening agents, absorption aids, tissue regenerating and/or protecting agents, preservatives, and thickening agents; in general, in accordance with these embodiments, each additional ingredient constitutes not more than about 5 wt.% of the total.

[0040] In general, the compositions may be prepared by taking quince seed jelly mixed in water, and mixing the additional ingredients into this. In some embodiments, the composition comprises about 75-85 wt.% quince seed jelly; and the remaining ingredients at the ranges set forth above between 15% up to 25% in the aggregate in wt.% of a mixture of dead sea minerals, Melaleuca alterniolia leaf oil (available from e.g. Essential Therapeutics, Hallam, Australia), anti-oxidants, skin softening agents, absorption aids, tissue regenerating and protecting agents, preservatives and thickening agents.

[0041] Examples of compositions in accordance with embodiments of the invention are the following:

[0042] Composition 1: A gel in accordance with embodiments of the invention may be prepared, containing ingredients in the following ranges:

Ingredient amount (wt.%) Function

Water q.s. Solvent

Quince seed jelly 5.00-10.00 Skin-Conditioning Agent

Propylene glycol 1.00-3.00 Humectant

Glycerin 1.00-3.00 Skin-Protectant

Polysorbate 20 1.00-2.00 Solubilizing Agent

SD alcohol 40 1.00-2.00 Solvent

Triethanolamine 0.50-1.00 Ph Adjuster

Carbomer (Carbopol) 1.00-2.00 Viscosity Increasing Agent

Panthenol 0.50-1.00 Skin-Conditioning Agent

Imidazolidinyl urea 0.10-0.30 Preservative

Methylparaben 0.10-0.30 Preservative

Allantoin 0.10-0.30 Skin-Protectant

Propylparaben 0.10-0.20 Preservative

Sea Salt (Dead Sea Minerals) 0.10-0.20 Humectant

Tea Tree Oil 0.10-0.30 Antioxidant

Aloe barbadensis leaf extract 0.10-0.30 Skin-Conditioning Agent Tocopheryl acetate 0.10-0.30 Antioxidant

Hyaluronic Acid 0.10-0.20 Skin-Conditioning Agent

Triclosan 0.10-0.30 Biocide

Perfume 0.10-0.30 Fragrance

[0043] Thus a gel was prepared by mixing Carbopol into water until completely swollen. The remaining ingredients were then mixed in one after the other, taking care that each one was solubilized properly. The pH of the mixture was finally adjusted to 5.50-6.50 using triethanolamine. The gel had the following percentages of ingredients:

[0044] Composition 2: Another gel in accordance with embodiments of the invention may be prepared containing the following ingredients:

Ingredient amount (wt.%) Function

Water q.s. Solvent

Quince seed jelly 5.00-10.00 Skin-Conditioning Agent

Propylene glycol 1.00-3.00 Humectant

Glycerin 1.00-3.00 Skin-Protectant

Polysorbate 20 1.00-2.00 Solubilizing Agent

SD alcohol 40 1.00-2.00 Solvent

Panthenol 0.50-1.00 Skin-Conditioning Agent

Imidazolidinyl urea 0.10-0.30 Preservative

Allantoin 0.10-0.30 Skin-Protectant

Sea Salt (Dead Sea Minerals) 0.10-0.20 Humectant

Tea Tree Oil 0.10-0.30 Antioxidant

Aloe barbadensis leaf extract 0.10-0.30 Skin-Conditioning Agent

Hyaluronic Acid 0.10-0.20 Skin-Conditioning Agent

Triclosan 0.01-0.10 Biocide

Hydroxethylcellulose 0.50-1.50 Viscosity Increasing Agent

Salicylic acid 1.50-2.50 Antiacne Agent

Sodium dehydroacetic acid, 0.20-0.50 Preservative

Sodium benzoate 0.10-0.30 Preservative DMDM hydantoin 0.10-0.30 Preservative

Fragrance 0.05-0.10 Parfum

[0045] A gel having ingredients within these ranges was prepared by dispersing all ingredients, except hydroxyethylcellulose, into the water with the help of a propeller mixer until they were dissolved properly. Hydroxyethylcellulose was then added slowly to the mixture with continued mixing until the mixture was completely swollen.

[0046] Composition 3: A cream in accordance with embodiments of the invention may be prepared containing the following ingredients:

[0047] Such a cream was prepared by separately mixing the water- and oil- soluble ingredients and heating to 60°C in separate mixers. When all ingredients were dissolved in their mixers, the water phase was added to the oil phase, mixed thoroughly, and gradually cooled to 30°C.

[0048] Administration: In accordance with embodiments of the invention, compositions in accordance with embodiments of the invention may be applied as necessary to the skin of a patient in need to treatment or prevention of acne. The term "preventing" as used herein refers to administering a medicament beforehand to forestall or obtund an attack. The person of ordinary skill in the medical art (to which the present method claims are directed) recognizes that the term "prevent" is not an absolute term. In the medical art it is understood to refer to the prophylactic administration of a drug to substantially diminish the likelihood or seriousness of a condition, and this is the sense intended in applicants' claims. The reader's attention is directed to the Physician's Desk Reference, a standard text in the field, in which the term "prevent" occurs hundreds of times. No person of skill in the medical art construes the term in an absolute sense.

[0049] Clinical Study: 40 patients with mild to moderate acne were enrolled in a clinical study to test the efficacy of composition 2. The grading system used was based on 5 color

photographs of facial acne, which were ranked in order of type and number of acne lesions, namely: black comedons; white comedons; papules; pustules; and nodules/cysts. Patients of both genders, ages 18-35, with mild to moderate facial acne (as assessed per the Leeds Acne Grading Technique) were included in the study. Patients having known hypersensitivity to the ingredients in Composition 2, who had been treated with topical drugs in the four weeks prior to commencement of the study, who had received systemic antibiotics within the previous three months, who had received systemic retinoids in the previous six months, and who were pregnant or lactating were excluded from the study. The patients were divided into two groups of 20, the first group receiving Composition 2, the latter receiving a placebo, which was identical to Composition 2 but lacking the quince seed jelly. Patients were asked to apply the material twice daily following facial washing with soap. Patients were assessed at baseline and after two, four and six weeks of treatment, as well as two week post-treatment during follow-up visits. To determine overall improvement, patients were assessed at each visit, using a 0-5 grading scale as follows:

[0050] The compositions may be applied once every-other-day, once daily, twice daily, three times daily, four times daily or even more frequently, for a period ranging from a single day to several weeks, months or even years. In some embodiments the composition is applied twice daily. In some embodiments the treatment regimen is carried out for a period of at least two weeks. In some embodiments the treatment regimen is carried out for a period of at least four weeks. In some embodiments the treatment regimen is carried out for a period of at least six weeks. In some embodiments, the skin to which the composition is to be applied is cleaned with soap and water prior to application of the composition.

[0051] Clinical Study: 40 patients with mild to moderate acne were enrolled in a clinical study to test the efficacy of composition 2. The grading system used was based on 5 color

0 - condition worsened

1 - less than 25% insufficient response

2 - 25-49% mild response

3 - 50-74% moderate response

4 - 75-95% excellent improvement

5 - >95% total cure

[0052] At each visit, treatment tolerability was also scored as negative, mild, moderate or severe for each of the following parameters: stinging, erythema (redness), dry skin, itching, irritation, peeling, edema.

[0053] 26 patients completed the study, 14 having received the placebo and 12 having received Composition 2. The results are shown in the tables below:

After two weeks of treatment

After six weeks of treatment and two weeks of follow-up

[0054] Unless otherwise defined, all technical and scientific terms used herein have the same meanings as are commonly understood by one of ordinary skill in the art to which this invention belongs. Although methods similar or equivalent to those described herein can be used in the practice or testing of the present invention, suitable methods are described herein.

[0055] All publications, patent applications, patents, and other references mentioned herein are incorporated by reference in their entirety. In case of conflict, the patent specification, including definitions, will prevail. In addition, the materials, methods, and examples are illustrative only and not intended to be limiting.

[0056] It will be appreciated by persons skilled in the art that the present invention is not limited to what has been particularly shown and described hereinabove. Rather the scope of the present invention is defined by the general combination of parts that perform the same functions as exemplified in the embodiments, and includes both combinations and sub-combinations of the various features described hereinabove as well as variations and modifications thereof, which would occur to persons skilled in the art upon reading the foregoing description.

Claims

WHAT IS CLAIMED IS:

1. A dermatological topical pharmaceutical composition for the treatment of acne,

comprising an efficacious amount of quince seed jelly and a pharmaceutically acceptable carrier or excipient therefor.

2. A composition according to claim 1, wherein the composition is in the form of a lotion.

3. A composition according to claim 1, wherein the composition is in the form of a gel.

4. A composition according to claim 1, wherein the composition is in the form of a cream.

5. A composition according to claim 1, wherein the composition is in the form of an

ointment.

6. A composition according to claim 1, wherein the composition is in the form of a paste.

7. A composition according to claim 1, wherein the composition is in the form of a salve.

8. A composition according to claim 1, wherein the composition is in the form of a foam.

9. A composition according to claim 1, wherein the composition is in the form of a liquid.

10. A composition according to claim 9, wherein the composition is in the form of an aerosol spray.

11. A composition according to any of claims 1 to 10, further comprising an emulsifier.

12. A composition according to any of claims 1 to 11, further comprising a thickener.

13. A composition according to any of claims 1 to 12, further comprising a penetration- enhancing or absorption aid agent.

14. A composition according to any of claims 1 to 13, further comprising a buffering agent.

15. A composition according to any of claims 1 to 14, further comprising an antioxidant.

16. A composition according to any of claims 1 to 15, further comprising an emollient.

17. A composition according to any of claims 1 to 16, further comprising a stabilizer.

18. A composition according to any of claims 1 to 17, further comprising a fragrance.

19. A composition according to any of claims 1 to 18, further comprising a skin softening agent.

20. A composition according to any of claims 1 to 19, further comprising a tissue

regenerating and/or protecting agent

A composition according to any of claims 1 to 20, further comprising a preservative.

A composition according to any of claims 1 to 21, further comprising an additional active ingredient.

23. A composition according to claim 1 as follows:

A composition according to claim 23 as follows:

25. A composition according to claim as follows:

27. A composition according to claim 1 which is a cream that comprises at least one of the following: cetyl alcohol, caprylic/capric triglyceride, propylene glycol, glycerin, lactic acid, glyceryl stearate, PEG-40 stearate, panthenol, salicylic acid, demethicone, sea salt (Dead Sea Minerals), imidazolidinyl urea, sorbitan tristearate, allantoin, tocopheryl acetate, Aloe barbadensis leaf extract, fragrance, phenoxyethanol, propylparaben, ethylparaben, methylparaben, butylparaben.

28. A composition according to claim 1 which is a gel that comprises at least one of the

following: propylene glycol, glycerin, polysorbate 20, SD alcohol 40, panthenol, imidazolidinyl urea, allantoin, sea salt (Dead Sea Minerals), tea tree oil, Aloe barbadensis leaf extract, hyaluronic acid, triclosan, hydroxethylcellulose, salicylic acid, sodium dehydroacetic acid, sodium benzoate, DMDM hydantoin, fragrance, triethanolamine, carbomer, methylparaben, allantoin, tocopheryl acetate, triclosan.

29. A composition according to claim 22, wherein the additional active ingredient is selected from the group consisting of salicylic acid or a pharmaceutically acceptable salt thereof, sulfur, resorcinol or a pharmaceutically acceptable salt thereof, and combinations thereof.

30. A method for treating or preventing acne, comprising applying to the skin of a patient in need of such treatment an efficacious amount of a dermatological topical pharmaceutical composition comprising quince seed jelly and a pharmaceutically acceptable carrier or excipient therefor.

31. The method according to claim 30, wherein the composition is a composition according to any of claims 1 to 29.

32. The method according to claim 31, wherein the composition is a composition according to claim 1.

33. The method according to claim 31, wherein the composition is a composition according to claim 2.

34. The method according to claim 31, wherein the composition is a composition according to claim 3.

35. The method according to claim 31, wherein the composition is a composition according to claim 4.

36. The method according to claim 31, wherein the composition is a composition according to claim 5.

37. The method according to claim 31, wherein the composition is a composition according to claim 6.

38. The method according to claim 31, wherein the composition is a composition according to claim 7.

39. The method according to claim 31, wherein the composition is a composition according to claim 8.

40. The method according to claim 31, wherein the composition is a composition according to claim 9.

41. The method according to claim 31, wherein the composition is a composition according to claim 10.

42. The method according to claim 31, wherein the composition is a composition according to claim 11.

43. The method according to claim 31, wherein the composition is a composition according to claim 12.

44. The method according to claim 31, wherein the composition is a composition according to claim 13.

45. The method according to claim 31, wherein the composition is a composition according to claim 14.

46. The method according to claim 31, wherein the composition is a composition according to claim 15.

47. The method according to claim 31, wherein the composition is a composition according to claim 16.

48. The method according to claim 31, wherein the composition is a composition according to claim 17.

49. The method according to claim 31, wherein the composition is a composition according to claim 18.

50. The method according to claim 31, wherein the composition is a composition according to claim 19.

51. The method according to claim 31, wherein the composition is a composition according to claim 20.

52. The method according to claim 31, wherein the composition is a composition according to claim 21.

53. The method according to claim 31, wherein the composition is a composition according to claim 22.

54. The method according to claim 31, wherein the composition is a composition according to claim 23.

55. The method according to claim 31, wherein the composition is a composition according to claim 24.

56. The method according to claim 31, wherein the composition is a composition according to claim 25.

57. The method according to claim 31, wherein the composition is a composition according to claim 26.

58. The method according to claim 31, wherein the composition is a composition according to claim 27.

59. The method according to claim 31, wherein the composition is a composition according to claim 28.

60. The method according to claim 31, wherein the composition is a composition according to claim 29.

61. The method according to any of claims 30 to 60, wherein the composition is applied once daily.

62. The method according to any of claims 30 to 60, wherein the composition is applied at least twice daily.

63. The method according to any of claims 30 to 62, wherein the treatment is conducted for a period of at least one week.

64. The method according to claim 63, wherein the treatment is conducted for a period of at least two weeks.